AU2019278527A1 - Pyrazole derivative and harmful organism-controlling agent - Google Patents

Pyrazole derivative and harmful organism-controlling agent Download PDF

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AU2019278527A1
AU2019278527A1 AU2019278527A AU2019278527A AU2019278527A1 AU 2019278527 A1 AU2019278527 A1 AU 2019278527A1 AU 2019278527 A AU2019278527 A AU 2019278527A AU 2019278527 A AU2019278527 A AU 2019278527A AU 2019278527 A1 AU2019278527 A1 AU 2019278527A1
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group
alkyl
cycloalkyl
mono
alkyl group
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AU2019278527C1 (en
AU2019278527B2 (en
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Ryo Ishikawa
Akira KINPARA
Takeshi Matsuda
Masao Nakatani
Akira TAKANEZAWA
Keiji Toriyabe
Akira Watanabe
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Kumiai Chemical Industry Co Ltd
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Kumiai Chemical Industry Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/02—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing liquids as carriers, diluents or solvents
    • A01N25/04—Dispersions, emulsions, suspoemulsions, suspension concentrates or gels
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/12—Powders or granules
    • A01N25/14—Powders or granules wettable
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/30—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests characterised by the surfactants
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/56—1,2-Diazoles; Hydrogenated 1,2-diazoles
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/64—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
    • A01N43/66—1,3,5-Triazines, not hydrogenated and not substituted at the ring nitrogen atoms
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/64—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
    • A01N43/707—1,2,3- or 1,2,4-triazines; Hydrogenated 1,2,3- or 1,2,4-triazines
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
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    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/74—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
    • A01N43/76—1,3-Oxazoles; Hydrogenated 1,3-oxazoles
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/74—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
    • A01N43/78—1,3-Thiazoles; Hydrogenated 1,3-thiazoles
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/80—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
    • A01N47/02—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
    • A01N47/02—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom
    • A01N47/04—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom containing >N—S—C≡(Hal)3 groups
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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Abstract

The present invention provides a harmful organism-controlling agent having excellent safety, controlling effect, residual efficacy, etc. Provided are: a pyrazole derivative represented by general formula [1][where, p represents an integer of 0 or 1, R

Description

PYRAZOLE DERIVATIVE AND PEST CONTROL AGENT BACKGROUND OF THE INVENTION
Field of the Invention
[0001] The present invention relates to a novel pyrazole derivative or an
agriculturally acceptable salt thereof, and a pest control agent containing the derivative as an
active ingredient.
Description of the Related Art
[0002] Patent Document 1 indicates a pyrazole derivative having a pest
control effect, but lacks specific disclosure about a compound having a carboxylic amide at
the 3-position of the pyrazole ring.
[0003] Non-Patent Document 1 indicates a pyrazole derivative substituted
with a phenyl group at the 4-position of the pyrazole ring, but lacks the description about the
pest control activity of the pyrazole derivative.
[0004]
[Patent Document 1] WO 2012/102387 A
[0005]
[Non-Patent Document 1] International Journal of Chem Tech Research,
2013, Vol.5, No.1, pp 80-84
SUMMARY OF THE INVENTION
[0006] A pest control agent used for useful crops is requested to be an agent
that is applied to soil or foliage, and exhibits sufficient pest controlling effect with a low dose.
Also, increased demands for the safety and the influence on environment of chemicals lead to
the request for developing a safer pest control agent. Furthermore, in recent years, as a result
of long-term use of a pest control agent such as an insecticide or a miticide, pests having
acquired the resistance to the pest control agent have emerged, so that it becomes difficult to
completely control pests. Also, use of pest control agents having high mammalian toxicity is problematic in terms of the safety and the like for operators.
[0007] In light of the aforementioned circumstance, it is an object of the
present invention to solve the problems faced by the conventional pest control agents, and to
further provide a pest control agent that is excellent in safety, control effect, residual activity,
and the like.
[0008] In order to develop a pest control agent having desirable
characteristics as described above, the present inventors synthesized a variety of pyrazole
derivatives, and diligently examined the physiological activity of the pyrazole derivatives.
As a result, the present inventors found that a pyrazole derivative represented by the following
general formula [I] (hereinafter, referred to as the present compound) shows outstanding
effectiveness on various pests, and further continued the research to finally accomplish the
present invention.
[0009] That is, the present invention has the subject matter having the
following features.
[0010] (1) A pyrazole derivative represented by general formula [I] or an
agriculturally acceptable salt thereof
[Chemical formula 1]
R3 R2A
RG N R' R (CI)p
wherein,
p represents an integer of 0 or 1,
R', R2, R3, R 4, and R 5 each independently represent a hydrogen atom, halogen
atom, C 1 -C 6 alkyl group, hydroxy group, C 1-C 6 haloalkyl group, CI-C6 alkoxy group, C 1 -C6
haloalkoxy group, C3-C6 cycloalkyl group, C1-C6 alkylthio group, C1-C6 alkylsulfinyl group,
Ci-C 6 alkylsulfonyl group, amino group, mono(Ci-C6 alkyl)amino group, di(C1-C6
alkyl)amino group, cyano group, or nitro group,
A represents an oxygen atom or sulfur atom,
Q represents a halogen atom, or C6-Cio aryl group that is unsubstituted or substituted with (R8)m, or heteroaryl group that is unsubstituted or substituted with (R8)m,
R6 and R7 each independently represent a hydrogen atom, C1-C6 alkyl group, C 3
C 6 cycloalkyl group, C 3 -C 6 cycloalkyl Ci-C6 alkyl group, C 2-C 7 alkynyl group, C 2 -C 6
alkenyl group, hydroxy group, C1-C 6 alkoxy group, C1-C6 alkoxy C1-C6 alkyl group, C1-C6
haloalkyl group, 2-tetrahydrofuranyl group, 3-tetrahydrofuranyl group, 2-tetrahydropyranyl
group, 4-tetrahydropyranyl group, cyano Ci-C6 alkyl group, cyano C3-C6 cycloalkyl group,
hydroxy C1-C 6 alkyl group, formyl group, amino group, mono(C1-C6 alkyl)amino group,
di(Ci-C 6 alkyl)amino group, Ci-C6 alkylcarbonyl group, Ci-C6 alkoxy Ci-C6 alkylcarbonyl
group, C 3 -C 6 cycloalkylcarbonyl group, C 3 -C 6 cycloalkyl C1-C6 alkylcarbonyl group, C1-C6
alkoxycarbonyl group, carbamoyl group, mono(C1-C6 alkyl)aminocarbonyl group, di(C1-C6
alkyl)aminocarbonyl group, phenylcarbonyl group that is unsubstituted or substituted with
(R9),, C7-C13 aralkylcarbonyl group that is unsubstituted or substituted with (R 9)n,
pyridylcarbonyl group that is unsubstituted or substituted with (R9)n, pyrazolylcarbonyl group
that is unsubstituted or substituted with (R9), pyridine-2-ylmethyl group, pyridine-3
ylmethyl group, (Ci-C6 alkyl)thiocarbonyl group, (C-C6 alkoxy)thiocarbonyl group,
thiocarbamoyl group, mono(Ci-C6 alkyl)aminothiocarbonyl group, di(Ci-C6
alkyl)aminothiocarbonyl group, C1-C6 alkylsulfonyl group, sulfamoyl group, mono(C1-C6
alkyl)aminosulfonyl group, di(Ci-C6 alkyl)aminosulfonyl group, RioR"N-Ci-C 6 alkyl group,
Ci-C6 alkoxycarbonyl Ci-C6 alkyl group, aminocarbonyl Ci-C6 alkyl group, mono(Ci-C
alkyl)aminocarbonyl Ci-C6 alkyl group, mono(C3-C6 cycloalkyl)aminocarbonyl Ci-C6 alkyl
group, mono(C1-C6 haloalkyl)aminocarbonyl C1-C6 alkyl group, di(C1-C6
alkyl)aminocarbonyl Ci-C6 alkyl group, hydroxyimino group, C1-C6 alkoxyimino group,
hydroxyimino C1-C 6 alkyl group, or C1-C6 alkoxyimino C1-C6 alkyl group, R 6 and R7 may
together form =CR12N(R13)R14 or =CR12OR", and further, R 6 and R 7 may form together with carbon atoms bound thereto, a 3 to 6-membered carbon ring, or a 3 to 6-membered hetero ring having 1 to 4 hetero atoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, the hetero ring may be substituted a halogen atom, cyano group, nitro group, C1-C6 alkyl group, Ci-C6 alkoxy group, Ci-C6 haloalkyl group, or oxo group,
R 8 represents a hydrogen atom, halogen atom, hydroxy group, thiol group, C1-C6
alkyl group, C1-C6 haloalkyl group, C 3 -C 6 cycloalkyl group, C 3 -C 6 cycloalkyl C1-C6 alkyl
group, C 3 -C 6 cycloalkyl C 2 -C 6 alkynyl group, C 3 -C 6 halocycloalkyl group, C 3 -C 6
halocycloalkyl C1-C 6 alkyl group, C 2 -C 6 alkenyl group, C 2 -C 6 haloalkenyl group, C 2 -C 7
alkynyl group, C 2 -C 6 haloalkynyl group, C1-C6 alkoxy group, C1-C6 haloalkoxy group, C 3
C 6 cycloalkoxy group, oxirane-2-yl group, mono(oxirane-2-yl)Ci-C 3 alkyl group, C 3 -C
halocycloalkoxy group, C1-C 6 alkylthio group, C1-C6 alkylsulfinyl group, C1-C6
alkylsulfonyl group, C3-C6 cycloalkylthio group, C3-C6 cycloalkylsulfinyl group, C3-C
cycloalkylsulfonyl group, C1-C 6 haloalkylthio group, C1-C6 haloalkylsulfinyl group, C1-C6
haloalkylsulfonyl group, formyl group, C1-C6 alkylcarbonyl group, C1-C haloalkylcarbonyl
group, C1-C6 alkoxycarbonyl group, aminocarbonyl group, mono(C1-C6 alkyl)aminocarbonyl
group, di(Ci-C 6 alkyl)aminocarbonyl group, amino Ci-C6 alkyl group, mono(Ci-C
alkyl)amino C1-C6 alkyl group, di(Ci-C6 alkyl)amino C1-C6 alkyl group, tri(Ci-C
alkyl)silyloxy C1-C 6 alkyl group, C1-C6 alkylcarbonyl C1-C 6 alkyl group, Ci
C 6 alkylcarbonyloxy C1-C 6 alkyl group, C1-C6 haloalkylcarbonyl C1-C 6 alkyl group, C1-C6
alkoxycarbonyl Ci-C6 alkyl group, hydroxy Ci-C6 alkyl group, Ci-C6 alkoxy Ci-C6 alkyl
group, C1-C 6 haloalkoxy C1-C 6 alkyl group, C1-C6 alkoxy C1-C6 haloalkyl group, C1-C6
haloalkoxy Ci-C6 haloalkyl group, formyloxy group, Ci-C6 alkylcarbonyloxy group, Ci-C6
haloalkylcarbonyloxy group, aminocarbonyloxy group, mono(C-C6 alkyl)aminocarbonyloxy
group, di(Ci-C6 alkyl)aminocarbonyloxy group, aminocarbonyloxy Ci-C6 alkyl group,
mono(C1-C6 alkyl)aminocarbonyloxy C1-C 6 alkyl group, di(C-C6 alkyl)aminocarbonyloxy
Ci-C 6 alkyl group, Ci-C6 alkoxycarbonyloxy group, Ci-C6 alkoxycarbonyloxy Ci-C6 alkyl
group, C1-C6 alkylsulfonyloxy group, C1-C6 haloalkylsulfonyloxy group, C1-C6 alkylthio
Ci-C6 alkyl group, Ci-C6 alkylsulfinyl Ci-C6 alkyl group, Ci-C6 alkylsulfonyl Ci-C6 alkyl group, C1-C6 haloalkylthio C1-C6 alkyl group, C1-C haloalkylsulfinyl C1-C6 alkyl group,
Ci-C 6 haloalkylsulfonyl Ci-C6 alkyl group, C3-C6 cycloalkyl Ci-C6 alkoxy group, C3-C6
halocycloalkyl C1-C 6 alkoxy group, C 3 -C 6 cycloalkyl C1-C6 alkylthio group, C 3-C
cycloalkyl Ci-C6 alkylsulfinyl group, C3-C6 cycloalkyl Ci-C alkylsulfonyl group, C3-C
halocycloalkyl C1-C 6 alkylthio group, C 3 -C 6 halocycloalkyl C1-C6 alkylsulfinyl group, C 3
C 6 halocycloalkyl C1-C 6 alkylsulfonyl group, phenyl group that is unsubstituted or substituted
with (R9), phenoxy group that is unsubstituted or substituted with (R9), benzyl group that is
unsubstituted or substituted with (R9), benzyloxy group that is unsubstituted or substituted
with (R9 ), amino group, mono(Ci-C6 alkyl)amino group, di(Ci-C6 alkyl)amino group,
carboxy group, 1,3-dioxolane-2-yl group, 1,3-dioxane-2-yl group, 1H-imidazole-2-yl group,
thiazole-2-yl group, oxazole-2-yl group, (hydroxyimino)methyl group,
(methyloxyimino)methyl group, isoxazole-3-yl, 4,5-dihydro-3-isoxazolyl group, cyano group,
or nitro group, and further, neighboring two R8 s may form, together with a carbon atom
bound to each R8, a 4 to 8-membered carbon ring, or a 4 to 8-membered hetero ring having 1
to 4 hetero atoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, the
carbon ring or hetero ring formed at this time may be substituted with one or more chemically
acceptable substituents selected from a halogen atom, cyano group, nitro group, C1-C6 alkyl
group, C1-C 6 haloalkyl group, C1-C6 alkoxy group, C1-C6 haloalkoxy group, or oxo group,
R9 represents a halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6
alkoxy group, Ci-C 6 haloalkoxy group, Ci-C6 alkylthio group, Ci-C alkylsulfinyl group,
Ci-C 6 alkylsulfonyl group, Ci-C6 haloalkylthio group, C1-C6 haloalkylsulfinyl group, C1-C6
haloalkylsulfonyl group, amino group, mono(Ci-C6 alkyl)amino group, di(Ci-C6 alkyl)amino
group, cyano group, or nitro group,
R 10 and R" each independently represent a hydrogen atom, Ci-C6 alkyl group,
Cl-C 6 haloalkyl group, or C 3 -C 6 cycloalkyl group, and further, R10 and R 1 may form,
together with carbon atoms bound thereto, a 3 to 6-membered ring,
R 12 represents a hydrogen atom, C1-C6 alkyl group, or C 3 -C cycloalkyl group,
R 13 and R 14 each independently represent a hydrogen atom, Ci-C6 alkyl group,
C 1-C 6 haloalkyl group, C 3-C 6 cycloalkyl group, or C1-C 6 alkoxy group, and further, R13 and
R14 may form, together with carbon atoms bound thereto, a 3 to 6-membered carbon ring, or a
3 to 6-membered hetero ring having 1 to 4 hetero atoms selected from an oxygen atom, a
sulfur atom, and a nitrogen atom,
R 1 5 represents a C1 -C 6 alkyl group,
m represents a number of chemically acceptable R 8s and is an integer of 0 to 7,
R 8s may be the same or different from each other when m is 2 or more,
n represents a number of chemically acceptable R 9s and is an integer of 0 to 5,
and R9s may be the same or different from each other when n is 2 or more.
[0011] (2)
A pyrazole derivative represented by general formula [II] or an agriculturally
acceptable salt thereof
[Chemical formula 2]
R3 R2 N OR 16
R4 NO' N () R' R5
[11] wherein, p represents an integer of 0 or 1,
R 1, R 2, R 3, R4, and R each independently represent a hydrogen atom, halogen
atom, CI-C6 alkyl group, hydroxy group, C1-C6 haloalkyl group, CI-C6 alkoxy group, C1-C6
haloalkoxy group, C3-C6 cycloalkyl group, C1-C6 alkylthio group, C1-C6 alkylsulfinyl group,
CI-C6 alkylsulfonyl group, amino group, mono(CI-C6 alkyl)amino group, di(CI-C6
alkyl)amino group, cyano group, or nitro group,
R 16 represents a hydrogen atom or CI-C6 alkyl group,
Q' represents a halogen atom, C1-C6 alkylsulfonyloxy group, C1-C6 haloalkylsulfonyloxy group, di(C1-C 6 alkyl)sulfamoyloxy group, phenylsulfonyloxy group that is unsubstituted or substituted with (R9),, C6-Cio aryl group that is unsubstituted or substituted with (R8)m, or heteroaryl group that is unsubstituted or substituted with (R8 )m,
R 8 represents a hydrogen atom, halogen atom, hydroxy group, thiol group, Ci-C6
alkyl group, C1-C6 haloalkyl group, C 3 -C 6 cycloalkyl group, C 3 -C 6 cycloalkyl C1-C6 alkyl
group, C 3 -C 6 cycloalkyl C 2 -C 6 alkynyl group, C 3-C 6 halocycloalkyl group, C 3 -C 6
halocycloalkyl C1-C 6 alkyl group, C 2-C 6 alkenyl group, C 2-C 6 haloalkenyl group, C 2 -C 7
alkynyl group, C 2 -C 6 haloalkynyl group, C1-C6 alkoxy group, C1-C6 haloalkoxy group, C 3
C 6 cycloalkoxy group, oxirane-2-yl group, mono(oxirane-2-yl)Ci-C3 alkyl group, C 3 -C 6
halocycloalkoxy group, Ci-C6 alkylthio group, Ci-C6 alkylsulfinyl group, Ci-C6
alkylsulfonyl group, C 3 -C 6 cycloalkylthio group, C 3 -C 6 cycloalkylsulfinyl group, C 3 -C
cycloalkylsulfonyl group, Ci-C6 haloalkylthio group, Ci-C6 haloalkylsulfinyl group, Ci-C6
haloalkylsulfonyl group, formyl group, C1-C6 alkylcarbonyl group, C1-C6 haloalkylcarbonyl
group, C1-C6 alkoxycarbonyl group, aminocarbonyl group, mono(C1-C alkyl)aminocarbonyl
group, di(C1-C 6 alkyl)aminocarbonyl group, amino C1-C 6 alkyl group, mono(C-C6
alkyl)amino Ci-C6 alkyl group, di(Ci-C6 alkyl)amino Ci-C6 alkyl group, tri(Ci-C6
alkyl)silyloxy Ci-C6 alkyl group, Ci-C6 alkylcarbonyl Ci-C6 alkyl group, Ci-C6
alkylcarbonyloxy Ci-C6 alkyl group, Ci-C6 haloalkylcarbonyl C1-C6 alkyl group, C1-C6
alkoxycarbonyl C1-C 6 alkyl group, hydroxy C1-C 6 alkyl group, C1-C6 alkoxy C1-C6 alkyl
group, Ci-C6 haloalkoxy Ci-C6 alkyl group, Ci-C6 alkoxy Ci-C6 haloalkyl group, Ci-C6
haloalkoxy C1-C6 haloalkyl group, formyloxy group, C1-C6 alkylcarbonyloxy group, C1-C6
haloalkylcarbonyloxy group, aminocarbonyloxy group, mono(Ci-C6 alkyl)aminocarbonyloxy
group, di(C1-C6 alkyl)aminocarbonyloxy group, aminocarbonyloxy C1-C6 alkyl group,
mono(Ci-C6 alkyl)aminocarbonyloxy Ci-C6 alkyl group, di(Ci-C6 alkyl)aminocarbonyloxy
Ci-C6 alkyl group, C1-C6 alkoxycarbonyloxy group, C1-C6 alkoxycarbonyloxy C1-C6 alkyl
group, C1-C6 alkylsulfonyloxy group, C1-C6 haloalkylsulfonyloxy group, C1-C6 alkylthio
C1-C 6 alkyl group, C1-C6 alkylsulfinyl C1-C6 alkyl group, C1-C6 alkylsulfonyl C1-C6 alkyl
group, Ci-C6 haloalkylthio Ci-C6 alkyl group, Ci-C6 haloalkylsulfinyl Ci-C6 alkyl group,
Ci-C 6 haloalkylsulfonyl C1-C6 alkyl group, C 3 -C 6 cycloalkyl C1-C6 alkoxy group, C 3-C 6
halocycloalkyl Ci-C6 alkoxy group, C3-C6 cycloalkyl Ci-C alkylthio group, C3-C
cycloalkyl C1-C6 alkylsulfinyl group, C 3 -C 6 cycloalkyl C1-C alkylsulfonyl group, C 3 -C
halocycloalkyl Ci-C 6 alkylthio group, C3-C6 halocycloalkyl Ci-C6 alkylsulfinyl group, C3
C 6 halocycloalkyl C1-C 6 alkylsulfonyl group, phenyl group that is unsubstituted or substituted
with (R9), phenoxy group that is unsubstituted or substituted with (R9), benzyl group that is
unsubstituted or substituted with (R9 ), benzyloxy group that is unsubstituted or substituted
with (R9 ), amino group, mono(Ci-C6 alkyl)amino group, di(Ci-C6 alkyl)amino group,
carboxy group, 1,3-dioxolane-2-yl group, 1,3-dioxane-2-yl group, 1H-imidazole-2-yl group,
thiazole-2-yl group, oxazole-2-yl group, (hydroxyimino)methyl group,
(methyloxyimino)methyl group, isoxazole-3-yl, 4,5-dihydro-3-isoxazolyl group, cyano group,
or nitro group, and further, neighboring two R8 s may form, together with a carbon atom
bound to each R8, a 4 to 8-membered carbon ring, or a 4 to 8-membered hetero ring having 1
to 4 hetero atoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, the
carbon ring or hetero ring formed at this time may be substituted with one or more chemically
acceptable substituents selected from a halogen atom, cyano group, nitro group, C1-C6 alkyl
group, Ci-C6 haloalkyl group, Ci-C6 alkoxy group, Ci-C6 haloalkoxy group, or oxo group,
R9 represents a halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6
alkoxy group, C1-C 6 haloalkoxy group, C1-C6 alkylthio group, C1-C alkylsulfinyl group,
Ci-C6 alkylsulfonyl group, Ci-C6 haloalkylthio group, Ci-C6 haloalkylsulfinyl group, Ci-C6
haloalkylsulfonyl group, amino group, mono(C1-C6 alkyl)amino group, di(C1-C6 alkyl)amino
group, cyano group, or nitro group,
m represents a number of chemically acceptable Rs and is an integer of 0 to 7,
R 8s may be the same or different from each other when m is 2 or more,
n represents a number of chemically acceptable R9 s and is an integer of 0 to 5,
and R9s may be the same or different from each other when n is 2 or more.
[0012] (3) A agrochemical composition including the pyrazole derivative or
an agriculturally acceptable salt thereof according to (1) or (2) as an active ingredient.
[0013] (4) The agrochemical composition according to (3), wherein the
agrochemical composition further includes a surfactant.
[0014] (5) A pest control agent including the pyrazole derivative or an
agriculturally acceptable salt thereof according to (1) or (2) as an active ingredient.
[0015] (6) The pest control agent according to (5) that is an insecticide.
[0016] (7) The pest control agent according to (5) having a control effect on a
pest in a dry field or a paddy field where a farming or gardening plant is cultured.
[0017] (8) The pest control agent according to (7), wherein the farming or
gardening plant is a plant provided with tolerance by a breeding method or a gene
recombination technique.
[0018] (9) A method for controlling a pest including using an active
ingredient amount of the pyrazole derivative or an agriculturally acceptable salt thereof
according to (1) or (2).
[0019] (10) A method for controlling a pest by letting a
agrochemical composition including the pyrazole derivative or an agriculturally acceptable
salt thereof according to (1) or (2) as an active ingredient act on a farming or gardening crop
or a place where the farming or gardening crop is to be grown or being grown, at once or in
batch.
[0020] (11) The method for controlling a pest according to (9) or (10),
wherein the place where the pest control agent is to be applied is a paddy field, a dry field, a
lawn, an orchard, a non-crop land, a greenhouse, a raising seeding facility, or a plant factory.
[0021] (12) The method for controlling a pest according to any one of (9) to
(11), wherein the pyrazole derivative or an agriculturally acceptable salt thereof is used as an
insecticide.
[0022] (13) A use method of a pest control agent, using the pest control agent
according to any one of (5) to (8) for controlling a pest for a farming or gardening crop.
[0023] The pest control agent containing the present compound shows
excellent controlling effect on a wide range of pests including Hemiptera pests, Lepidoptera pests, Coleoptera pests, Diptera pests, Hymenoptera pests, Orthoptera pests, Isoptera pests,
Thysanoptera pests, Acari pests, and plant parasitic nematoda, and is capable of controlling a
pest having acquired drug resistance.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0024] Symbols and terms used in this specification are described.
[0025] In the present invention, "pest control agent" means insecticides,
miticides, nematocides, and the like in farming and gardening fields, for animals such as
domestic animals and pets, for household use or for prevention of epidemics.
[0026] In the present invention, "halogen atom" refers to a fluorine atom, a
chlorine atom, a bromine atom, or an iodine atom.
[0027] In the present invention, unless otherwise specified, "C6-Cio aryl
group" refers to an aromatic hydrocarbon group having 6 to 10 carbon atoms, and examples
of the C6 -Cio aryl group include a phenyl, naphthalene--yl, or naphthalene-2-yl group.
[0028] In the present invention, unless otherwise specified, "heteroaryl
group" refers to an aromatic heterocyclic or condensed heterocyclic group, and examples of
the heteroaryl group include a pyrrolyl, furanyl, thienyl, pyrazolyl, oxazolyl, isoxazolyl,
imidazolyl, 1,2,4-oxadiazolyl, 1,2,3-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,4-triazolyl, 1,2,3
triazolyl, thiazolyl, isothiazolyl, 1,2,4-thiadiazolyl, 1,2,3-thiadiazolyl, 1,3,4-thiadiazolyl,
pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, benzofuranyl,
benzothienyl, indolyl, benzoxazolyl, benzoimidazolyl, benzotriazolyl, benzothiazolyl,
quinolinyl, quinazolinyl, quinoxalinyl, phthalazinyl, or naphthyridinyl group.
[0029] In the present invention, unless otherwise specified, "C1-C 3 alkyl
group" refers to a linear or branched alkyl group having 1 to 3 carbon atoms, and examples of
the C1-C 3 alkyl group include a methyl, ethyl, n-propyl, or isopropyl group.
[0030] In the present invention, unless otherwise specified, "C1-C6 alkyl
group" refers to a linear or branched alkyl group having 1 to 6 carbon atoms, and examples of
the C1-C6 alkyl group include, in addition to those exemplified in the "C1-C3 alkyl group", a n-butyl, s-butyl, isobutyl, tert-butyl, n-pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 1 ethylpropyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, neopentyl, n-hexyl, 1-methylpentyl, 2 methylpentyl, 3-methylpentyl, 4-methylpentyl, 1-ethylbutyl, 2-ethylbutyl, 1,1-dimethylbutyl,
1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3
dimethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-I-methylpropyl, or 1
ethyl-2-methylpropyl group.
[0031] In the present invention, unless otherwise specified, "C1-C6 haloalkyl
group" refers to a linear or branched alkyl group having 1 to 6 carbon atoms, substituted with
1 to 13 same or different halogen atoms, and refers to, for example, a haloalkyl group, and
examples of the Ci-C6 haloalkyl group include a fluoromethyl, difluoromethyl,
trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, bromomethyl,
dibromomethyl, tribromomethyl, iodomethyl, chlorodifluoromethyl, dichlorofluoromethyl, 1
fluoroethyl, 2-fluoroethyl, 1,1-difluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, 1,1,2,2
tetrafluoroethyl, pentafluoroethyl, 1-chloroethyl, 2-chloroethyl, 1,1-dichloroethyl, 2,2
dichloroethyl, 2,2,2-trichloroethyl, 1,1,2,2-tetrachloroethyl, pentachloroethyl, 1-bromoethyl,
2-bromoethyl, 2,2,2-tribromoethyl, 1-iodoethyl, 2-iodoethyl, 2-chloro-2,2-difluoroethyl, 2,2
dichloro-2-fluoroethyl, 1-fluoropropyl, 2-fluoropropyl, 3-fluoropropyl, 1,1-difluoropropyl,
2,2-difluoropropyl, 3,3-difluoropropyl, 3,3,3-trifluoropropyl, 2,2,3,3,3-pentafluoropropyl,
1,1,2,3,3,3-hexafluoropropyl, heptafluoropropyl, 1-fluoropropane-2-yl, 2-fluoropropane-2-yl,
1,1-difluoropropane-2-yl, 1,2-difluoropropane-2-yl, 1,3-difluoropropane-2-yl, 1,2,3
trifluoropropane-2-yl, 1,1,3,3-tetrafluoropropane-2-yl, 1,1,1,3,3,3-hexafluoropropane-2-yl,
heptafluoropropane-2-yl, 1-chloropropyl, 2-chloropropyl, 3-chloropropyl, 1,1-dichloropropyl,
2,2-dichloropropyl, 3,3-dichloropropyl, 3,3,3-trichloropropyl, 2,2,3,3,3-pentachloropropyl,
heptachloropropyl, 1-chloropropane-2-yl, 2-chloropropane-2-yl, 1,1-dichloropropane-2-yl,
1,2-dichloropropane-2-yl, 1,3-dichloropropane-2-yl, 1,2,3-trichloropropane-2-yl, 1,1,3,3
tetrachloropropane-2-yl, 1,1,1,3,3,3-hexachloropropane-2-yl, heptachloropropane-2-yl, 1
bromopropyl, 2-bromopropyl, 3-bromopropyl, 1-bromopropane-2-yl, 2-bromopropane-2-yl,
1-iodopropyl, 2-iodopropyl, 3-iodopropyl, 1-iodopropane-2-yl, 2-iodopropane-2-yl, 1- fluorobutyl, 2-fluorobutyl, 3-fluorobutyl, 4-fluorobutyl, 4,4-difluorobutyl, 4,4,4-trifluorobutyl,
3,3,4,4,4-pentafluorobutyl, 2,2,3,3,4,4,4-heptafluorobutyl, nonafluorobutyl, 1,1,1
trifluorobutane-2-yl, 4,4,4-trifluorobutane-2-yl, 3,3,4,4,4-pentafluorobutane-2-yl,
nonafluorobutane-2-yl, 1,1,1,3,3,3-hexafluoro-2-(trifluoromethyl)propane-2-yl, 2,2,3,4,4,4
hexafluorobutyl, 1-chlorobutyl, 2-chlorobutyl, 3-chlorobutyl, 4-chlorobutyl, 4,4-dichlorobutyl,
4,4,4-trichlorobutyl, nonachlorobutyl, 1,1,1-trichlorobutane-2-yl, 4,4,4-trichlorobutane-2-yl,
nonachlorobutane-2-yl, 1-bromobutyl, 2-bromobutyl, 3-bromobutyl, 4-bromobutyl, 1
iodobutyl, 2-iodobutyl, 3-iodobutyl, 4-iodobutyl, 4-chloro-1,1,2,2,3,3,4,4-octafluorobutyl, 4
bromo-1,1,2,2,3,3,4,4-octafluorobutyl, 1-fluoropentyl, 2-fluoropentyl, 3-fluoropentyl, 4
fluoropentyl, 5-fluoropentyl, 5,5,5-trifluoropentyl, 4,4,5,5,5-pentafluoropentyl, 3,3,4,4,5,5,5
heptafluoropentyl, 2,2,3,3,4,4,5,5-octafluoropentyl, 2,2,3,3,4,4,5,5,5-nonafluoropentyl,
undecafluoropentyl, 4,4,4-trifluoro-3-methylbutyl, 1-chloropentyl, 2-chloropentyl, 3
chloropentyl, 4-chloropentyl, 5-chloropentyl, 5,5,5-trichloropentyl, 4,4,5,5,5
pentachloropentyl, 3,3,4,4,5,5,5-heptachloropentyl, 2,2,3,3,4,4,5,5,5-nonachloropentyl,
undecachloropentyl, 1-bromopentyl, 2-bromopentyl, 3-bromopentyl, 4-bromopentyl, 5
bromopentyl, 5-iodopentyl, 1-fluorohexyl, 2-fluorohexyl, 3-fluorohexyl, 4-fluorohexyl, 5
fluorohexyl, 6-fluorohexyl, 6,6,6-trifluorohexyl, 5,5,6,6,6-pentafluorohexyl, 4,4,5,5,6,6,6
heptafluorohexyl, 3,3,4,4,5,5,6,6,6-nonafluorohexyl, 2,2,3,3,4,4,5,5,6,6-decafluorohexyl,
2,2,3,3,4,4,5,5,6,6,6-undecafluorohexyl, tridecafluorohexyl, 1-chlorohexyl, 2-chlorohexyl, 3
chlorohexyl, 4-chlorohexyl, 5-chlorohexyl, 6-chlorohexyl, 5-bromohexyl, 6-bromohexyl, 5
iodohexyl, or 6-iodohexyl group.
[0032] In the present invention, unless otherwise specified, "Ci-C6 alkoxy
group" refers to a (C1-C6 alkyl)-O- group in which the alkyl moiety is as defined above, and
examples of the C1-C6 alkoxy group include a methoxy, ethoxy, n-propoxy, isopropoxy, n
butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentoxy, 1-methylbutoxy, 2-methylbutoxy, 3
methylbutoxy, 1-ethylpropoxy, 1,1-dimethylpropoxy, 1,2-dimethylpropoxy, or n-hexyloxy
group.
[0033] In the present invention, unless otherwise specified, "Ci-C6 haloalkoxy group" refers to a (C1-C6 haloalkyl)-O- group in which the haloalkyl moiety is as defined above, and examples of the C-C haloalkoxy group include difluoromethoxy, dichloromethoxy, trifluoromethoxy, trichloromethoxy, tribromomethoxy, chlorodifluoromethoxy, bromodifluoromethoxy, 2-fluoroethoxy, 1-chloroethoxy, 2 chloroethoxy, 1-bromoethoxy, 2-bromoethoxy, 2,2-difluoroethoxy, 1,2-dichloroethoxy, 2,2 dichloroethoxy, 2,2,2-trifluoroethoxy, 2,2,2-trichloroethoxy, 1,1,2,2-tetrafluoroethoxy, pentafluoroethoxy, 2-bromo-2-chloroethoxy, 2-chloro-1,1,2,2-tetrafluoroethoxy, 1-chloro
1,2,2,2-tetrafluoroethoxy, 1-chloropropoxy, 2-chloropropoxy, 3-chloropropoxy, 2
bromopropoxy, 3-bromopropoxy, 2-bromo-1-methylethoxy, 3-iodopropoxy, 2,3
dichloropropoxy, 2,3-dibromopropoxy, 3,3,3-trifluoropropoxy, 3,3,3-trifluoro-2-propoxy,
3,3,3-trichloropropoxy, 3-bromo-3,3-difluoropropoxy, 2,2-difluoropropoxy, 3,3-dichloro-3
fluoropropoxy, 2,2,3,3-tetrafluoropropoxy, 1-bromo-3,3,3-trifluoropropoxy, 2,2,3,3,3
pentafluoropropoxy, 2,2,2-trifluoro-1-trifluoromethylethoxy, heptafluoropropoxy,
heptafluoro-2-propoxy, 1,2,2,2-tetrafluoro-1-trifluoromethylethoxy, 1,1,2,3,3,3
hexafluoropropoxy, 2-chlorobutoxy, 3-chlorobutoxy, 4-chlorobutoxy, 2-chloro-1,1
dimethylethoxy, 4-bromobutoxy, 3-bromo-2-methylpropoxy, 2-bromo-1,1-dimethylethoxy,
2,2-dichloro-1,1-dimethylethoxy, 2-chloro-1-chloromethyl-2-methylethoxy, 4,4,4
trifluorobutoxy, 3,3,3-trifluoro-1-methylpropoxy, 3,3,3-trifluoro-2-methylpropoxy, 2,3,4
trichlorobutoxy, 2,2,2-trichloro-1,1-dimethylethoxy, 4-chloro-4,4-difluorobutoxy, 4,4
dichloro-4-fluorobutoxy, 4-bromo-4,4-difluorobutoxy, 2,4-dibromo-4,4-difluorobutoxy, 3,4
dichloro-3,4,4-trifluorobutoxy, 3,3-dichloro-4,4,4-trifluorobutoxy, 4-bromo-3,3,4,4
tetrafluorobutoxy, 4-bromo-3-chloro-3,4,4-trifluorobutoxy, 2,2,3,3,4,4-hexafluorobutoxy,
2,2,3,4,4,4-hexafluorobutoxy, 2,2,2-trifluoro-1-methyl-1-trifluoromethylethoxy, 3,3,3
trifluoro-2-trifluoromethylpropoxy, 2,2,3,3,4,4,4-heptafluorobutoxy, 3,3,4,4,4-pentafluoro-2
butoxy, 2,3,3,3-tetrafluoro-2-trifluoromethylpropoxy, 1,1,2,2,3,3,4,4-octafluorobutoxy,
nonafluorobutoxy, perfluoro-tert-butoxy, 4-chloro-1,1,2,2,3,3,4,4-octafluorobutoxy, 5,5,5
trifluoropentoxy, 4,4,5,5,5-pentafluoropentoxy, 3,3,4,4,5,5,5-heptafluoropentoxy,
3,3,4,4,5,5,5-heptafluoro-2-pentoxy, 2,2,3,3,4,4,5,5,5-nonafluoropentoxy, 2,2,3,3,4,4,5,5- octafluoropentoxy,perfluoropentoxy,4,4,5,5,5-pentafluoro-2-butoxy,2,2 bis(trifluoromethyl)propoxy,2,2,3,3,4,4,5,5,6,6,6-undecafluorohexyloxy,3,3,4,4,5,5,6,6,6 nonafluorohexyloxy,4,4,5,5,6,6,6-heptafluorohexyloxy,2,2,3,3,4,4,5,5,6,6 decafluorohexyloxy,4,4,4-trifluoro-3,3-bis(trifluoromethyl)butyloxy,orperfluorohexyloxy group.
[0034] In the present invention, unless otherwise specified, "C 3 -C 6
cycloalkyl group" refers to a cycloalkyl group having 3 to 6 carbon atoms, and examples of
the C 3-C 6 cycloalkyl group include a cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl
group.
[0035] In the present invention, unless otherwise specified, "C3-C6
halocycloalkyl group" refers to a cycloalkyl group having 3 to 6 carbon atoms, substituted by
the same or different 1 to11 halogen atoms, and examples of the C3-C halocycloalkyl group
include a 1-fluorocyclopropyl, 2-fluorocyclopropyl, 2,2-difluorocyclopropyl, 2,2,3,3
tetrafluorocyclopropyl, 1-chlorocyclopropyl, 2-chlorocyclopropyl, 2,2-dichlorocyclopropyl,
2,2,3,3-tetrachlorocyclopropyl, 2,2-dibromocyclopropyl, 2,2-diiodocyclopropyl, 1
fluorocyclobutyl, 2-fluorocyclobutyl, 3-fluorocyclobutyl, 3,3-difluorocyclobutyl,
heptafluorocyclobutyl, 2-chlorocyclobutyl, 3-chlorocyclobutyl, 3,3-dichlorocyclobutyl, 3,3
dibromocyclobutyl, 3,3-diiodocyclobutyl, 1-fluorocyclopentyl, 2-fluorocyclopentyl, 3
fluorocyclopentyl, 2,2-difluorocyclopentyl, 3,3-difluorocyclopentyl, nonafluorocyclopentyl,
2,2-dichlorocyclopentyl, 3,3-dichlorocyclopentyl, 2,2-dibromocyclopentyl, 3,3
dibromocyclopentyl, 2,2-diiodocyclopentyl, 3,3-diiodocyclopentyl, 1-fluorocyclohexyl, 2
fluorocyclohexyl, 3-fluorocyclohexyl, 4-fluorocyclohexyl, 2,2-difluorocyclohexyl, 3,3
difluorocyclohexyl, 4,4-difluorocyclohexyl, 1-chlorocyclohexyl, 2-chlorocyclohexyl, 3
chlorocyclohexyl, 4-chlorocyclohexyl, 2,2-dichlorocyclohexyl, 3,3-dichlorocyclohexyl, 4,4
dichlorocyclohexyl, 3,3-dibromocyclohexyl, 4,4-dibromocyclohexyl, 3,3-diiodocyclohexyl,
or 4,4-diiodocyclohexyl group.
[0036] In the present invention, unless otherwise specified, "C 3 -C 6
cycloalkyl Ci-C6 alkyl group" refers to a (C 3 -C cycloalkyl)-(Ci-C6 alkyl)- group in which the cycloalkyl moiety and the alkyl moiety are as defined above, and examples of the C 3 -C cycloalkyl Ci-C6 alkyl group include a cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, 2-cyclopropylethyl, 2-cyclobutylethyl, or 2-cyclopentylethyl group.
[0037] In the present invention, unless otherwise specified, "C3-C6
halocycloalkyl C1-C 6 alkyl group" refers to a (C 3 -C halocycloalkyl)-(C1-C 6 alkyl)- group in
which the halocycloalkyl moiety and the alkyl moiety are as defined above, and examples of
the C 3 -C 6 halocycloalkyl C1-C6 alkyl group include a (1-fluorocyclopropyl)methyl, (2
fluorocyclopropyl)methyl, (2,2-difluorocyclopropyl)methyl, (1-chlorocyclopropyl)methyl, (2
chlorocyclopropyl)methyl, or (2,2-dichlorocyclopropyl)methyl group.
[0038] In the present invention, "Ci-C6 alkoxy Ci-C6 alkyl group" refers to a
(Ci-C 6 alkoxy)-(C1-C 6 alkyl)- group in which the alkoxy moiety is as defined above, and
examples of the Ci-C6 alkoxy Ci-C6 alkyl group include a methoxymethyl, 1-methoxyethyl,
2-methoxyethyl, 2-ethoxyethyl, 3-ethoxypropyl, 3-methoxypropyl, 1-methyl-3-methoxybutyl,
or 3-butoxybutyl group.
[0039] In the present invention, "C 1 -C 6 alkoxy C 1 -C 6 haloalkyl group" refers
to a (Ci-C6 alkoxy)-(Ci-C6 haloalkyl)- group in which the alkoxy moiety is as defined above,
and examples of the Ci-C6 alkoxy Ci-C6 haloalkyl group include a 2-methoxy-1,1,2
trifluoroethyl or 2-ethoxy-1,1,2-trifluoroethyl group.
[0040] In the present invention, "C1 -C 6 haloalkoxy C 1 -C 6 alkyl group" refers
to a (Ci-C6 haloalkoxy)-(Ci-C6 alkyl)- group in which the haloalkoxy moiety is as defined
above, and examples of the C1-C6 haloalkoxy C1-C 6 alkyl group include a 2
(difluoromethoxy)ethyl, 2-(trifluoromethoxy)ethyl, 2-(2,2-difluoroethoxy)ethyl, or 2-(2,2,2
trifluoroethoxy)ethyl group.
[0041] In the present invention, "Ci-C6 haloalkoxy Ci-C6 haloalkyl group"
refers to a (C1-C6 haloalkoxy)-(C1-C6 haloalkyl)- group in which the haloalkoxy moiety is as
defined above, and examples of the C1-C6 haloalkoxy C1-C6 haloalkyl group include a 1,1,2
trifluoro-2-(trifluoromethoxy)ethyl, 1,1,2-trifluoro-2-(pentafluoroethoxy)ethyl, or 1,1,2
trifluoro-2-(heptafluoropropoxy)ethyl group.
[0042] In the present invention, unless otherwise specified, "C 2 -C 6 alkenyl
group" refers to a linear or branched alkenyl group having 2 to 6 carbon atoms, and examples
of the C 2 -C 6 alkenyl group include a vinyl, 1-propenyl, isopropenyl, 2-propenyl, 1-butenyl, 1
methyl-i-propenyl, 2-butenyl, 1-methyl-2-propenyl, 3-butenyl, 2-methyl-i-propenyl, 2
methyl-2-propenyl, 1,3-butadienyl, i-pentenyl, i-ethyl-2-propenyl, 2-pentenyl, i-methyl-
butenyl, 3-pentenyl, 1-methyl-2-butenyl, 4-pentenyl, 1-methyl-3-butenyl, 3-methyl--butenyl,
1,2-dimethyl-2-propenyl, 1,1-dimethyl-2-propenyl, 2-methyl-2-butenyl, 3-methyl-2-butenyl,
1,2-dimethyl-i-propenyl, 2-methyl-3-butenyl, 3-methyl-3-butenyl, 1,3-pentadienyl, i-vinyl-2
propenyl, i-hexenyl, i-propyl-2-propenyl, 2-hexenyl, 1-methyl--pentenyl, i-ethyl-2-butenyl,
3-hexenyl, 4-hexenyl, 5-hexenyl, 1-methyl-4-pentenyl, i-ethyl-3-butenyl, 1-(isobutyl)vinyl,
I-ethyl-i-methyl-2-propenyl, i-ethyl-2-methyl-2-propenyl, 1-(isopropyl)-2-propenyl, 2
methyl-2-pentenyl, 3-methyl-3-pentenyl, 4-methyl-3-pentenyl, 1,3-dimethyl-2-butenyl, 1,1
dimethyl-3-butenyl, 3-methyl-4-pentenyl, 4-methyl-4-pentenyl, 1,2-dimethyl-3-butenyl, 1,3
dimethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl, 1,5-hexadienyl, i-vinyl-3-butenyl, or 2,4
hexadienyl group.
[0043] In the present invention, unless otherwise specified, "C2-C7 alkynyl
group" refers to a linear or branched alkynyl group having 2 to 7 carbon atoms, and examples
of the C 2 -C 7 alkynyl group include an ethynyl, I-propynyl, 2-propynyl, i-butynyl, i-methyl
2-propynyl, 2-butynyl, 3-butynyl, I-pentynyl, I-ethyl-2-propynyl, 2-pentynyl, 3-pentynyl, I
methyl-2-butynyl, 4-pentynyl, 1-methyl-3-butynyl, 2-methyl-3-butynyl, 1-hexynyl, 1-(n
propyl)-2-propynyl, 2-hexynyl, i-ethyl-2-butynyl, 3-hexynyl, 1-methyl-2-pentynyl, i-methyl
3-pentynyl, 4-methyl-i-pentynyl, 3-methyl-i-pentynyl, 5-hexynyl, i-ethyl-3-butynyl, i-ethyl
1-methyl-2-propynyl, 1-(isopropyl)-2-propynyl, 1,1-dimethyl-2-butynyl or 2,2-dimethyl-3
butynyl, i-heptynyl, 1-(n-butyl)-2-propynyl, 1-(s-butyl)-2-propynyl, 1-isobutyl-2-propynyl, 2
heptynyl, 3-heptynyl, 1-methyl-2-hexynyl, 4-methyl-2-hexynyl, 5-methyl-2-hexynyl, 6
heptynyl, 1,1-diethyl-2-propynyl, 1-methyl--propyl-2-propynyl, 1-isopropyl--methyl-2
propynyl, 1,1-dimethyl-2-pentynyl, 1,4-dimethyl-2-pentynyl, or 4,4-dimethyl-2-pentynyl
group.
[0044] In the present invention, unless otherwise specified, "C 2 -C 6
haloalkynyl group" refers to a linear or branched alkynyl group having 2 to 6 carbon atoms,
substituted with the same or different 1 to 9 halogen atoms, and examples of the C 2 -C
haloalkynyl group include a fluoroethynyl, chloroethynyl, bromoethynyl, iodoethynyl, 3
fluoro-2-propynyl, 3-chloro-2-propynyl, 3-bromo-2-propynyl, 3-iodo-2-propynyl, 4-fluoro-3
butynyl, 4-chloro-3-butynyl, 4-bromo-3-butynyl, 4-iodo-3-butynyl, 4,4-difluoro-2-butynyl,
4,4-dichloro-2-butynyl, 4,4,4-trifluoro-2-butynyl, 4,4,4-trichloro-2-butynyl, 3-fluoro-1
methyl-2-propynyl, 3-chloro-1-methyl-2-propynyl, 5-fluoro-4-pentynyl, 5-chloro-4-pentynyl,
5,5,5-trifluoro-3-pentynyl, 5,5,5-trichloro-3-pentynyl, 4-fluoro-2-methyl-3-butynyl, 4-chloro
2-methyl-3-butynyl, 6-fluoro-5-hexynyl, 6-chloro-5-hexynyl, 6,6,6-trifluoro-4-hexynyl, 6,6,6
trichloro-4-hexynyl, 5-fluoro-3-methyl-4-pentynyl, or 5-chloro-3-methyl-4-pentynyl group.
[0045] In the present invention, unless otherwise specified, "C2-C6
haloalkenyl group" refers to a linear or branched alkenyl group having 2 to 6 carbon atoms,
substituted with the same or different 1 to 11 halogen atoms, and examples of the C 2 -C
haloalkenyl group include a 1-fluorovinyl, 2-fluorovinyl, 1,2-difluorovinyl, 2,2-difluorovinyl,
trifluorovinyl, 1-chlorovinyl, 2-chlorovinyl, 1,2-dichlorovinyl, 2,2-dichlorovinyl,
trichlorovinyl, 1,2-dibromovinyl, 2,2-dibromovinyl, tribromovinyl, 1,2-diiodovinyl, 2,2
diiodovinyl, triodovinyl, 1-fluoro-2-propenyl, 2-fluoro-2-propenyl, 3-fluoro-2-propenyl, 2,3
difluoro-2-propenyl, 3,3-difluoro-2-propenyl, 3,3-difluoro-1-propenyl, 2,3,3-trifluoro-2
propenyl, 3,3,3-trifluoro-1-propenyl, 2-chloro-3,3,3-trifluoro-1-propenyl, 1,2,3,3,3
pentafluoro-1-propenyl, 1-chloro-2-propenyl, 2-chloro-2-propenyl, 3-chloro-2-propenyl, 2,3
dichloro-2-propenyl, 3,3-dichloro-2-propenyl, 3,3-dichloro-1-propenyl, 2,3,3-trichloro-2
propenyl, 3,3,3-trichloro-1-propenyl, 3-bromo-2-propenyl, 3,3-dibromo-2-propenyl, 3,3
diiodo-2-propenyl, 2,2-difluoro-1-propene-2-yl, 3,3,3-trifluoro-1-propene-2-yl, 3,3,3
trichloro-1-propene-2-yl, 4-fluoro-3-butenyl, 4,4-difluoro-3-butenyl, 4,4-difluoro-3-butene-2
yl, 4,4,4-trifluoro-2-butenyl, 3,4,4-trifluoro-3-butenyl, 2-trifluoromethyl-2-propenyl, 2
trifluoromethyl-3,3-difluoro-2-propenyl, 4,4,4-trifluoro-3-chloro-2-butenyl, 4,4-dichloro-3
butenyl, 4,4,4-trichloro-2-butenyl, 2-trichloromethyl-2-propenyl, 5,5-difluoro-4-pentenyl,
4,5,5-trifluoro-4-pentenyl, 5,5,5-trifluoro-3-pentenyl, 4,4,4-trifluoro-3-methyl-2-butenyl,
4,4,4-trifluoro-3-trifluoromethyl-2-butenyl, 5,5-dichloro-4-pentenyl, 4,4,4-trichloro-3-methyl
2-butenyl, 6,6-difluoro-5-hexenyl, 5,6,6-trifluoro-5-pentenyl, 6,6,6-trifluoro-4-pentenyl,
5,5,5-trifluoro-4-methyl-3-pentenyl, 5,5,5-trifluoro-4-trifluoromethyl-3-pentenyl, 6,6
dichloro-5-hexenyl, or 5,5,5-trichloro-4-methyl-3-pentenyl group.
[0046] In the present invention, "C1-C6 alkylthio group" refers to a (C1-C
alkyl)-S- group in which the alkyl moiety is as defined above, and examples of the C1-C
alkylthio group include a methylthio, ethylthio, n-propylthio, isopropylthio, n-butylthio,
isobutylthio, sec-butylthio, or tert-butylthio group.
[0047] In the present invention, "Ci-C6 alkylsulfinyl group" refers to a (Ci
C 6 alkyl)-S(=)- group in which the alkyl moiety is as defined above, and examples of the
C1-C6 alkylsulfinyl group include a methylsulfinyl, ethylsulfinyl, n-propylsulfinyl,
isopropylsulfinyl, n-butylsulfinyl, isobutylsulfinyl, sec-butylsulfinyl, or tert-butylsulfinyl
group.
[0048] In the present invention, "C1-C6 alkylsulfonyl group" refers to a (C1
C6 alkyl)-S(=0)2- group in which the alkyl moiety is as defined above, and examples of the
C1-C6 alkylsulfonyl group include a methylsulfonyl, ethylsulfonyl, n-propylsulfonyl,
isopropylsulfonyl, n-butylsulfonyl, isobutylsulfonyl, sec-butylsulfonyl, or tert-butylsulfonyl
group.
[0049] In the present invention, unless otherwise specified, "Ci-C6
haloalkylthio group" refers to a (C1-C 6 haloalkyl)-S- group in which the haloalkyl moiety is
as defined above, and examples of the Ci-C haloalkylthio group include a fluoromethylthio,
difluoromethylthio, trifluoromethylthio, trichloromethylthio, 2,2,2-trifluoroethylthio,
pentafluoroethylthio, 2,2,2-trichloroethylthio, 3,3,3-trifluoropropylthio, 1,1,2,3,3,3
hexafluoropropyl, heptafluoropropylthio, 1,1,1,3,3,3-hexafluoropropane-2-ylthio,
heptafluoropropane-2-ylthio, or 4,4,4-trifluorobutylthio group.
[0050] In the present invention, unless otherwise specified, "C1-C6
haloalkylsulfinyl group" refers to a (Ci-C6 haloalkyl)-S(=O)- group in which the haloalkyl moiety is as defined above, and examples of the C1-C haloalkylsulfinyl group include a difluoromethylsulfinyl, trifluoromethylsulfinyl, trichloromethylsulfinyl, 2,2,2 trifluoroethylsulfinyl, 2,2,2-trichloroethylsulfinyl, pentafluoroethylsulfinyl, 3,3,3 trifluoropropylsulfinyl, heptafluoropropylsulfinyl, or heptafluoro-2-propylsulfinyl group.
[0051] In the present invention, unless otherwise specified, "C1-C6
haloalkylsulfonyl group" refers to a (C1-C6 haloalkyl)-S(=0) 2 - group in which the haloalkyl
moiety is as defined above, and examples of the C 1-C haloalkylsulfonyl group include a
difluoromethylsulfonyl, trifluoromethylsulfonyl, trichloromethylsulfonyl, 2,2,2
trifluoroethylsulfonyl, pentafluoroethylsulfonyl, 3,3,3-trifluoropropylsulfonyl,
heptafluoropropylsulfonyl, or heptafluoro-2-propylsulfonyl group.
[0052] In the present invention, unless otherwise specified, "C1-C6 alkylthio
C1-C6 alkyl group" refers to a (Ci-C6 alkyl)-S-(Ci-C6 alkyl)- group in which the alkyl moiety
is as defined above, and examples of the C1-C6 alkylthio C1-C6 alkyl group include a
methylthiomethyl, ethylthiomethyl, n-propylthiomethyl, isopropylthiomethyl, 1
(methylthio)ethyl, 2-(methylthio)ethyl, 2-(ethylthio)ethyl, 1-(n-propylthio)ethyl, 2-(n
propylthio)ethyl, 1-(methylthio)propyl, 2-(methylthio)propyl, 3-(methylthio)propyl, 1
(ethylthio)propyl, 2-(ethylthio)propyl, 3-(ethylthio)propyl, 1-(n-propylthio)propyl, 2-(n
propylthio)propyl, 3-(n-propylthio)propyl, 2-(n-butylthio)ethyl, 2-(isobutylthio)ethyl, sec
butylthioethyl, 2-(tert-butylthio)ethyl, pentylthiomethyl, or hexylthiomethyl group.
[0053] In the present invention, unless otherwise specified, "Ci-C6
alkylsulfinyl C1-C 6 alkyl group" refers to a (C1-C alkyl)-S(=O)-(Ci-C6 alkyl)- group in
which the alkyl moiety is as defined above, and examples of the C-C alkylsulfinyl C-C
alkyl group include a methylsulfinylmethyl, ethylsulfinylmethyl, n-propylsulfinylmethyl,
isopropylsulfinylmethyl, 1-(methylsulfinyl)ethyl, 2-(methylsulfinyl)ethyl, 2
(ethylsulfinyl)ethyl, 1-(n-propylsulfinyl)ethyl, 2-(n-propylsulfinyl)ethyl, 1
(methylsulfinyl)propyl, 2-(methylsulfinyl)propyl, 3-(methylsulfinyl)propyl, 1
(ethylsulfinyl)propyl, 2-(ethylsulfinyl)propyl, 3-(ethylsulfinyl)propyl, 1-(n
propylsulfinyl)propyl, 2-(n-propylsulfinyl)propyl, 3-(n-propylsulfinyl)propyl, 2-(n- butylsulfinyl)ethyl, 2-(isobutylsulfinyl)ethyl, sec-butylsulfinylethyl, 2-(tert-butylsulfinyl)ethyl, pentylsulfinylmethyl, or hexylsulfinylmethyl group.
[0054] In the present invention, unless otherwise specified, "C1-C6
alkylsulfonyl Ci-C 6 alkyl group" refers to a (C-C alkyl)-S(=0)2-(Ci-C6 alkyl)- group in
which the alkyl moiety is as defined above, and examples of the C1-C alkylsulfonyl C1-C6
alkyl group include a methylsulfonylmethyl, ethylsulfonylmethyl, n-propylsulfonylmethyl,
isopropylsulfonylmethyl, 1-(methylsulfonyl)ethyl, 2-(methylsulfonyl)ethyl, 2
(ethylsulfonyl)ethyl, 1-(n-propylsulfonyl)ethyl, 2-(n-propylsulfonyl)ethyl, 1
(methylsulfonyl)propyl, 2-(methylsulfonyl)propyl, 3-(methylsulfonyl)propyl, 1
(ethylsulfonyl)propyl, 2-(ethylsulfonyl)propyl, 3-(ethylsulfonyl)propyl, 1-(n
propylsulfonyl)propyl, 2-(n-propylsulfonyl)propyl, 3-(n-propylsulfonyl)propyl, 2-(n
butylsulfonyl)ethyl, 2-(isobutylsulfonyl)ethyl, sec-butylsulfonylethyl, 2-(tert
butylsulfonyl)ethyl, pentylsulfonylmethyl, or hexylsulfonylmethyl group.
[0055] In the present invention, "C 1 -C 6 haloalkylthio C 1 -C 6 alkyl group"
refers to a (C1-C haloalkyl)-S-(C 1 -C 6 alkyl)- group in which the haloalkylthio moiety and
the alkyl moiety are as defined above, and examples of the C-C haloalkylthio C-C6 alkyl
group include a 2-(difluoromethylthio)ethyl, 2-(trifluoromethylthio)ethyl, 2-(2,2
difluoroethylthio)ethyl, 2-(2,2,2-trifluoroethylthio)ethyl, 2-(3,3-difluoropropylthio)ethyl, 2
(3,3,3-trifluoroethylthio)ethyl, 3-(difluoromethylthio)propyl, 3-(trifluoromethylthio)propyl, 3
(2,2-difluoroethylthio)propyl, 3-(2,2,2-trifluoroethylthio)propyl, 3-(3,3
difluoropropylthio)propyl, or 3-(3,3,3-trifluoropropylthio)propyl group.
[0056] In the present invention, "C1-C6 haloalkylsulfinyl C1-C6 alkyl group"
refers to a (C1-C6 haloalkyl)-S(=O)-(Ci-C 6 alkyl)- group in which the haloalkylsulfinyl
moiety and the alkyl moiety are as defined above, and examples of the C1-C6
haloalkylsulfinyl C1-C 6 alkyl group include a 2-(difluoromethylsulfinyl)ethyl, 2
(trifluoromethylsulfinyl)ethyl, 2-(2,2-difluoroethylsulfinyl)ethyl, 2-(2,2,2
trifluoroethylsulfinyl)ethyl, 2-(3,3-difluoropropylsulfinyl)ethyl, 2-(3,3,3
trifluoroethylsulfinyl)ethyl, 3-(difluoromethylsulfinyl)propyl, 3-
(trifluoromethylsulfinyl)propyl, 3-(2,2-difluoroethylsulfinyl)propyl, 3-(2,2,2
trifluoroethylsulfinyl)propyl, 3-(3,3-difluoropropylsulfinyl)propyl, or 3-(3,3,3
trifluoropropylsulfinyl)propyl group.
[0057] In the present invention, "Ci-C6 haloalkylsulfonyl Ci-C6 alkyl group"
refers to a (C1-C haloalkyl)-S(=0) 2 -(Ci-C 6 alkyl)- group in which the haloalkylsulfonyl
moiety and the alkyl moiety are as defined above, and examples of the C1-C6
haloalkylsulfonyl C1-C 6 alkyl group include a 2-(difluoromethylsulfonyl)ethyl, 2
(trifluoromethylsulfonyl)ethyl, 2-(2,2-difluoroethylsulfonyl)ethyl, 2-(2,2,2
trifluoroethylsulfonyl)ethyl, 2-(3,3-difluoropropylsulfonyl)ethyl, 2-(3,3,3
trifluoroethylsulfonyl)ethyl, 3-(difluoromethylsulfonyl)propyl, 3
(trifluoromethylsulfonyl)propyl, 3-(2,2-difluoroethylsulfonyl)propyl, 3-(2,2,2
trifluoroethylsulfonyl)propyl, 3-(3,3-difluoropropylsulfonyl)propyl, or 3-(3,3,3
trifluoropropylsulfonyl)propyl group.
[0058] In the present invention, "mono(C1-C6 alkyl)amino group" refers to a
(C1-C 6 alkyl)-NH- group in which the alkyl moiety is as defined above, and examples of the
mono(Ci-C6 alkyl)amino group include a methylamino, ethylamino, n-propylamino, or
isopropyl amino group.
[0059] In the present invention, "di(C1-C 6 alkyl)amino group" refers to a
(C1-C 6 alkyl) 2-N- group in which the alkyl moiety is as defined above, and the two alkyl
groups may be different from each other, and examples of the di(Ci-C alkyl)amino group
include a dimethylamino, diethylamino, or N-ethyl-N-methylamino group.
[0060] In the present invention, "mono(Ci-C6 alkyl)aminocarbonyl group"
refers to a (C1-C6 alkyl)-NH-C(=O)- group in which the alkyl moiety is as defined above, and
examples of the mono(Ci-C6 alkyl)aminocarbonyl group include a methylaminocarbonyl,
ethylaminocarbonyl, propylaminocarbonyl, or isopropylaminocarbonyl group.
[0061] In the present invention, "di(C1-C alkyl)aminocarbonyl group" refers
to a (C1-C6 alkyl) 2-N-C(=)- group in which the alkyl moiety is as defined above, and the
two alkyl groups may be different from each other, and examples of the di(C1-C6 alkyl)aminocarbonyl group include a dimethylaminocarbonyl, diethylaminocarbonyl, di(n propyl)aminocarbonyl, or N-ethyl-N-methylaminocarbonyl group.
[0062] In the present invention, "C1-C6 alkylcarbonyl C1-C6 alkyl group"
refers to a (Ci-C6 alkyl)-C(=O)-(Ci-C6 alkyl)- group in which the alkyl moiety is as defined
above, and examples of the C1-C6 alkylcarbonyl C1-C6 alkyl group include an acetonyl,
propionylmethyl, 2-methylpropionylmethyl, pivaloylmethyl, 2-acetylethyl, 2-propionylethyl,
2(2-methylpropionyl)ethyl, 2-pivaloylethyl, 3-acetylpropyl, 3-propionylpropyl, 3(2
methylpropionyl)propyl, or 3-pivaloylpropyl group.
[0063] In the present invention, "C1-C6 haloalkylcarbonyl C1-C6 alkyl
group" refers to a (Ci-C6 haloalkyl)-C(=O)-(Ci-C6 alkyl)- group in which the haloalkyl
moiety and the alkyl moiety are as defined above, and examples of the C1-C6
haloalkylcarbonyl C1-C6 alkyl group include a 3,3,3-trifluoro-2-oxopropyl group.
[0064] In the present invention, "C1-C6 alkoxycarbonyl C1-C6 alkyl group"
refers to a (C1-C6 alkoxy)-C(=O)-(Ci-C 6 alkyl)- group in which the alkoxy moiety and the
alkyl moiety are as defined above, and examples of the C1-C6 alkoxycarbonyl C1-C6 alkyl
group include a methoxycarbonylmethyl, ethoxycarbonylmethyl, n-propoxycarbonylmethyl,
isopropoxycarbonylmethyl, tert-butoxycarbonylmethyl, 2-(methoxycarbonyl)ethyl, 2
(ethoxycarbonyl)ethyl, or 2-(tert-butoxycarbonyl)ethyl group.
[0065] In the present invention, unless otherwise specified, "hydroxy C1-C6
alkyl group" refers to a (hydroxy)-(C1-C6 alkyl)- group in which the alkyl moiety is as
defined above, and examples of the hydroxy C1-C6 alkyl group include a 2-hydroxyethyl, 2
hydroxypropyl, 3-hydroxypropyl, or 4-hydroxybutyl group.
[0066] In the present invention, unless otherwise specified, "cyano C1-C6
alkyl group" refers to a (cyano)-(Ci-C6 alkyl)- group in which the alkyl moiety is as defined
above, and examples of the cyano C1-C6 alkyl group include a cyanomethyl, 1-cyanoethyl, 2
cyanoethyl, 3-cyanopropyl, 2-cyanopropane-2-yl, 1-cyanobutyl, 4-cyanobutyl, 5-cyanopentyl,
or 6-cyanohexyl group.
[0067] In the present invention, unless otherwise specified, "Ci-C6 alkylsulfonyloxy group" refers to a (C1-C6 alkyl)-S(=0) 2 -0- group in which the alkyl moiety is as defined above, and examples of the C-C alkylsulfonyloxy group include a methylsulfonyloxy, ethylsulfonyloxy, or isopropylsulfonyloxy group.
[0068] In the present invention, unless otherwise specified, "Ci-C6
haloalkylsulfonyloxy group" refers to a (C1-C6 haloalkyl)-S(=0) 2 -0- group in which the
haloalkyl moiety is as defined above, and examples of the C1-C6 haloalkylsulfonyloxy group
include a trifluoromethylsulfonyloxy, perfluoroethylsulfonyloxy, perfluoropropylsulfonyloxy,
or perfluorobutylsulfonyloxy group.
[0069] In the present invention, unless otherwise specified, "C1-C6
alkylcarbonyl group" refers to a (Ci-C6 alkyl)-C(=O)- group in which the alkyl moiety is as
defined above, and examples of the C1-C6 alkylcarbonyl group include an acetyl or propionyl
group.
[0070] In the present invention, unless otherwise specified, "C1-C6
haloalkylcarbonyl group" refers to a (C-C6 haloalkyl)-C(=O)- group in which the haloalkyl
moiety is as defined above, and examples of the C1-C6 haloalkylcarbonyl group include a
2,2,2-trifluoroacetyl group or 2,2,2-trichloroacetyl group.
[0071] In the present invention, "Ci-C6 alkoxycarbonyl group" refers to a
(Ci-C6 alkoxy)-C(=)- group in which the alkoxy moiety is as defined above, and examples
of the C1-C6 alkoxycarbonyl group include a methoxycarbonyl, ethoxycarbonyl, n
propoxycarbonyl, isopropoxycarbonyl, or tert-butoxycarbonyl group.
[0072] In the present invention, unless otherwise specified, "C 3 -C 6
cycloalkoxy group" refers to a (C3-C6 cycloalkyl)-O- group in which the cycloalkyl moiety is
as defined above, and examples of the C 3 -C cycloalkoxy group include a cyclopropoxy,
cyclobutoxy, cyclopentyloxy, or cyclohexyloxy group.
[0073] In the present invention, unless otherwise specified, "C 3 -C 6
halocycloalkoxy group" refers to a (C 3 -C 6 halocycloalkyl)-O- group in which the
halocycloalkyl moiety is as defined above, and examples of the C 3-C halocycloalkoxy group
include a 1-fluorocyclopropoxy, 2-fluorocyclopropoxy, 2,2-difluorocyclopropoxy, 2,2,3,3- tetrafluorocyclopropoxy, 1-chlorocyclopropoxy, 2-chlorocyclopropoxy, 2,2 dichlorocyclopropoxy, 2,2,3,3-tetrachlorocyclopropoxy, 1-fluorocyclobutoxy, 2 fluorocyclobutoxy, 3-fluorocyclobutoxy, 3,3-difluorocyclobutoxy, 2-chlorocyclobutoxy, 3 chlorocyclobutoxy, 3,3-dichlorocyclobutoxy, 2-fluorocyclopentyloxy, 3-fluorocyclopentyloxy,
2,2-difluorocyclopentyloxy, 3,3-difluorocyclopentyloxy, 2,2-dichlorocyclopentyloxy, 3,3
dichlorocyclopentyloxy, 1-fluorocyclohexyloxy, 2-fluorocyclohexyloxy, 3
fluorocyclohexyloxy, 4-fluorocyclohexyloxy, 2,2-difluorocyclohexyloxy, 3,3
difluorocyclohexyloxy, 4,4-difluorocyclohexyloxy, 1-chlorocyclohexyloxy, 2
chlorocyclohexyloxy, 3-chlorocyclohexyloxy, 4-chlorocyclohexyloxy, 2,2
dichlorocyclohexyloxy, 3,3-dichlorocyclohexyloxy, or 4,4-dichlorocyclohexyloxy group.
[0074] In the present invention, unless otherwise specified, "C 3 -C 6
cycloalkyl Ci-C6 alkoxy group" refers to a (C 3 -C cycloalkyl)-(Ci-C6 alkyl)-O- group in
which the cycloalkyl moiety is as defined above, and examples of the C 3 -C cycloalkyl C1-C
alkoxy group include a cyclopropylmethoxy, cyclobutylmethoxy, cyclopentylmethoxy, 2
cyclopropylethoxy, 2-cyclobutylethoxy, or 2-cyclopentylethoxy group.
[0075] In the present invention, unless otherwise specified, "C3-C6
halocycloalkyl Ci-C6 alkoxy group" refers to a (C3-C halocycloalkyl)-(C1-C6 alkyl)-O
group in which the halocycloalkyl moiety is as defined above, and examples of the C 3 -C
halocycloalkyl C1-C 6 alkoxy group include a (1-fluorocyclopropyl)methoxy, (2
fluorocyclopropyl)methoxy, (2,2-difluorocyclopropyl)methoxy, (2
chlorocyclopropyl)methoxy, or (2,2-dichlorocyclopropyl)methoxy group.
[0076] In the present invention, unless otherwise specified, "C3-C6
cycloalkyl C1-C 6 alkylthio group" refers to a (C 3 -C cycloalkyl)-(C1-C 6 alkyl)-S- group in
which the cycloalkyl moiety is as defined above, and examples of the C3-C cycloalkyl Ci-C6
alkylthio group include a (cyclopropylmethyl)thio, (cyclobutylmethyl)thio,
(cyclopentylmethyl)thio, (2-cyclopropylethyl)thio, (2-cyclobutylethyl)thio, or (2
cyclopentylethyl)thio group.
[0077] In the present invention, unless otherwise specified, "C3-C6 cycloalkyl C1-C6 alkylsulfinyl group" refers to a (C 3-C cycloalkyl)-(C1-C alkyl)-S(=O) group in which the cycloalkyl moiety is as defined above, and examples of the C3-C cycloalkyl C1-C6 alkylsulfinyl group include a (cyclopropylmethyl)sulfinyl,
(cyclobutylmethyl)sulfinyl, (cyclopentylmethyl)sulfinyl, (2-cyclopropylethyl)sulfinyl, (2
cyclobutylethyl)sulfinyl, or (2-cyclopentylethyl)sulfinyl group.
[0078] In the present invention, unless otherwise specified, "C 3 -C 6
cycloalkyl C1-C6 alkylsulfonyl group" refers to a (C 3 -C cycloalkyl)-(C1-C alkyl)-S(=0)2
group in which the cycloalkyl moiety is as defined above, and examples of the C 3 -C
cycloalkyl C1-C6 alkylsulfonyl group include a (cyclopropylmethyl)sulfonyl,
(cyclobutylmethyl)sulfonyl, (cyclopentylmethyl)sulfonyl, (2-cyclopropylethyl)sulfonyl, (2
cyclobutylethyl)sulfonyl, or (2-cyclopentylethyl)sulfonyl group.
[0079] In the present invention, unless otherwise specified, "C3-C6
halocycloalkyl C1-C 6 alkylthio group" refers to a (C 3 -C halocycloalkyl)-(C1-C6 alkyl)-S
group in which the halocycloalkyl moiety is as defined above, and examples of the C 3 -C
halocycloalkyl C1-C 6 alkylthio group include a (1-fluorocyclopropyl)methylthio, (2
fluorocyclopropyl)methylthio, (2,2-difluorocyclopropyl)methylthio, (2
chlorocyclopropyl)methylthio, or (2,2-dichlorocyclopropyl)methylthio group.
[0080] In the present invention, unless otherwise specified, "C 3 -C 6
halocycloalkyl C1-C 6 alkylsulfinyl group" refers to a (C 3 -C halocycloalkyl)-(C1-C6 alkyl)
S(=O)- group in which the halocycloalkyl moiety is as defined above, and examples of the
C 3 -C 6 halocycloalkyl C1-C 6 alkylsulfinyl group include a (1
fluorocyclopropyl)methylsulfinyl, (2-fluorocyclopropyl)methylsulfinyl, (2,2
difluorocyclopropyl)methylsulfinyl, (2-chlorocyclopropyl)methylsulfinyl, or (2,2
dichlorocyclopropyl)methylsulfinyl group.
[0081] In the present invention, unless otherwise specified, "C 3 -C 6
halocycloalkyl C1-C 6 alkylsulfonyl group" refers to a (C 3 -C halocycloalkyl)-(C1-C alkyl)
S(=0) 2 - group in which the cycloalkyl moiety is as defined above, and examples of the C 3 -C
halocycloalkyl Ci-C6 alkylsulfonyl group include a (1-fluorocyclopropyl)methylsulfonyl, (2- fluorocyclopropyl)methylsulfonyl, (2,2-difluorocyclopropyl)methylsulfonyl, (2 chlorocyclopropyl)methylsulfonyl, or (2,2-dichlorocyclopropyl)methylsulfonyl group.
[0082] In the present invention, unless otherwise specified, "mono(oxirane-2
yl) Ci-C 3 alkyl group" refers to an (oxirane-2-yl)-(Ci-C3 alkyl)- group in which the alkyl
moiety is as defined above, and examples of the mono(oxirane-2-yl) C1-C 3 alkyl group
include an oxirane-2-ylmethyl, 2-(oxirane-2-yl)ethyl, or 3-(oxirane-2-yl)propyl group.
[0083] In the present invention, unless otherwise specified, "C1-C6
alkylcarbonyloxy group" refers to a (Ci-C6 alkyl)-C(=O)-O- group in which the alkyl moiety
is as defined above, and examples of the C1-C alkylcarbonyloxy group include an acetoxy or
propionyloxy group.
[0084] In the present invention, unless otherwise specified, "C1-C6
haloalkylcarbonyloxy group" refers to a (C1-C6 haloalkyl)-C(=O)-O- group in which the
haloalkyl moiety is as defined above, and examples of the C1-C6 haloalkylcarbonyloxy group
include a 2,2,2-trifluoroacetoxy or 2,2,2-trichloroacetoxy group.
[0085] In the present invention, unless otherwise specified, "mono(C1-C6
alkyl)aminocarbonyloxy group" refers to a (Ci-C6 alkyl)-NH-C(=O)-O- group in which the
alkyl moiety is as defined above, and examples of the mono(Ci-C alkyl)aminocarbonyloxy
group include a (methylcarbamoyl)oxy or (ethylcarbamoyl)oxy group.
[0086] In the present invention, unless otherwise specified, "di(C1-C6
alkyl)aminocarbonyloxy group" refers to a (Ci-C6 alkyl)2-N-C(=O)-O- group in which the
alkyl moiety is as defined above, and examples of the di(C1-C6 alkyl)aminocarbonyloxy
group include a (dimethylcarbamoyl)oxy or (diethylcarbamoyl)oxy group.
[0087] In the present invention, unless otherwise specified, "aminocarbonyloxy Ci-C6 alkyl group" refers to an (amino)-C(=O)-O-(Ci-C6 alkyl)- group
in which the alkyl moiety is as defined above, and examples of the aminocarbonyloxy C1-C6
alkyl group include a carbamoyloxymethyl or carbamoyloxyethyl group.
[0088] In the present invention, unless otherwise specified, "mono(C1-C6
alkyl)aminocarbonyloxy Ci-C6 alkyl group" refers to a (Ci-C alkyl)-NH-C(=O)-O-(Ci-C alkyl)- group in which the alkyl moiety is as defined above, and examples of the mono(C1-C6 alkyl)aminocarbonyloxy Ci-C6 alkyl group include a methylcarbamoyloxymethyl or ethylcarbamoyloxymethyl group.
[0089] In the present invention, unless otherwise specified, "di(Ci-C6
alkyl)aminocarbonyloxy C1-C 6 alkyl group" refers to a (C1-C alkyl) 2-N-C(=O)-O-(Ci-C6
alkyl)- group in which the alkyl moiety is as defined above, and examples of the di(C1-C6
alkyl)aminocarbonyloxy Ci-C 6 alkyl group include a dimethylcarbamoyloxymethyl or
diethylcarbamoyloxymethyl group.
[0090] In the present invention, unless otherwise specified, "C1-C6
alkoxycarbonyloxy group" refers to a (Ci-C6 alkoxy)-C(=O)-O- group in which the alkoxy
moiety is as defined above, and examples of the C1-C6 alkoxycarbonyloxy group include a
methoxycarbonyloxy or ethoxycarbonyloxy group.
[0091] In the present invention, "C1-C6 alkoxycarbonyloxy C1-C6 alkyl
group" refers to a (C-C6 alkoxy)-C(=O)-O-(Ci-C 6 alkyl)- group in which the alkoxy moiety
is as defined above, and examples of the C1-C6 alkoxycarbonyloxy C1-C6 alkyl group include
a methoxycarbonyloxymethyl or ethoxycarbonyloxymethyl group.
[0092] In the present invention, "C3-C6 cycloalkyl C2-C6 alkynyl group"
refers to a (C 3 -C 6 cycloalkyl)-(C2-C6 alkynyl)- group in which the cycloalkyl moiety is as
defined above, and examples of the C 3 -C 6 cycloalkyl C 2 -C 6 alkynyl group include a
cyclopropylethynyl or cyclobutylethynyl group.
[0093] In the present invention, "C 3 -C 6 cycloalkylthio group" refers to a
(C3-C6 cycloalkyl)-S- group in which the cycloalkyl moiety is as defined above, and
examples of the C 3 -C 6 cycloalkylthio group include a cyclopropylthio, cyclobutylthio, or
cyclopentylthio group.
[0094] In the present invention, "C 3 -C 6 cycloalkylsulfinyl group" refers to a
(C 3 -C 6 cycloalkyl)-S(=)- group in which the cycloalkyl moiety is as defined above, and
examples of the C 3 -C 6 cycloalkylsulfinyl group include a cyclopropylsulfinyl,
cyclobutylsulfinyl, or cyclopentylsulfinyl group.
[0095] In the present invention, "C 3 -C 6 cycloalkylsulfonyl group" refers to a
(C 3 -C 6 cycloalkyl)-S(=0)2- group in which the cycloalkyl moiety is as defined above, and
examples of the C 3 -C 6 cycloalkylsulfonyl group include a cyclopropylsulfonyl,
cyclobutylsulfonyl, or cyclopentylsulfonyl group.
[0096] In the present invention, "C1-C6 alkylcarbonyloxy C1-C6 alkyl group"
refers to a (C1-C6 alkyl)-C(=O)-O-(Ci-C6 alkyl)- group in which the alkyl moiety is as
defined above, and examples of the C1-C6 alkylcarbonyloxy C1-C6 alkyl group include an
acetoxymethyl, 2-acetoxyethyl, or propionylmethyl group.
[0097] In the present invention, "di(C1-C6 alkyl)sulfamoyloxy group" refers
to a (C1-C6 alkyl)2-N-S(=0)2-0- group in which the alkyl moiety is as defined above, and
examples of the di(C1-C6 alkyl)sulfamoyloxy group include a dimethylsulfamoyloxy or
diethylsulfamoyloxy group.
[0098] In the present invention, unless otherwise specified, "cyano C 3 -C 6
cycloalkyl group" refers to a (cyano)-(C3-C6 cycloalkyl) group in which the cycloalkyl
moiety is as defined above, and examples of the cyano C 3 -C 6 cycloalkyl group include a 1
cyanocyclopropyl, 2-cyanocyclopropyl, 1-cyanocyclobutyl, 3-cyanocyclobutyl, or 1
cyanocyclopentyl group.
[0099] In the present invention, unless otherwise specified, "C1-C6 alkoxy
C1-C 6 alkylcarbonyl group" refers to a (C1-C6 alkyl)-O-(C1-C6 alkyl)-C(=O)- group in which
the alkyl moiety is as defined above, and examples of the Ci-C6 alkoxy Ci-C6 alkylcarbonyl
group include a methoxyacetyl, ethoxyacetyl, propoxyacetyl, isopropoxyacetyl, butoxyacetyl,
2-methoxypropionyl, 3-methoxypropionyl, 2-ethoxypropionyl, 3-ethoxypropionyl, 2
methoxybutanoyl, 4-methoxybutanoyl, 2-methoxypentanoyl, or 5-methoxypentanoyl group.
[0100] In the present invention, unless otherwise specified, "C3-C6
cycloalkylcarbonyl group" refers to a (C 3 -C 6 cycloalkyl)-C(=O)- group in which the
cycloalkyl moiety is as defined above, and examples of the C 3 -C cycloalkylcarbonyl group
include a cyclopropanecarbonyl, cyclobutanecarbonyl, cyclopentanecarbonyl, or
cyclohexanecarbonyl group.
[0101] In the present invention, "C 3 -C 6 cycloalkyl C1-C6 alkylcarbonyl
group" refers to a (C3-C6 cycloalkyl Ci-C6 alkyl)-C(=O)- group in which the cycloalkyl alkyl
moiety is as defined above, and examples of the C 3 -C cycloalkyl C1-C alkylcarbonyl group
include a 2-cyclopropylacetyl, 2-cyclobutylacetyl, 2-cyclopentylacetyl, 2-cyclohexylacetyl, 2
cyclopropylpropanoyl, or 2-cyclopropylbutanoyl group.
[0102] In the present invention, unless otherwise specified, "C 7-C13
aralkylcarbonyl group" refers to a (C 7-C13 aralkyl)-C(=O)- group in which the aralkyl moiety
is as defined above, and examples of the C 7-C13 aralkylcarbonyl group include a
phenylethanoyl, 1-phenylpropanoyl, or 2-phenylpropanoyl group.
[0103] In the present invention, unless otherwise specified, "(Ci-C6
alkyl)thiocarbonyl group" refers to a (C1-C6 alkyl)-C(=S)- group in which the alkyl moiety is
as defined above, and examples of the (Ci-C alkyl)thiocarbonyl group include a
methylthiocarbonyl, ethylthiocarbonyl, n-propylthiocarbonyl, isopropylthiocarbonyl, n
butylthiocarbonyl, isobutylthiocarbonyl, sec-butylthiocarbonyl, tert-butylthiocarbonyl, or n
pentylthiocarbonyl group.
[0104] In the present invention, unless otherwise specified, "(Ci-C6
alkoxy)thiocarbonyl group" refers to a (C1-C6 alkyl)-O-C(=S)- group in which the alkyl
moiety is as defined above, and examples of the (C1-C6 alkoxy)thiocarbonyl group include a
methoxythiocarbonyl, ethoxythiocarbonyl, n-propoxythiocarbonyl, isopropoxythiocarbonyl,
n- butoxythiocarbonyl, isobutoxythiocarbonyl, sec-butoxythiocarbonyl, tert
butoxythiocarbonyl, n-pentoxythiocarbonyl, 1-methyl butoxythiocarbonyl, 2-methyl
butoxythiocarbonyl, 3-methyl butoxythiocarbonyl, 1-ethylpropoxythiocarbonyl, 1,1
dimethylpropoxythiocarbonyl, 1,2-dimethylpropoxythiocarbonyl, or 2,2
dimethylpropoxythiocarbonyl group.
[0105] In the present invention, "mono(C-C alkyl)aminothiocarbonyl
group" refers to a (C1-C6 alkyl)-NH-C(=S)- group in which the alkyl moiety is as defined
above, and examples of the mono(C-C6 alkyl)aminothiocarbonyl group include a
methylaminothiocarbonyl, ethylaminothiocarbonyl, n-propylaminothiocarbonyl, isopropylaminothiocarbonyl, n-butylaminothiocarbonyl, isobutylaminothiocarbonyl, see butylaminothiocarbonyl, tert-butylaminothiocarbonyl, n-pentylaminothiocarbonyl, 1 methylbutylaminothiocarbonyl, 2-methylbutylaminothiocarbonyl, 3 methylbutylaminothiocarbonyl, 1-ethylpropylaminothiocarbonyl, 1,1 dimethylpropylaminothiocarbonyl, 1,2-dimethylpropylaminothiocarbonyl, 2,2 dimethylpropylaminothiocarbonyl, or n-hexylaminothiocarbonyl group.
[0106] In the present invention, "di(C1-C alkyl)aminothiocarbonyl group"
refers to a (Ci-C6 alkyl) 2-N-C(=S)- group in which the alkyl moiety is as defined above, and
the two alkyl groups may be different from each other, and examples of the di(C1-C6
alkyl)aminothiocarbonyl group include a dimethylaminothiocarbonyl,
diethylaminothiocarbonyl, di(n-propyl)aminothiocarbonyl, diisopropylaminothiocarbonyl,
dibutylaminothiocarbonyl, N-ethyl-N-methylaminothiocarbonyl, N-methyl-N
propylaminothiocarbonyl, N-isopropyl-N-methylaminothiocarbonyl, N-butyl-N
methylaminothiocarbonyl, N-(s-butyl)-N-methylaminothiocarbonyl, N-isobutyl-N
methylaminothiocarbonyl, N-pentyl-N-methylaminothiocarbonyl, N-ethyl-N
propylaminothiocarbonyl, N-ethyl-N-isopropylaminothiocarbonyl, or N-ethyl-N
butylaminothiocarbonyl group.
[0107] In the present invention, "mono(C1-C6 alkyl)aminosulfonyl group"
refers to a (C1-C6 alkyl)-NH-S(=O)- group in which the alkyl moiety is as defined above, and
examples of the mono(Ci-C6 alkyl)aminosulfonyl group include a methylaminosulfonyl,
ethylaminosulfonyl, n-propylaminosulfonyl, isopropylaminosulfonyl, n-butylaminosulfonyl,
isobutylaminosulfonyl, sec-butylaminosulfonyl, tert-butylaminosulfonyl, n
pentylaminosulfonyl, 1-methylbutylaminosulfonyl, 2-methylbutylaminosulfonyl, 3
methylbutylaminosulfonyl, 1-ethylpropylaminosulfonyl, 1,1-dimethylpropylaminosulfonyl,
1,2-dimethylpropylaminosulfonyl, 2,2-dimethylpropylaminosulfonyl, or n
hexylaminosulfonyl group.
[0108] In the present invention, "di(C1-C6 alkyl)aminosulfonyl group" refers
to a (Ci-C6 alkyl)2-N-S(=0)2- group in which the alkyl moiety is as defined above, and the two alkyl groups may be different from each other, and examples of the di(C1-C6 alkyl)aminosulfonyl group include a dimethylaminosulfonyl, diethylaminosulfonyl, di(n propyl)aminosulfonyl, diisopropylaminosulfonyl, dibutylaminosulfonyl, N-ethyl-N methylaminosulfonyl, N-methyl-N-propylaminosulfonyl, N-isopropyl-N methylaminosulfonyl, N-butyl-N-methylaminosulfonyl, N-(s-butyl)-N-methylaminosulfonyl,
N-isobutyl-N-methylaminosulfonyl, N-pentyl-N-methylaminosulfonyl, N-ethyl-N
propylaminosulfocarbonyl, N-ethyl-N-isopropylaminosulfocarbonyl, or N-ethyl-N
butylaminosulfonyl group.
[0109] In the present invention, "aminocarbonyl C1-C 6 alkyl group" refers to
a H2N-C(=)-(Ci-C 6 alkyl)- group in which the alkyl moiety is as defined above, and
examples of the aminocarbonyl C1-C6 alkyl group include a carbamoylmethyl, 1
carbamoylethyl, or 2-carbamoylethyl group.
[0110] In the present invention, "mono(C1-C6 alkyl)aminocarbonyl C1-C6
alkyl group" refers to a (C1-C6 alkyl)-NH-C(=O)-(Ci-C 6 alkyl)- group in which the alkyl
moiety is as defined above, and examples of the mono(C1-C6 alkyl)aminocarbonyl C1-C6
alkyl group include a N-methylcarbamoylmethyl, N-ethylcarbamoylmethyl, or N-(tert
butyl)carbamoylmethyl group.
[0111] In the present invention, "mono(C1-C6 haloalkyl)aminocarbonyl Ci
C6 alkyl group" refers to a (C1-C6 haloalkyl)-NH-C(=O)-(C1-C 6 alkyl)- group in which the
haloalkyl moiety is as defined above, and examples of the mono(Ci-C6
haloalkyl)aminocarbonyl C1-C 6 alkyl group include a N-(2,2-difluoroethyl)carbamoylmethyl,
N-(2,2,2-trifluoroethyl)carbamoylmethyl, 1-{N-(2,2-difluoroethyl)carbamoyl}ethyl, 1-{N
(2,2-trifluoroethyl)carbamoyl]}ethyl, 1-{N-(2,2-difluoroethyl)carbamoyl}-1-methylethyl, or
1-{N-(2,2-trifluoroethyl)carbamoyl}-1-methylethyl group.
[0112] In the present invention, "mono(C3-C6 cycloalkyl)aminocarbonyl Ci
C6 alkyl group" refers to a (C 3 -C cycloalkyl)-NH-C(=O)-(Ci-C6 alkyl)- group in which the
cycloalkyl moiety is as defined above, and examples of the mon(C 3 -C
cycloalkyl)aminocarbonyl Ci-C6 alkyl group include a N-cyclopropylcarbamoylmethyl, N- cyclobutylcarbamoylmethyl, N-cyclopentylcarbamoylmethyl, or N cyclohexylcarbamoylmethyl group.
[0113] In the present invention, "di(C1-C alkyl)aminocarbonyl C1-C6 alkyl
group" refers to a (Ci-C alkyl)2-N-C(=O)-(Ci-C6 alkyl)- group in which the alkyl moiety is
as defined above, and examples of the di(C1-C6 alkyl)aminocarbonyl C1-C6 alkyl group
include a N,N-dimethylcarbamoylmethyl, N,N-diethylcarbamoylmethyl, N,N
dipropylcarbamoylmethyl, N-ethyl-N-methylcarbamoylmethyl, or N-methyl-N
propylcarbamoylmethyl group.
[0114] In the present invention, unless otherwise specified, "C1-C6
alkoxyimino group" refers to a (Ci-C6 alkyl)-O-N=C- group in which the alkyl moiety is as
defined above, and examples of the C1-C alkoxyimino group include a methoxyimino,
ethoxyimino, or isopropoxyimino group.
[0115] In the present invention, unless otherwise specified, "hydroxyimino
Ci-C 6 alkyl group" refers to a HO-N=(Ci-C 6 alkyl) group in which the alkyl moiety is as
defined above, and examples of the hydroxyimino C1-C 6 alkyl group include a 1
(hydroxyimino)ethyl, 2-(hydroxyimino)ethyl, 1-(hydroxyimino)propyl, 2
(hydroxyimino)propyl, or 3-(hydroxyimino)propyl group.
[0116] In the present invention, unless otherwise specified, "C1-C6
alkoxyimino C1-C 6 alkyl group" refers to a (C1-C6 alkyl)-O-N=(Ci-C 6 alkyl) group in which
the alkyl moiety is as defined above, and examples of the Ci-C6 alkoxyimino Ci-C6 alkyl
group include a 1-(methoxyimino)ethyl, 2-(methoxyimino)ethyl, 1-(methoxyimino)propyl, 2
(methoxyimino)propyl, 3-(methoxyimino)propyl, 1-(ethoxyimino)ethyl, 2-(ethoxyimino)ethyl,
1-(ethoxyimino)propyl, 2-(ethoxyimino)propyl, 3-(ethoxyimino)propyl, 1
(isopropoxyimino)ethyl, or 2-(isopropoxyimino)ethyl group.
[0117] In the present invention, unless otherwise specified, "amino C1-C6
alkyl group" refers to a H 2N-(Ci-C6 alkyl)- group in which the alkyl moiety is as defined
above, and examples of the amino C1-C6 alkyl group include an aminomethyl, or 2
aminoethyl group.
[0118] In the present invention, unless otherwise specified, "mono(C1-C6
alkyl)amino Ci-C 6 alkyl group" refers to a (Ci-C alkyl)-NH-(Ci-C6 alkyl)- group in which
the alkyl moiety is as defined above, and examples of the mono(C-C alkyl)amino C1-C
alkyl group include a N-methylaminomethyl, or N-ethylaminomethyl group.
[0119] In the present invention, unless otherwise specified, "di(C1-C6
alkyl)amino C1-C 6 alkyl group" refers to a (C-C alkyl) 2-N-(Ci-C6 alkyl)- group in which
the alkyl moiety is as defined above, and examples of the di(C1-C alkyl)amino C 1-C 6 alkyl
group include a N,N-dimethylaminomethyl or N,N-diethylaminomethyl group.
[0120] In the present invention, unless otherwise specified, "tri(C1-C
alkyl)silyloxy C1-C6 alkyl group" refers to a (Ci-C alkyl)3-Si-O-(Ci-C6 alkyl)- group in
which the alkyl moiety is as defined above, and examples of the tri(C1-C6 alkyl)silyloxy C 1
C6 alkyl group include a trimethylsilyloxymethyl, trimethylsilyloxyethyl,
triethylsilyloxymethyl,triethylsilyloxyethyl,triisopropylsilyloxymethyl,
triisopropylsilyloxyethyl,tert-butyldimethylsilyloxymethyl,ortert-butyldimethylsilyloxyethyl
group.
[0121] In the present invention, the wording "agriculturally acceptable salt"
or "salt" refers to a salt of a hydroxyl group, a carboxyl group, an amino group or the like
when such a group exists in the structure of the present compound represented by general
formula [I] or [II], or a nitrogen atom in a pyridine ring, with metal or an organic base, or a
salt with a mineral acid or an organic acid, and examples of the metal include alkali metal
such as sodium or potassium, and alkali earth metal such as magnesium or calcium, examples
of the organic base include triethylamine or diisopropylamine, examples of the mineral acid
include phosphoric acid, hydrochloric acid, hydrobromic acid, hydroiodic acid, boric acid, or
sulfuric acid, and examples of the organic acid include formic acid, acetic acid, lactic acid,
ascorbic acid, succinic acid, fumaric acid, maleic acid, oxalic acid, citric acid, benzoic acid,
salicylic acid, tartaric acid, methanesulfonic acid, 4-toluenesulfonic acid, or
trifluoromethanesulfonic acid.
[0122] Next, representative compound examples of compounds included in the pyrazole derivative of the present invention represented by general formula [I] are shown in Table I to Table 194, and representative compound examples of compounds included in the pyrazole derivative of the present invention represented by general formula [II] are shown in
Table 195 to Table 314. However, the compounds included in the derivatives of the present
invention are not limited to these. The compound numbers in Tables are referred to in the
following description.
[0123] The compounds included in the pyrazole derivatives of the present
invention can have geometrical isomers of E-form and Z-form depending on the kind of the
substituent, and the present invention encompasses such E-form, Z-form, or a mixture
containing E-form and Z-form in any ratio. The compounds encompassed in the present
invention can have optical isomers caused by the existence of one or two or more asymmetric
carbon atoms and asymmetric sulfur atoms, and the present invention encompasses any
optically active substances, racemic modifications, or diastereomers.
[0124] In the present specification, the following signs in tables respectively
represent the corresponding groups as shown below.
[0125]
Me: methyl
Et: ethyl
Pr: n-propyl
i-Pr: isopropyl
Bu: n-butyl
t-Bu: tert-butyl
OMe: methoxy
O(i-Pr): isopropoxy
2-CF 3 : 2-trifluoromethyl
4-Me,2-CF 3 : 4-methyl-2-trifluoromethyl
2-CF3-pyridin-3-yl: 2-trifluoromethylpyridine-3-yl
3,6-Cl2-pyridin-2-yl: 3,6-dichloropyridine-2-yl
CH 2 OTBS: tert-butyldimethylsilyloxymethyl
C(=O(4-Cl)Ph: 4-chlorobenzoyl
[0126]
[Table 1]
(O) _R1 R5 R6 (R 8 )m
oom pound R RR R Rb R/ ( p A-0001 HWWTHTHTHW H H H 0 A-0002 H HH H HC H H 2-F 0) A-0003 HWWTHTHTHW H H 3-F 0 A-0004 WWH WTHWHT H H 4-F 0) A-0005 HWWTHTHTHW H H 2 -Cl1 0 A-0006 H HH HHO0 H H 3 -Cl1 0 A-0007 H HH HHO0 H H 4-Cl1 0 A-0008 H H H H H 0 H H 2-B r 0 A-0009 HWWTHTHTHW H H 3-BEr 0 A-0010 HWWWTHWW H H 4-BEr 0 A-001 1 HWWWTHWT H H 2-1 0 A-001 2 H HH HHO0 H H 3-1 0 A-001 3 WWH WTHWHT H H 4-1 0 A-001 4 HWWTHTHTHW H H 2-O H 0 A-00O15 H HH HHO0 H H 3-O0H 0 A-00 16 H HH HHO0 H H 4-O H 0 A-00 17 H HH H HC H H 2-SH 0 A-001 8 HJHWH H HW H H 3-SH0 A-001 9 H HWH H HW H H 4-SH 0 A-0020 H HH HHO0 H H 2-M e 0 A-0021 WWHWHHWHT H H 3-M e 0 A-0022 H HH H HC H H 4-M e 0 A-0023 H HWH H HW H H 2-Et 0 A-0024 H H H H H 0 H H 3-Et 0F A-0025 H HH HHO0 H H 4-Et 0 A-0026 H HH HHO0 H H 2-Pr 0 A-0027 H H H HTHE0 H H 3-Pr 0 A-0028 H HH H HC H H 4-Pr 0 A-0029 HTHWHETTHW H H 2-i-Pr 0 A-0030 HTHWHETTHW H H 3-i-Pr 0 A-0031 H HWH HVHV0 H H 4-i-Pr 0 A-0032 H H H H H 0 H H 2-Eu 0 A-0033 H HH HHO0 H H 3-Eu 0 A-0034 H HH HHO0 H H 4-E u 0 A-0035 H HH HHO0 H H 2-s-E u 0 A-0036 HWHTH1H1H H H 3-s-Eu 0 A-003 7 H HH H HC H H 4-s-Eu0 A-0038 HTHWHETTHW H H 2-i-Eu0 A-0039 H HH HHO0 H H 3-i-Eu 0 A-0040 HTHWHETTHW H H 4-i-Eu 0 A-0041 HTHFHEHTHT H H 2 -t-E u 0 A-0042 HTHWHETTHW H H 3 -t-E u0 A-0043 H HH HHO0 H H 4 -t-E u0 A-0044 H HH HHO0 H H 2 -CF3 0 A-0045 H HFH H HT H H 3-CF3, 0 A-0046 H HH HHO0 H H 4 -CF3 0 A-0047 H HWH HVH 0 H H 2-CH F 2 0 A-0048 HWHTH1H HW H H 3-CH F 2 0 A-0049 HWWTHTH HT H H 4-CH F2 0 A-0050 HHHHH H H 2 -CH2F 0 A-0051 HH HH H H 3 -CH2F 0 A-0052 UETTE H H 4-CH 2F 0
[0127]
[Table 2]
com pound RI R2 R R R A R R' (R)m P A-0053 H H H H H 0 H H 2-CF 2C1 0 A-0054 H H H H H 0 H H 3-CF 2C1 0 A-0055 H H H H H 0 H H 4-CF 2C1I 0 A-0056 H H H H H 0 H H 2-CF(CF,) 2 0 A-005 7 H H H H H 0 H H 3-CF(CF 3 ) 2 0 A-005 8 H H H H H 0 H H 4-CF(CF 3 ) 2 0 A-0059 H H H H H 0 H H 2-cycbpropyl 0 A-0060 H H H H H 0 H H 3-cycbpropyl 0 A-0061 H H H H H 0 H H 4-cycbpropyl 0 A-0062 H H H H H 0 H H 2-cycbbutyl 0 A-0063 H H H H H 0 H H 3-cycbbutyl 0 A-0064 H H H H H 0 H H 4-cycbbutyl 0 A-0065 H H H H H 0 H H 2-cycbpentyl 0 A-0066 H H H H H 0 H H 3-cycbpentyl 0 A-0067 H H H H H 0 H H 4-cycbpentyl 0 A-0068 H H H H H 0 H H 2-(cycbpropyh ethyl) 0 A-0069 H H H H H 0 H H 3-(cycbpropyh ethyl) 0 A-0070 H H H H H 0 H H 4-(cycbpropyh ethyD 0 A-0071 H H H H H 0 H H 2-(cycobbuty IethyD 0 A-0072 H H H H H 0 H H 3-(cycobbutyImethyD 0 A-0073 H H H H H 0 H H 4-(cycobbuty IethyD 0 A-0074 H H H H H 0 H H 2-(cycbpentyh ethyl) 0 A-0075 H H H H H 0 H H 3-(cycbpentyhmethyD 0 A-0076 H H H H H 0 H H 4-(cycbpentyh ethyD 0 A-0077 H H H H H 0 H H 2-(cycobpropylethyD 0 A-0078 H H H H H 0 H H 3-(cycobpropylethyD 0 A-0079 H H H H H 0 H H 4-(cycobpropylethyD 0 A-0080 H H H H H 0 H H 2-(2,2-difluorocyclopropyD 0 A-0081 H H H H H 0 H H 3-(2,2-difluorocyclopropyD 0 A-0082 H H H H H 0 H H 4-(2,2-difluorocyclopropyD 0 A-0083 H H H H H 0 H H 2-(2,2-dichbrocycbpropyD 0 A-0084 H H H H H 0 H H 3-(2,2-dichbrocycbpropyD 0 A-0085 H H H H H 0 H H 4-(2,2-dichbrocycbpropyD 0 A-0086 H H H H H 0 H H 2-ethenyl 0 A-0087 H H H H H 0 H H 3-ethenyl 0 A-0088 H H H H H 0 H H 4-ethenyl 0F A-0089 H H H H H 0 H H 2-aIlyl 0 A-0090 H H H H H 0 H H 3-allyl 0 A-0091 H H H H H 0 H H 4-aIlyl 0 A-0092 H H H H H 0 H H 2-(prop-1-en-1-yD 0 A-0093 H H H H H 0 H H 3-(prop-1-en-1-yD 0 A-0094 H H H H H 0 H H 4-(prop-1-en-1-yD 0 A-0095 H H H H H 0 H H 2-(trifluoroethenyD 0 A-0096 H H H H H 0 H H 3-(trifluoroethenyD 0 A-0097 H H H H H 0 H H 4-(trifluoroethenyD 0 A-0098 H H H H H 0 H H 2-(2,2-dich broethenyD 0 A-0099 H H H H H 0 H H 3-(2,2-dichbroethenyD 0 A-0100 H H H H H 0 H H 4-(2,2-dichbroethenyD 0 A-0101 H H H H H 0 H H 2-ethyny 1 0 A-0102 H H H H H 0 H H 3-ethyny 1 0 A-0103 H H H H H 0 H H 4-ethyny 1 0 A-0104 H H H H H 0 H H 2-(1-propyn-1-yD 0 A-0105 H H H H H 0 H H 3-(1-propyn-1-yD 0 A-0106 H H H H H 0 H H 4-(1-propyn-1-yD 0 A-0107 H H H H H 0 H H 2-(2-propyn-1-yD 0 A-0108 H H H H H 0 H H 3-(2-propyn-1-yD 0 A-0109 H Hf H H 0 H H 4-(2-propyn-1-yl) 0
[0128]
[Table 3]
com pound RI R2 R R R A R R' (R)m P A-0110 H H H H H 0 H H 2-(2-cyclopropylethynyD 0 A-0111 H H H H H 0 H H 3-(2-cyclopropylethynyD 0 A-0112 H H H H H 0 H H 4-(2-cyclopropylethyny 0 A-0113 H H H H H 0 H H 2-(2-chbroethynyD 0 A-0114 H H H H H 0 H H 3-(2-chbroethynyD 0 A-01 15 H H H H H 0 H H 4-(2-chbroethynyD 0 A-0116 H H H H H 0 H H 2-(2-brom oethynyD 0 A-0117 H H H H H 0 H H 3-(2-brom oethynyD 0 A-0 1 18 H H H H H 0 H H 4-(2-brom oethynyD 0 A-0119 H H H H H 0 H H 2-0Me 0 A-0120 H H H H H 0 H H 3-0Me 0 A-0121 H H H H H 0 H H 4-0Me 0 A-0122 H H H H H 0 H H 2-0Et 0 A-0123 H H H H H 0 H H 3-0Et 0 A-0124 H H H H H 0 H H 4-0Et 0 A-0125 H H H H H 0 H H 2-0Pr 0 A-0126 H H H H H 0 H H 3-0Pr 0 A-0127 H H H H H 0 H H 4-0Pr 0 A-0128 H H H H H 0 H H 2-0(/-Pr) 0 A-0129 H H H H H 0 H H 3-0(/-Pr) 0 A-0130 H H H H H 0 H H 4-0(/-Pr) 0 A-0131 H H H H H 0 H H 2-0Bu 0 A-0132 H H H H H 0 H H 3-0Bu 0 A-0133 H H H H H 0 H H 4-0Bu 0 A-0134 H H H H H 0 H H 2-0 (s-Bu) 0 A-0135 H H H H H 0 H H 3-0 (s-Bu) 0 A-0136 H H H H H 0 H H 4-0 (s-Bu) 0 A-0137 H H H H H 0 H H 2-0(/-Bu) 0 A-0138 H H H H H 0 H H 3-0 (/-Bu) 0 A-0139 H H H H H 0 H H 4-0 (/-Bu) 0 A -0140 H H H H H 0 H H 2-0 (t-Bu) 0 A -0141 H H H H H 0 H H 3-0 (t-Bu) 0 A -0142 H H H H H 0 H H 4-0 (t-Bu) 0 A-0143 H H H H H 0 H H 2-00F 0 A-0144 H H H H H 0 H H 3-0CF, 0 A-0145 H H H H H 0 H H 4-00F 0 A-0146 H H H H H 0 H H 2-0CHF 2 0 A-0147 H H H H H 0 H H 3-0CHF 2 0 A-0148 H H H H H 0 H H 4-0CHF 2 0 A-0149 H H H H H 0 H H 2-0CH 2 CF 0 A-0150 H H H H H 0 H H 3-0CH 2 CF3 0 A-0151 H H H H H 0 H H 4-0CH 2 CF3 0 A-0152 H H H H H 0 H H 2-(cycbpropy bxy) 0 A-0153 H H H H H 0 H H 3-(cycbpropy bxy) 0 A-0154 H H H H H 0 H H 4-(cycbpropy bxy) 0 A-0155 H H H H H 0 H H 2-(cycobbutyloxy) 0 A-0156 H H H H H 0 H H 3-(cycobbutybxy) 0 A-0157 H H H H H 0 H H 4-(cycobbutybxy) 0 A-0158 H H H H H 0 H H 2-(cycbpentybxy) 0 A-0159 H H H H H 0 H H 3-(cycbpentybxy) 0 A-0160 H H H H H 0 H H 4-(cycbpentybxy) 0 A-0161 H H H H H 0 H H 2-((2,2-dichbrocycbpropyDoxy) 0 A-0162 H H H H H 0 H H 3-((2,2-dichbrocycbpropyDoxy) 0 A-0163 H H H H H 0 H H 4-((2,2-dichbrocycbpropyDoxy) 0 A-0164 H H H H H 0 H H 2-(cycbpropyh ethoxy) 0 A-065 H H H H H 0 H H 3-(cycbpropyh ethoxy) 0 A-0166 f FH IH 0 H H 4-(cycbpropyh ethoxy) 0
[0129]
[Table 4]
com pound RI R2 R R R A R R' (R)m P A-0167 H H H H H 0 H H 2-((2,2-difluorocycobpropyDm ethoxy) 0 A-0168 H H H H H 0 H H 3-((2,2-difluorocycbpropylm ethoxy) 0 A-0169 H H H H H 0 H H 4-((2,2-difluorocycobpropyDm ethoxy) 0 A-0170 H H H H H 0 H H 2-(oxiran-2-yD 0 A-0171 H H H H H 0 H H 3-(oxiran-2-yD 0 A-0172 H H H H H 0 H H 4-(oxiran-2-yD 0 A-0173 H H H H H 0 H H 2-(oxiran-2-yh ethyD 0 A-0174 H H H H H 0 H H 3-(oxiran-2-yh ethyD 0 A-0175 H H H H H 0 H H 4-(oxiran-2-yh ethyD 0 A-0176 H H H H H 0 H H 2-SMe 0 A-0177 H H H H H 0 H H 3-SMe 0 A-0178 H H H H H 0 H H 4-SMe 0 A-0179 H H H H H 0 H H 2-SEt 0 A-0180 H H H H H 0 H H 3-SEt 0 A-0181 H H H H H 0 H H 4-SEt 0 A-0182 H H H H H 0 H H 2-S(=0)Me 0 A-0183 H H H H H 0 H H 3-S(=0)Me 0 A-0184 H H H H H 0 H H 4-S(=0)Me 0 A-0185 H H H H H 0 H H 2-S(=0) 2 Me 0 A-0186 H H H H H 0 H H 3-S(=0) 2Me 0 A-0187 H H H H H 0 H H 4-S(=0) 2Me 0 A-0188 H H H H H 0 H H 2-SCF, 0 A-0189 H H H H H 0 H H 3-SCF, 0 A-0190 H H H H H 0 H H 4-SCF, 0 A-0191 H H H H H 0 H H 2-S(=0)GCF 0 A-0192 H H H H H 0 H H 3-S(=0)GCF 0 A-0193 H H H H H 0 H H 4-S(=0)G03 0 A-0194 H H H H H 0 H H 2-S (=0) 2CF3 0 A-0195 H H H H H 0 H H 3-S (=0) 2CF3 0 A-0196 H H H H H 0 H H 4-S (=0) 2 F3 0 A-0197 H H H H H 0 H H 2-SCF(CF3) 2 0 A-0198 H H H H H 0 H H 3-SCF(CF3) 2 0 A-0199 H H H H H 0 H H 4-SCF(CF3) 2 0 A-0200 H H H H H 0 H H 2-(cycobpropyfthio) 0 A-0201 H H H H H 0 H H 3-(cycobpropyfthio) 0 A-0202 H H H H H 0 H H 4-(cycobpropyfthio) 0 A-0203 H H H H H 0 H H 2-(cycbpropylsulfhyl) 0 A-0204 H H H H H 0 H H 3-(cycbpropylsulfhy) 0 A-0205 H H H H H 0 H H 4-(cycbpropylsulfhy) 0 A-0206 H H H H H 0 H H 2-(cycobpropysufonyD 0 A-0207 H H H H H 0 H H 3-(cycbpropysulfonyD 0 A-0208 H H H H H 0 H H 4-(cycbpropysulfonyD 0 A-0209 H H H H H 0 H H 2-((cycobpropyhiethyDthio) 0 A-0210 H H H H H 0 H H 3-((cycobpropyhiethyDthio) 0 A-0211 H H H H H 0 H H 4-((cycobpropyhi ethyDth io) 0 A-0212 H H H H H 0 H H 2-((cycbpropyhi ethyDsulfinyD 0 A-0213 H H H H H 0 H H 3-((cycbpropyhi ethyDsulfinyD 0 A-0214 H H H H H 0 H H 4-((cycbpropyhi ethyDsulfinyD 0 A-0215 H H H H H 0 H H 2-((cyclopropyhiethyDsulfonyD 0 A-0216 H H H H H 0 H H 3-((cyclopropyhiethyDsulfonyD 0 A-0217 H H H H H 0 H H 4-((cyclopropyhiethyDsulfonyD 0 A-0218 H H H H H 0 H H 2-(((2,2-difluorocycbpropyDm ethyDthio) 0 A-0219 H H H H H 0 H H 3-(((2,2-difluorocycbpropyDm ethyDthio) 0 A-0220 H H H H H 0 H H 4-(((2,2-diflorocycbpropyDm ethyDthio) 0 A-0221 H H H H H 0 H H 2-(((2,2-difluorocycbpropyDm ethyDsulfinyD 0 A-0222 H H H H H 0 H H 3-(((2,2-difluorocycbpropyDm ethyDsulfinyD 0 A-0223 H H H H H0 H H 4-(((2,2-dfluorocycbpropyDm ethyDsulfinyl 0
[0130]
[Table 5]
com pound R' R2 R R A R R' (R)m p A-0224 H H H D 0 H H 2-(((2,2-difluorocycbpropyDm ethyDsultonyD 0 A-0225 H H H H i 0 H H 3-(((2,2-difuorocycbpropylDm ethysultonyD A-0226 H H H H 0 H H 4-(((2,2-difuorocycbpropylm ethysultonyD A-0227 H H H H H H H 2-0(=U)Me A-0228 H H H H H H H 3-0(=)Me 0 A-0229 H H H H 0Di H H 4-0(=)Me 0 A-0230 H H H H 0Di H H 2-0(=O)Et 0 A-0231 H H H H 0Di H H 3-0(=O)Et 0 A-0232 H H H H H 0 H H 4-C(=0)Et 0 A-0233 H H H H 0 H H 2-C(=0)G H3 A-0234 H H H H f0 H H 3-C(=0)G3 0 A-0235 H H H H 0 H H 4-C(=0)G H3 A-0236 H H H H f0 H H 2-G(=0)UMe 0 A-0237 H H H H 0 H H 3-G(=0)0Me 0 A-0238 H H H H 0 H H 4-G(=0)0Me 0 A-0239 H H H H Hi0 H H 2-C(=0)UEt 0 A-0240 H H H H HD0 H H 3-C(=0)UEt 0 A-0241 H H H H 0 H H 4-C(=0)0Et 0 A-0242 H H H H Hi0 H H 2-C(=0)NH 2 0 A-0243 H H H H 0 H H 3-C(=0)NH 2 0 A-0244 H H H H Hi0 H H 4-C(=0)NH 2 0 A-0245 H H H H f0 H H 2-C(=0)NHMe 0 A-0246 H H H H 0 H H 3-C(=0)NHMe 0 A-0247 H H H H f0 H H 4-C(=0)NHMe 0 A-0248 H H H H HD0 H H 2-C(=0)NMe 2 0 A-0249 H H H H f0 H H 3-C(=0)NMe 2 0 A-0250 H H H H f0 H H 4-C(=0)NMe 2 0 A-0251 H H H H i 0 H H 2-CH 2C(=0)CH 3 0 A-0252 H H H H 0 H H 3-CH 2 C(=0)CH 3 0
A-0253 H H H H 0 H H 4-CH 2 C(=0)CH 3 0 A-0254 H H H H 0 H H 2-CH 2 C(=0)0F 3 0 A-0255 H H H H 0 H H 3-CH 2 C(=0)0F 3 0 A-0256 H H H H HD0 H H 4-CH 2 C(=0)0F 3 0 A-0257 H H H H Hi0 H H 2-CH 2C(=0)0H 3 0 A-0258 H H H H 0 H H 3-CH 2C(=0)0H 3 0
A-0259 H H H H 0 H H 4-CH 2C(=0)0H 3 0
A-0260 H H H H HD0 H H 2-CH 20H 0 A-0261 H H H H f Di H H 3-CH 2 UH 0 A-0262 H H H H 0Di H H 4-CH 2 UH 0 A-0263 H H H H H 0 H H 2-CH 20H 3 0 A-0264 H H H H 0 H H 3-CH 20H 3 0 A-0265 H H H H 0 H H 4-CH 20H 3 0
A-0266 H H H H Hi0 H H 2-CH 20H 2CH 3 0 A-0267 H H H H i 0 H H 3-CH 20H 2CH 3 0
A-0268 H H H H 0 H H 4-CH 20H 2CH 3 0
A-0269 H H H H Hi0 H H 2-CH (GH 3 )0H 3 0 A-0270 H H H H 0 H H 3-CH (CH 3 )0H 3 0 A-0271 H H H H 0Di H H 4-OH (CH 3 )0H 3 0 A-0272 H H H H 0 H H 2-CH 2 CH 2 0H 3 0 A-0273 H H H H Hi0 H H 3-CH 2 CH 20H 3 0 A-0274 H H H H 0 H H 4-CH 2 CH 2 0H 3 0
A-02/b H H H H 0 H H 2-CH 20U 3 0 A-0276 H H H H H 0 H H 3-CH 20F 3 0 A-02// H H H H 0 H H 4-CH 20GF 3 A-02/8 IH H H H 0 H H 2-CF 20GH 3 0 A-0279 H H H H Hi0 H H 3-CF 20H 3 0 A-0280 H H H H 0 H H 4-F2UGCH 3 0
[0131]
[Table 6]
com pound R' R2 R R A R R' (R)m p A-0281 H H H H 0 H H 2-0FGF 2 2 0F 3 0 A-0282 H H H H H 0 H H 3-0FGF 2 2 0F 3 0 A-0283 H H H H 0 H H 4-F 20F 2 0F 3 0 A-0284 H H H H i 0 H H 2-UG(=U)GH 3 A-0285 H H H H 0 H H 3-UC(=0)CH 3 A-0286 H H H H 0 H H 4-UC(=0)GH 3 0 A-0287 H H H H 0 H H 2-UC(=0)GF 3 0 A-0288 H H H H 0 H H 3-UC(=0)GF 3 0 A-0289 H H H H 0 H H 4-UC(=0)G 3 0 A-0290 H H H H H0 H H 2-UG(=U)NH 2 0
A-0291 H H H H i 0 H H 3-UG(=U)NH 2 0 A-0292 H H H H 0 H H 4-UG(=U)NH 2 0
A-0293 H H H H f0 H H 2-O(=O)NHGH 3 0 A-0294 H H H H 0 H H 3-OC(=U)NHGH 3 0 A-0295 H H H H 0 H H 4-OC(=U)NHGH 3 0 A-0296 H H H H Hi0 H H 33-(=U)N(H 2 0 A-0297 H H H H HD0 H H 3-UG(=U)N(GH 3 2 0 A-0298 H H H H 0 H H 4-UC(=U)N(H 3) 2 0
A-0299 H H H H Hi0 H H 2-CH 2 00(=U)NH 2 0 A-0300 H H H H 0 H H 3-0H 2 00(=0)NH 2 0 A-0301 H H H H Hi0 H H 4-GH 2 00(=0)NH 2 0 A-0302 H H H H f0 H H 2-GH 200(=0)NHCH 3 0 A-0303 H H H H 0 H H 3-GH 200(=0)NHCH 3 0 A-0304 H H H H f0 H H 4-GH 20(=0)NHH 3 0 A-0305 H H H H Hi0 H H 2-CH 20(=U)N (H 33)2 A-0306 H H H H f0 H H 3-CH 200(=)N (H 3) 2 0 A-0307 H H H H f0 H H 4-CH 20(=U)N (H 3) 2 A-0308 H H H H i 0 H H 2-UC(=U)U0H 3 0 A-0309 H H H H 0 H H 3-UC(=U)UGH 3 0 A-0310 H H H H 0 H H 4-UC(=U)UGH 3 0 A-0311 H H H H 0 H H 2-GH 2 0(=U)UGH 3 0 A-0312 H H H H 0 H H 3-0H 2 0(=U)UGH 3 0 A-0313 H H H H Hi0 H H 4-GH 2 0(=U)UGH 3 0 A-0314 H H H H Hi0 H H 2-GH 20(=O)GH 3 0 A-0315 H H H H 0 H H 3-GH 20C(=U)H 3 0 A-0316 H H H H 0 H H 4-GH 20(=O)GH 3 0 A-0317 H H H H Hi0 H H 2-U S=U) 2 CH3 A-0318 H H H H 0 H H 3-US(=0) 2 CH3 A-0319 H H H H 0 H H 4-US(=0) 2 H 3 0 A-0320 H H H H H 0 H H 2-CH 2SCH 3 0 A-0321 H H H H 0 H H 3-CH 2SCH 3 0 A-0322 H H H H 0 H H 4-CH 2SCH 3 0 A-0323 H H H H Hi0 H H 2-CH 2St=U)GH 3 0 A-0324 H H H H 0 H H 3-CH 2St=U)GH 3 0
A-0325 H H H H 0 H H 4-CH 2St=U)GH 3 0
A-0326 H H H H Hi0 H H 2-CH 2St=U) 20H 3 0 A-0327 H H H H 0 H H 3-CH 2S(=0) 2 CH 3 0 A-0328 H H H H 0Di H H 4-CH 2S(=0) 2 CH 3 0 A-0329 H H H H 0 H H 2-CH 2 SGF 3 0 A-0330 H H H H Hi0 H H 3-CH 2SCF 3 0 A-0331 H H H H 0 H H 4-CH 2 SGF 3 A-0332 H H H H Hi0 H H 2-CH 2s=U)GH 3 0 A-0333 H H H H Hi0 H H 3-CH 2S=U)GF 3 A-0334 H H H H 0 H H 4-CH 2S(=0)0F 3 0 A-0335 H H H H Hi0 H H 2-CH 2S(=U) 20F 3 0 A-0336 H H H H 0 H H 3-CH 2S(=U) 20F 3 0 A-0337 FF H IH 10 H H 4-CH 2S(=U) 20F3 0
[0132]
[Table 7]
com pound RI R2 R R R A R R' (R)m P A-0338 H H H H H 0 H H 2-phenyl 0 A-0339 H H H H H 0 H H 3-phenyl 0 A-0340 H H H H H 0 H H 4-phenylI A-0341 H H H H H 0 H H 2-(phenyloxy) 0 A-0342 H H H H H 0 H H 3-(phenyloxy) 0 A-0343 H H H H H 0 H H 4-(phenyloxy) 0 A-0344 H H H H H 0 H H 2-benzyl 0 A-0345 H H H H H 0 H H 3-benzyl 0 A-0346 H H H H H 0 H H 4-benzyl 0 A-0347 H H H H H 0 H H 2-(benzybxy) 0 A-0348 H H H H H 0 H H 3-(benzybxy) 0 A-0349 H H H H H 0 H H 4-(benzybxy) 0 A-0350 H H H H H 0 H H 2-((2-fLorobenzyDoxy) 0 A-0351 H H H H H 0 H H 3-((2-fLorobenzyDoxy) 0 A-0352 H H H H H 0 H H 4-((2-fLorobenzyDoxy) 0 A-0353 H H H H H 0 H H 2-((3-fborobenzyDoxy) 0 A-0354 H H H H H 0 H H 3-((3-fLorobenzyDoxy) 0 A-0355 H H H H H 0 H H 4-((3-fLorobenzyDoxy) 0 A-0356 H H H H H 0 H H 2-((4-fLorobenzyDoxy) 0 A-0357 H H H H H 0 H H 3-((4-fLorobenzyDoxy) 0 A-0358 H H H H H 0 H H 4-((4-fborobenzyDoxy) 0 A-0359 H H H H H 0 H H 2-((2-chbrobenzyDoxy) 0 A-0360 H H H H H 0 H H 3-((2-chbrobenzyDoxy) 0 A-0361 H H H H H 0 H H 4-((2-chbrobenzyDoxy) 0 A-0362 H H H H H 0 H H 2-((3-chbrobenzyDoxy) 0 A-0363 H H H H H 0 H H 3-((3-chbrobenzyDoxy) 0 A-0364 H H H H H 0 H H 4-((3-chbrobenzyDoxy) 0 A-0365 H H H H H 0 H H 2-((4-chbrobenzyDoxy) 0 A-0366 H H H H H 0 H H 3-((4-chbrobenzyDoxy) 0 A-0367 H H H H H 0 H H 4-((4-chbrobenzyDoxy) 0 A-0368 H H H H H 0 H H 2-((2-m ethylbenzyDoxy) 0 A-0369 H H H H H 0 H H 3-((2-m ethylbenzyDoxy) 0 A-0370 H H H H H 0 H H 4-((2-m ethylbenzyDoxy) 0 A-0371 H H H H H 0 H H 2-((3-m ethylbenzyDoxy) 0 A-0372 H H H H H 0 H H 3-((3-m ethylbenzyDoxy) 0 A-0373 H H H H H 0 H H 4-((3-m ethylbenzyDoxy) 0 A-0374 H H H H H 0 H H 2-((4-m ethylbenzyDoxy) 0 A-0375 H H H H H 0 H H 3-((4-m ethylbenzyDoxy) 0 A-0376 H H H H H 0 H H 4-((4-m ethylbenzyDoxy) 0 A-0377 H H H H H 0 H H 2-((2-(trifLorom ethyDbenzyDoxy) 0 A-0378 H H H H H 0 H H 3-((2-(trifLorom ethyDbenzyDoxy) 0 A-0379 H H H H H 0 H H 4-((2-(trifborom ethyDbenzyDoxy) 0 A-0380 H H H H H 0 H H 2-((3-(trifLorom ethyDbenzyDoxy) 0 A-0381 H H H H H 0 H H 3-((3-(trifborom ethyDbenzyDoxy) 0 A-0382 H H H H H 0 H H 4-((3-(trifLorom ethy Dbenzy Doxy) 0 A-0383 H H H H H 0 H H 2-((4-(trifborom ethyDbenzyDoxy) 0 A-0384 H H H H H 0 H H 3-((4-(trifLorom ethyDbenzyDoxy) 0 A-0385 H H H H H 0 H H 4-((4-(trifLorom ethyDbenzyDoxy) 0 A-0386 H H H H H 0 H H 2-((2-m ethoxybenzyDoxy) 0 A-0387 H H H H H 0 H H 3-((2-m ethoxybenzyDoxy) 0 A-0388 H H H H H 0 H H 4-((2-m ethoxybenzyDoxy) 0 A-0389 H H H H H 0 H H 2-((3-m ethoxybenzyDoxy) 0 A-0390 H H H H H 0 H H 3-((3-m ethoxybenzyDoxy) 0 A-0391 H H H H H 0 H H 4-((3-m ethoxybenzyDoxy) 0 A-0392 H H H H H 0 H H 2-((4-m ethoxybenzyDoxy) 0 A-0393 H H H H H 0 H H 3-((4-m ethoxybenzyDoxy) 0 A-0394 H H H H H0 H H 4-((4-m ethoxybenzyDoxy) 0
[0133]
[Table 8]
com pound RI R2 R R R A R R' (R)m P A-0395 H H H H H 0 H H 2-((2-(trifluorom ethoxy)benzyDoxy) 0 A-0396 H H H H H 0 H H 3-((2-(trifluorom ethoxy)benzyDoxy) 0 A-0397 H H H H H 0 H H 4-((2-(trifluorom ethoxy)benzyDoxy) W A-0398 H H H H H 0 H H 2-((3-(trifluorom ethoxy)benzyDoxy) W A-0399 H H H H H 0 H H 3-((3-(trifluorom ethoxy)benzyDoxy) 0 A-0400 H H H H H 0 H H 4-((3-(trifluorom ethoxy)benzyDoxy) 0 A-0401 H H H H H 0 H H 2-((4-(trifluorom ethoxy)benzyDoxy) 0 A-0402 H H H H H 0 H H 3-((4-(trifluorom ethoxy)benzyDoxy) 0 A-0403 H H H H H 0 H H 4-((4-(trifluorom ethoxy)benzyDoxy) 0 A-0404 H H H H H 0 H H 2-((2-(m ethylthio)benzyDoxy) 0 A-0405 H H H H H 0 H H 3-((2-(m ethylthio)benzyl)oxy) 0 A-0406 H H H H H 0 H H 4-((2-(m ethylthio)benzyDoxy) 0 A-0407 H H H H H 0 H H 2-((3-(m ethylthio)benzyl)oxy) 0 A-0408 H H H H H 0 H H 3-((3-(m ethylthio)benzyDoxy) 0 A-0409 H H H H H 0 H H 4-((3-(m ethylthio)benzyDoxy) 0 A-0410 H H H H H 0 H H 2-((4-(m ethylthio)benzyl)oxy) 0 A-0411 H H H H H 0 H H 3-((4-(m ethylthio)benzyl)oxy) 0 A-0412 H H H H H 0 H H 4-((4-(m ethylthio)benzyDoxy) 0 A-0413 H H H H H 0 H H 2-((2-(m ethylsulhyDbenzyDoxy) 0 A-0414 H H H H H 0 H H 3-((2-(m ethylsulhyDbenzyDoxy) 0 A-0415 H H H H H 0 H H 4-((2-(m ethylsulhyDbenzyDoxy) 0 A-0416 H H H H H 0 H H 2-((3-(m ethylsulhyDbenzyDoxy) 0 A-0417 H H H H H 0 H H 3-((3-(m ethylsulhyDbenzyDoxy) 0 A-0418 H H H H H 0 H H 4-((3-(m ethylsulhyDbenzyDoxy) 0 A-0419 H H H H H 0 H H 2-((4-(m ethylsulhyDbenzyDoxy) 0 A-0420 H H H H H 0 H H 3-((4-(m ethylsulhyDbenzyDoxy) 0 A-0421 H H H H H 0 H H 4-((4-(m ethylsulhyDbenzyDoxy) 0 A-0422 H H H H H 0 H H 2-((2-(m ethyIsulfonyDbenzyDoxy) 0 A-0423 H H H H H 0 H H 3-((2-(m ethyIsulfonyDbenzyDoxy) 0 A-0424 H H H H H 0 H H 4-((2-(m ethyIsulfonyDbenzyDoxy) 0 A-0425 H H H H H 0 H H 2-((3-(m ethyIsulfonyDbenzyDoxy) 0 A-0426 H H H H H 0 H H 3-((3-(m ethyIsulfonyDbenzyDoxy) 0 A-0427 H H H H H 0 H H 4-((3-(m ethyIsulfonyDbenzyDoxy) 0 A-0428 H H H H H 0 H H 2-4-(m ethyIsulfonyDbenzyloxy) 0 A-0429 H H H H H 0 H H 3-((4-(m ethyIsulfonyDbenzyDoxy) 0 A-0430 H H H H H 0 H H 4-((4-(m ethyIsulfonyDbenzyDoxy) 0 A-0431 H H H H H 0 H H 2-((2-(trifluorom ethylthio)benzyDoxy) 0 A-0432 H H H H H 0 H H 3-((2-(trifluorom ethylthio)benzyDoxy) 0 A-0433 H H H H H 0 H H 4-((2-(trifluorom ethylthio)benzyDoxy) 0 A-0434 H H H H H 0 H H 2-((3-(trifluorom ethylthio)benzyDoxy) 0 A-0435 H H H H H 0 H H 3-((3-(trifluorom ethylthio)benzyDoxy) 0 A-0436 H H H H H 0 H H 4-((3-(trifluorom ethylthio)benzyDoxy) 0 A-0437 H H H H H 0 H H 2-((4-(trifluorom ethylthio)benzyDoxy) 0 A-0438 H H H H H 0 H H 3-((4-(trifluorom ethylthio)benzyDoxy) W A-0439 H H H H H 0 H H 4-((4-(trifluorom ethy lth io)benzy Doxy) 0 A-0440 H H H H H 0 H H 2-((2-(trifluorom ethyIsulfinyDbenzyDoxy) 0 A-0441 H H H H H 0 H H 3-((2-(trifluorom ethyIsulfinyDbenzyDoxy) 0 A-0442 H H H H H 0 H H 4-((2-(trifluorom ethyIsulfinyDbenzyDoxy) 0 A-0443 H H H H H 0 H H 2-((3-(trifluorom ethyIsulfinyDbenzyDoxy) 0 A-0444 H H H H H 0 H H 3-((3-(trifluorom ethyIsulfinyDbenzyDoxy) 0 A-0445 H H H H H 0 H H 4-((3-(trifluorom ethyIsulfinyDbenzyDoxy) 0 A-0446 H H H H H 0 H H 2-((4-(trifluorom ethyIsulfinyDbenzyDoxy) 0 A-0447 H H H H H 0 H H 3-((4-(trifluorom ethyIsulfinyDbenzyDoxy) 0 A-0448 H H H H H 0 H H 4-((4-(trifluorom ethyIsulfinyDbenzyDoxy) 0 A-0449 H H H H H 0 H H 2-((2-(trifluorom ethylsulfonyI)benzyDoxy) 0 A-0450 H H H H H 0 H H 3-((2-(trifluorom ethylsulfonyI)benzyDoxy) 0 A-0451 H H H H H0 H H 4-((2-(trfluorom ethylsulfonyl)benzyDoxy) 0
[0134]
[Table 9]
com pound RI R2 R R R A R R' (R)m P A-0452 H H H H H 0 H H 2-((3-(trifluorom ethybulfonyI)benzyDoxy) 0 A-0453 H H H H H 0 H H 3-((3-(trifluorom ethybulfonyI)benzyDoxy) 0 A-0454 H H H H H 0 H H 4-((3-(trifluorom ethybulfonyI)benzyDoxy) W A-0455 H H H H H 0 H H 2-((4-(trifluorom ethybulfony)benzyDoxy) W A-0456 H H H H H 0 H H 3-((4-(trifluorom ethybulfonyI)benzyDoxy) 0 A-0457 H H H H H 0 H H 4-((4-(trifluorom ethybulfonyI)benzyDoxy) 0 A-0458 H H H H H 0 H H 2-((2-am inobenzyDoxy) 0 A-0459 H H H H H 0 H H 3-((2-am inobenzyDoxy) 0 A-0460 H H H H H 0 H H 4-((2-am inobenzyDoxy) 0 A-0461 H H H H H 0 H H 2-((3-am inobenzyDoxy) 0 A-0462 H H H H H 0 H H 3-((3-am inobenzy)oxy) 0 A-0463 H H H H H 0 H H 4-((3-am inobenzyDoxy) 0 A-0464 H H H H H 0 H H 2-((4-am inobenzy)oxy) 0 A-0465 H H H H H 0 H H 3-((4-am inobenzyDoxy) 0 A-0466 H H H H H 0 H H 4-((4-am inobenzyDoxy) 0 A-0467 H H H H H 0 H H 2-((2-(m ethybm ho)benzyDoxy) 0 A-0468 H H H H H 0 H H 3-((2-(m ethybm ho)benzyDoxy) 0 A-0469 H H H H H 0 H H 4-((2-(m ethybm ho)benzyDoxy) 0 A-0470 H H H H H 0 H H 2-((3-(m ethybm ho)benzyDoxy) 0 A-0471 H H H H H 0 H H 3-((3-(m ethybm ho)benzyDoxy) 0 A-0472 H H H H H 0 H H 4-((3-(m ethybm ho)benzyDoxy) 0 A-0473 H H H H H 0 H H 2-((4-(m ethybm ho)benzyDoxy) 0 A-0474 H H H H H 0 H H 3-((4-(m ethybm ho)benzyDoxy) 0 A-0475 H H H H H 0 H H 4-((4-(m ethybm ho)benzyDoxy) 0 A-0476 H H H H H 0 H H 2-((2-(d iethylam ino)benzyDoxy) 0 A-0477 H H H H H 0 H H 3-((2-(d iethylam ino)benzyDoxy) 0 A-0478 H H H H H 0 H H 4-((2-(d iethylam ino)benzyDoxy) 0 A-0479 H H H H H 0 H H 2-((3-(d iethylam ino)benzyDoxy) 0 A-0480 H H H H H 0 H H 3-((3-(d iethylam ino)benzyDoxy) 0 A-0481 H H H H H 0 H H 4-((3-(d iethylam ino)benzyDoxy) 0 A-0482 H H H H H 0 H H 2-((4-(d iethylam ino)benzyDoxy) 0 A-0483 H H H H H 0 H H 3-((4-(d iethylam ino)benzyDoxy) 0 A-0484 H H H H H 0 H H 4-((4-(d iethylam ino)benzyDoxy) 0 A-0485 H H H H H 0 H H 2-((2-cyanobenzyDoxy) 0 A-0486 H H H H H 0 H H 3-((2-cyanobenzyDoxy) 0 A-0487 H H H H H 0 H H 4-((2-cyanobenzyDoxy) 0 A-0488 H H H H H 0 H H 2-((3-cyanobenzyDoxy) 0 A-0489 H H H H H 0 H H 3-((3-cyanobenzyDoxy) 0 A-0490 H H H H H 0 H H 4-((3-cyanobenzyDoxy) 0 A-0491 H H H H H 0 H H 2-((4-cyanobenzyDoxy) 0 A-0492 H H H H H 0 H H 3-((4-cyanobenzyDoxy) 0 A-0493 H H H H H 0 H H 4-((4-cyanobenzyDoxy) 0 A-0494 H H H H H 0 H H 2-((2-nitrobenzyDoxy) 0 A-0495 H H H H H 0 H H 3-((2-nitrobenzyDoxy) 0 A-0496 H H H H H 0 H H 4-((2-n itrobenzy Doxy) 0 A-0497 H H H H H 0 H H 2-((3-nitrobenzyDoxy) 0 A-0498 H H H H H 0 H H 3-((3-nitrobenzyDoxy) 0 A-0499 H H H H H 0 H H 4-((3-nitrobenzyDoxy) 0 A-0500 H H H H H 0 H H 2-((4-nitrobenzyDoxy) 0 A-0501 H H H H H 0 H H 3-((4-nitrobenzyDoxy) 0 A-0502 H H H H H 0 H H 4-((4-nitrobenzyDoxy) 0 A-0503 H H H H H 0 H H 2-NH 2 0 A-0504 H H H H H 0 H H 3-NH 2 0 A-0505 H H H H H 0 H H 4-NH 2 0 A-0506 H H H H H 0 H H 2-NHMe 0 A-0507 H H H H H 0 H H 3-NHMe 0 A-0508 H H FfH H 0 H H 4-NHMe 0
[0135]
[Table 10]
com pound RI R2 R R R A R R' (R)m P A-0509 H H H H H 0 H H 2-NHEt 0 A-0510 H H H H H 0 H H 3-NHEt 0 A-0511 H H H H H 0 H H 4-NHEt 0 A-0512 H H H H H 0 H H 2-N (Me) 2 0 A-0513 H H H H H 0 H H 3-N (Me) 2 0 A-0514 H H H H H 0 H H 4-N(Me) 2 0 A-0515 H H H H H 0 H H 2-N (Et) 2 0 A-0516 H H H H H 0 H H 3-N (Et) 2 0 A-0517 H H H H H 0 H H 4-N(Et) 2 0 A-0518 H H H H H 0 H H 2-CHO 0 A-0519 H H H H H 0 H H 3-CHO 0 A-0520 H H H H H 0 H H 4-CHO 0 A-0521 H H H H H 0 H H 2-C(=0)0H 0 A-0522 H H H H H 0 H H 3-C(=0)0H 0 A-0523 H H H H H 0 H H 4-C(=0)0H 0 A-0524 H H H H H 0 H H 2-(1,3-dioxolan-2-yD 0 A-0525 H H H H H 0 H H 3-(1,3-dioxolan-2-yD 0 A-0526 H H H H H 0 H H 4-(1,3-dioxolan-2-yD 0 A-0527 H H H H H 0 H H 2-(1,3-dioxan-2-yD 0 A-0528 H H H H H 0 H H 3-(1,3-dioxan-2-yD 0 A-0529 H H H H H 0 H H 4-(1,3-dioxan-2-yD 0 A-0530 H H H H H 0 H H 2-(1H-in idazol-2-yD 0 A-0531 H H H H H 0 H H 3-(1H-in idazol-2-yD 0 A-0532 H H H H H 0 H H 4-(1H-in idazol-2-yD 0 A-0533 H H H H H 0 H H 2-(thiazol-2-yl) 0 A-0534 H H H H H 0 H H 3-(thiazol-2-yl) 0 A-0535 H H H H H 0 H H 4-(thiazol-2-yl) 0 A-0536 H H H H H 0 H H 2-(oxazol-2-yD 0 A-0537 H H H H H 0 H H 3-(oxazol-2-yD 0 A-0538 H H H H H 0 H H 4-(oxazol-2-y) 0 A-0539 H H H H H 0 H H 2-CH=N0H 0 A-0540 H H H H H 0 H H 3-CH=N0H 0 A-0541 H H H H H 0 H H 4-CH=N0H 0 A-0542 H H H H H 0 H H 2-CH=NOMe 0 A-0543 H H H H H 0 H H 3-CH=NOMe 0 A-0544 H H H H H 0 H H 4-4H=N0Me 0 A-0545 H H H H H 0 H H 2-(4,5-dihydro-3-soxazolyD 0 A-0546 H H H H H 0 H H 3-(4,5-dihydro-3-soxazolyD 0 A-0547 H H H H H 0 H H 4-(4,5-dihydro-3-soxazolyD 0 A-0548 H H H H H 0 H H 2-CN 0 A-0549 H H H H H 0 H H 3-CN 0 A-0550 H H H H H 0 H H 4-CN 0 A-0551 H H H H H 0 H H 2-N0 2 0 A-0552 H H H H H 0 H H 3-N0 2 0 A-0553 H H H H H 0 H H 4-N0 2 0 A-0554 H H H H H 0 H H 2,342 0 A-0555 H H H H H 0 H H 2,4+2 0 A-0556 H H H H H 0 H H 2,5-F2 0 A-0557 H H H H H 0 H H 2,6-F2 0 A-0558 H H H H H 0 H H 3,4- 2 0 A-0559 H H H H H 0 H H 3,5-F2 0 A-0560 H H H H H 0 H H 2-F,3-CI 0 A-0561 H H H H H 0 H H 2-F,4-CI 0 A-0562 H H H H H 0 H H 2-F,5-CI 0 A-0563 H H H H H 0 H H 2-F,6-CI 0 A-0564 H H H H H 0 H H 3-F,2-CI 0 A-0565 FH H H H 0 H H 3-F,4-CI 0
[0136]
[Table 11]
com pound RI R2 R R R A R R' (R)m P A-0566 H H 0 H H H H H 3-F,5-CI 0 A-0567 H H 0 H H H H H 3-F,6-CI 0 A-0568 H H H H H 0 H H 4-F,2-CI I A-0569 H H H H H 0 H H 4-F,3-CI 0 A-0570 H H 0 H H H H H 2-F,3-Me 0 A-0571 H H H H H 0 H H 2-F,4--M e 0 A-0572 H H 0 H H H H H 2-F,5-Me 0 A-0573 H H 0 H H H H H 2-F,6-Me 0 A-0574 H H H H H 0 H H 3-F,2-Me 0 A-0575 H H H H H 0 H H 3-F,4--M e 0 A-0576 H H H H H 0 H H 3-F,5-Me 0 A-057 7 H H 0 H H H H H 3-F,6-Me 0 A-0578 H H 0 H H H H H 4-F,2-Me 0 A-0579 H H 0 H H H H H 4-F,3-Me 0 A-0580 H H 0 H H H H H 2-F,3-CF 0 A-0581 H H H H H 0 H H 2-F,4-F, 0 A-0582 H H H H H 0 H H 2+5-O-G 3 0 A-0583 H H H H H 0 H H 2-F,6-CF3 0 A-0584 H H H H H 0 H H 3-F,2-F 3 0 A-0585 H H H H H 0 H H 3-F,4-CF3 0 A-0586 H H H H H 0 H H 3-F,5-CF3 0 A-0587 H H H H H 0 H H 3-F,6-CF3 0 A-0588 H H H H H 0 H H 4-F,2-CF 0 A-0589 H H H H H 0 H H 4-F,3-CF3 0 A-0590 H H H H H 0 H H 2-F,3-0Me 0 A-0591 H H H H H 0 H H 2-F,4-0Me 0 A-0592 H H H H H 0 H H 2-F,5-0Me 0 A-0593 H H H H H 0 H H 2-F,6-0Me 0 A-0594 H H H H H 0 H H 3-F,2-0Me 0 A-0595 H H H H H 0 H H 3-F,4-0Me 0 A-0596 H H H H H 0 H H 3-F,5-0Me 0 A-0597 H H H H H 0 H H 3-F,6-0Me 0 A-0598 H H H H H 0 H H 4-F,2-0Me 0 A-0599 H H H H H 0 H H 4-F,3-0Me 0 A-0600 H H H H H 0 H H 2,3-C 0 A-0601 H H H H H 0 H H 2,4-0 0 A-0602 H H H H H 0 H H 2,5-O 0 A-0603 H H H H H 0 H H 2,6-C 0 A-0604 H H H H H 0 H H 3,4-C 0 A-0605 H H H H H 0 H H 3,b-C 0 A-0606 H H H H H 0 H H 2-CI,3-Me 0 A-0607 H H H H H 0 H H 2-CI,4-Me 0 A-0608 H H H H H 0 H H 2-CI,5-Me 0 A-0609 H H H H H 0 H H 2-CI,6-Me 0 A-0610 H H H H H 0 H H 3-CI,2-Me 0 A-0611 H H H H H 0 H H 3-CI,4-Me 0 A-0612 H H H H H 0 H H 3-CI,5-Me 0 A-0613 H H H H H 0 H H 3-CI,6-Me 0 A-0614 H H H H H 0 H H 4-CI,2-Me 0 A-0615 H H H H H 0 H H 4-CI,3-Me 0 A-0616 H H H H H 0 H H 2-C1,3-CF 0 A-0617 H H H H H 0 H H 2-CI,4-F 3 0 A-0618 H H H H H 0 H H 2-C1,5-F 3 0 A-0619 H H H H H 0 H H 2-C 1,6-CF 0 A-0620 H H H H H 0 H H 3-C 1,2-CF 0 A-0621 H IH H H H 0 H H 3-C I,4-G 0 A-0622 HfH Hf H Hi0 H H 3-C 1,5-CF 0
[0137]
[Table 12]
com pound RI R2 R R R A R R' (R)m P A -0623 H H H H H 0 H H 3-C 1,6-CF, 0 A -0624 H H H H H 0 H H 4-C 1,2-CF, 0 A -0625 H H H H H 0 H H 4-C 1,3-CF, 0 A-0626 H H H H H 0 H H 2-C1,3-0Me 0 A-0627 H H H H H 0 H H 2-CI,4-0Me 0 A-0628 H H H H H 0 H H 2-C1,5-0Me 0 A-0629 H H H H H 0 H H 2-C1,6-0Me 0 A-0630 H H H H H 0 H H 3-C1,2-0Me 0 A-0631 H H H H H 0 H H 3-CI,4-0Me 0 A-0632 H H H H H 0 H H 3-C1,5-0Me 0 A-0633 H H H H H 0 H H 3-C1,6-0Me 0 A-0634 H H H H H 0 H H 4-C1,2-0Me 0 A-0635 H H H H H 0 H H 4-C1,3-0Me 0 A-0636 H H H H H 0 H H 2,3-Me 2 0 A-0637 H H H H H 0 H H 2,4-Me2 0 A-0638 H H H H H 0 H H 2,b-Me 2 0 A-0639 H H H H H 0 H H 2,6-Me2 0 A-0640 H H H H H 0 H H 3,4-Me 2 0 A-0641 H H H H H 0 H H 3,5-Me2 0 A-0642 H H H H H 0 H H 2-Me,3-CF3 0 A-0643 H H H H H 0 H H 2-Me,4-CFA 0 A-0644 H H H H H 0 H H 2-Me,5-CF3 0 A-0645 H H H H H 0 H H 2-Me,6-CF3 0 A-0646 H H H H H 0 H H 3-Me,2-CF3 0 A-0647 H H H H H 0 H H 3-Me,4-F 3 0 A-0648 H H H H H 0 H H 3-Me,5-CF 3 0 A-0649 H H H H H 0 H H 3-Me,6-F 3 0 A-0650 H H H H H 0 H H 4-Me,2-CF3 0 A-0651 H H H H H 0 H H 4-Me,3-CF3 0 A-0652 H H H H H 0 H H 2-Me,3-0Me 0 A-0653 H H H H H 0 H H 2-Me,4-0Me 0 A-0654 H H H H H 0 H H 2-Me,5-0Me 0 A-0655 H H H H H 0 H H 2-Me,6-0Me 0 A-0656 H H H H H 0 H H 3-Me,2-0Me 0 A-0657 H H H H H 0 H H 3-Me,4-0Me 0 A-0658 H H H H H 0 H H 3-Me,5-0Me 0 A-0659 H H H H H 0 H H 3-Me,6-0Me 0 A-0660 H H H H H 0 H H 4-Me,2-0Me 0 A-0661 H H H H H 0 H H 4-Me,3-0Me 0 A-0662 H H H H H 0 H H 2,3-0Me 2 0 A-0663 H H H H H 0 H H 2,4-0Me 2 0 A-0664 H H H H H 0 H H 2,5-0Me 2 0 A-0665 H H H H H 0 H H 2,6-0Me 2 0 A-0666 H H H H H 0 H H 3,4-0Me 2 0 A-0667 H H H H H 0 H H 3,5-0Me 2 0 A-0668 H H H H H 0 H H 2-0Me,3-G 3 0 A-0669 H H H H H 0 H H 2-0Me,4-CF3 0 A-0670 H H H H H 0 H H 2-0Me,5-CF3 0 A-0671 H H H H H 0 H H 2-0Me,6-CF3 0 A-0672 H H H H H 0 H H 3-0Me,2-F3 0 A-0673 H H H H H 0 H H 3-0Me,4-CF3 0 A-0674 H H H H H 0 H H 3-0Me,5-G 3 0 A-0675 H H H H H 0 H H 3-0Me,6-F3 0 A-0676 H H H H H 0 H H 4-0Me,2-CF3 0 A-0677 H H H H H 0 H H 4-0Me,3-CF3 0 A-0678 H H H H H 0 H H 2-CHF 2,3-F 0 A-0679 H H H H 0 H H 2-CHF 2,4-F 0
[0138]
[Table 13]
com pound RI R2 R R R A R R' (R)m P A-0680 i H H H H H 0 H H 2-C2HF,5-F 0 A-0681 H H H H H 0 H H 2-CHF 2,6-F 0 A-0682 H H H H H 0 H H 2-CHF 2,3-Me 0 A-0683 H H H H H 0 H H 2-CHF 2,4-Me 0 A-0684 H H H H H 0 H H 2-CHF 2,5-Me 0 A-0685 H H H H H 0 H H 2-CHF 2,6-Me 0 A-0686 H H H H H 0 H H 2-cycbpropyl,3-F 0 A-0687 H H H H H 0 H H 2-cycbpropyl,4-F 0 A-0688 H H H H H 0 H H 2-cycbpropyl,5-F 0 A-0689 H H H H H 0 H H 2-cycbpropyl,6-F 0 A-0690 H H H H H 0 H H 2-cycbpropyl,3-Me 0 A-0691 H H H H H 0 H H 2-cycbpropyl,4-M e 0 A-0692 H H H H H 0 H H 2-cycbopropyl,5-Me 0 A-0693 H H H H H 0 H H 2-cycbopropyl,6-Me 0 A-0694 H H H H H 0 H H 2-ethenyl,3-F 0 A-0695 H H H H H 0 H H 2-ethenyl,4-F 0 A-0696 H H H H H 0 H H 2-ethenyl,5-F 0 A-0697 H H H H H 0 H H 2-ethenyl,6-F 0 A-0698 H H H H H 0 H H 2-ethenyl,3-M e 0 A-0699 H H H H H 0 H H 2-ethenyl,4-M e 0 A-0700 H H H H H 0 H H 2-ethenyl1,5-Me 0 A-0701 H H H H H 0 H H 2-ethenyl,6-M e 0 A-0702 H H H H H 0 H H 2-0Et,3-F 0 A-0703 H H H H H 0 H H 2-0Et,4-F 0 A-0704 H H H H H 0 H H 2-0Et,5-F 0 A-0705 H H H H H 0 H H 2-0Et,6-F 0 A-0706 H H H H H 0 H H 2-0Et3-CI 0 A-0707 H H H H H 0 H H 2-0Et4-CI 0 A-0708 H H H H H 0 H H 2-0Et5-CI 0 A-0709 H H H H H 0 H H 2-0Et6-CI 0 A-0710 H H H H H 0 H H 2-OEt,3-Me 0 A-0711 H H H H H 0 H H 2-0Et,4-Me 0 A-0712 H H H H H 0 H H 2-0Et,5-M e 0 A-0713 H H H H H 0 H H 2-0Et,6-Me 0 A-0714 H H H H H 0 H H 2-0Pr,3-F 0 A-0715 H H H H H 0 H H 2-0Pr4-F 0 A-0716 H H H H H 0 H H 2-0Pr,5-F 0 A-0717 H H H H H 0 H H 2-0Pr,6-F 0 A-0718 H H H H H 0 H H 2-OPr,3-Me 0 A-0719 H H H H H 0 H H 2-OPr,4-M e 0 A-0720 H H H H H 0 H H 2-0Pr,5-Me 0 A-0721 H H H H H 0 H H 2-0Pr,6-Me 0 A-0722 H H H H H 0 H H 2-0(/-Pr),3-F 0 A-0723 H H H H H 0 H H 2-0(/-Pr),4-F 0 A-0724 H H H H H 0 H H 2-0(/-Pr),5-F 0 A-0725 H H H H H 0 H H 2-0(/-Pr),6-F 0 A-0726 H H H H H 0 H H 2-0(/-Pr),3-Me 0 A-0727 H H H H H 0 H H 2-0(/-Pr),4-M e 0 A-0728 H H H H H 0 H H 2-0(/-Pr),5-Me 0 A-0729 H H H H H 0 H H 2-0(/-Pr),6-Me 0 A-0730 H H H H H 0 H H 2-0CF,,3-F 0 A-0731 H H H H H 0 H H 2-0CF,4-F 0 A-0732 H H H H H 0 H H 2-00CF,b-F 0 A-0733 H H H H H 0 H H 2-0CF3 ,6-F 0 A-0734 IH H H H H 0 H H 2-0CF 3,3-Me 0 A-0735 H H H H H 0 H H 2-0CF 3A,4-Me 0 A-0736 H H H H 0 H H 2-0CF 3,5-Me 0
[0139]
[Table 14]
com pound RI R2 R R R A R R' (R)m P A-0737 i H H H H H 0 H H 2-0CF3,6-Me 0 A-0738 H H H H H 0 H H 2-0CHF 2,3-F 0 A-0739 H H H H H 0 H H 2-0CHF 2,4-F 0 A-0740 H H H H H 0 H H 2-0CHIF 2,b-|- 0 A-0741 H H H H H 0 H H 2-0CHF 2,6-F 0 A-0742 H H H H H 0 H H 2-0CHF 2 ,3-Me 0 A-0743 H H H H H 0 H H 2-0CHF 2 ,4-M e 0 A-0744 H H H H H 0 H H 2-0CHF 2 ,b-Me 0 A-0745 H H H H H 0 H H 2-0CHF 2 ,6-Me 0 A-0746 H H H H H 0 H H 2-(cycbpropybxy),3-F 0 A-0747 H H H H H 0 H H 2-(cycbpropybxy),4-F 0 A-0748 H H H H H 0 H H 2-(cycbpropybxy),5-F 0 A-0749 H H H H H 0 H H 2-(cycbpropybxy),6-F 0 A-0750 H H H H H 0 H H 2-(cyclopropyoxy),3-Me 0 A-0751 H H H H H 0 H H 2-(cyclopropyoxy),4-Me 0 A-0752 H H H H H 0 H H 2-(cyclopropybxy),5-M e 0 A-0753 H H H H H 0 H H 2-(cyclopropybxy),6-M e 0 A-0754 H H H H H 0 H H 2-(oxiran-2-yD,3-F 0 A-0755 H H H H H 0 H H 2-(oxiran-2-yD,4-F 0 A-0756 H H H H H 0 H H 2-(oxiran-2-yD,5-F 0 A-0757 H H H H H 0 H H 2-(oxiran-2-yD,6-F 0 A-0758 H H H H H 0 H H 2-(oxiran-2-yD,3-Me 0 A-0759 H H H H H 0 H H 2-(oxiran-2-yD,4-Me 0 A-0760 H H H H H 0 H H 2-(oxiran-2-yD,5-Me 0 A-0761 H H H H H 0 H H 2-(oxiran-2-yD,6-Me 0 A-0762 H H H H H 0 H H 2-(oxiran-2-yhiethyD,3-F 0 A-0763 H H H H H 0 H H 2-(oxiran-2-y hethyD,4-F 0 A-0764 H H H H H 0 H H 2-(oxiran-2-yhiethyD,5-F 0 A-0765 H H H H H 0 H H 2-(oxiran-2-yhiethyD,6-F 0 A-0766 H H H H H 0 H H 2-(oxiran-2-y hethy),3-Me 0 A-0767 H H H H H 0 H H 2-(oxiran-2-y hethy),4-Me 0 A-0768 H H H H H 0 H H 2-(oxiran-2-y hethy),5-Me 0 A-0769 H H H H H 0 H H 2-(oxiran-2-yhiethyl),6-M e 0 A-0770 H H H H H 0 H H 2-SMe,3-F 0 A-0771 H H H H H 0 H H 2-SMe,4-F 0 A-0772 H H H H H 0 H H 2-SMe,5-F 0 A-0773 H H H H H 0 H H 2-SMe,6-F 0 A-0774 H H H H H 0 H H 2-SMe,3-Me 0 A-0775 H H H H H 0 H H 2-SMe,4-Me 0 A-0776 H H H H H 0 H H 2-SMe,5-M e 0 A-0777 H H H H H 0 H H 2-SMe,6-Me 0 A-0778 H H H H H 0 H H 2-SEt,3-F 0 A-0779 H H H H H 0 H H 2-SEt,4-F 0 A-0780 H H H H H 0 H H 2-SEt,5-F 0 A-0781 H H H H H 0 H H 2-SEt,6-F 0 A-0782 H H H H H 0 H H 2-SEt,3-Me 0 A-0783 H H H H H 0 H H 2-SEt,4-Me 0 A-0784 H H H H H 0 H H 2-SEt,5-Me 0 A-0785 H H H H H 0 H H 2-SEt,6-Me 0 A-C786 H H H H H 0 H H 2-S(=0)Me,3-F 0 A-0787 H H H H H 0 H H 2-S(=0)Me,4-F 0 A-0788 H H H H H 0 H H 2-S(=0)Me,5-F 0 A-0789 H H H H H 0 H H 2-S(=0)Me,6-F 0 A-0790 H H H H H 0 H H 3-S(=0)Me,2-F 0 A-0791 H H H H H 0 H H 3-S(=0)Me,4-F 0 A-0792 H H H H H 0 H H 3-S(=0)Me,5-F 0 A-0793 H H H H H0 H H 3-S(=0)Me,6-F 0
[0140]
[Table 15]
com pound RI R2 R R R A R R' (R)m P A-0794 H H H H H 0 H H 2-S(=0)Me,3-M e 0 A-0795 H H H H H 0 H H 2-S(=0)Me,4-Me 0 A-0796 H H H H H 0 H H 2-S(=0)Me,5-Me A-0797 H H H H H 0 H H 2-S(=0)Me,6-M e 0 A-0798 H H H H H 0 H H 3-S(=0)Me,2-Me A-0799 H H H H H 0 H H 3-S(=0)Me,4-M e 0 A-0800 H H H H H 0 H H 3-S(=0)Me,5-M e 0 A-0801 H H H H H 0 H H 3-S(=0)Me,6-M e 0 A-0802 H H H H H 0 H H 2-S(=0) 2Me,3-F 0 A-0803 H H H H H 0 H H 2-S(=0) 2Me,4-F 0 A-0804 H H H H H 0 H H 2-S(=0) 2Me,b-F 0 A-080 5 H H H H H 0 H H 2-S(=0) 2Me,6-F 0 A-0806 H H H H H 0 H H 2-S(=0) 2 Me,3-M e 0 A-0807 H H H H H 0 H H 2-S(=0) 2 Me,4-M e 0 A-0808 H H H H H 0 H H 2-S(=0) 2 Me,5-M e 0 A-0809 H H H H H 0 H H 2-S(=0) 2 Me,6-Me 0 A-0810 H H H H H 0 H H 2-S CF,3-F 0 A-0811 H H H H H 0 H H 2-SCF 3 ,4-F 0 A-0812 H H H H H 0 H H 2-SC F,b-F 0 A-0813 H H H H H 0 H H 2-SCF 3 ,6-F 0 A-0814 H H H H H 0 H H 2-SCF 3 ,3-M e 0 A-0815 H H H H H 0 H H 2-SCF 3 ,4-M e 0 A-0816 H H H H H 0 H H 2-SCF 3 ,5-M e 0 A-0817 H H H H H 0 H H 2-SCF 3 ,6-M e 0 A-0818 H H H H H 0 H H 2-S (=O)F 3 ,3-F 0 A-0819 H H H H H 0 H H 2-S (=O)F 3 ,4-F 0 A-0820 H H H H H 0 H H 2-S (=O)F 3 ,b-F 0 A-0821 H H H H H 0 H H 2-S (=0)F 3 ,6-F 0 A-0822 H H H H H 0 H H 2-S(=O)CF 3 ,3-M e 0 A-0823 H H H H H 0 H H 2-S(=O)CF3 ,4-M e 0 A-0824 H H H H H 0 H H 2-S(=O)CF 3 ,5-M e 0 A-0825 H H H H H 0 H H 2-S(=O)CF 3 ,6-M e 0 A-0826 H H H H H 0 H H 2-S(=0) 2CF3 ,3-F 0 A-0827 H H H H H 0 H H 2-S(=0) 20F 3 ,4-F 0 A-0828 H H H H H 0 H H 2-S(=0) 2CF,5-F 0 A-0829 H H H H H 0 H H 2-S(=0) 20F 3 ,6-F 0 A-0830 H H H H H 0 H H 2-S(=0) 2CF 3 ,3-M e 0 A-0831 H H H H H 0 H H 2-S(=0) 2 CF3 ,4-M e 0 A-0832 H H H H H 0 H H 2-S(=0) 2 CF 3 ,5-Me 0 A-0833 H H H H H 0 H H 2-S(=0) 2 CF 3 ,6-M e 0 A-0834 H H H H H 0 H H 2-(cycobpropylthb),3-F 0 A-0835 H H H H H 0 H H 2-(cycobpropylthb),4-F 0 A-0836 H H H H H 0 H H 2-(cycobpropylthb),5-F 0 A-0837 H H H H H 0 H H 2-(cycobpropylthb),6-F 0 A-0838 H H H H H 0 H H 2-(cycbpropyth b),3-M e 0 A-0839 H H H H H 0 H H 2-(cycbpropylthb),4-M e 0 A-0840 H H H H H 0 H H 2-(cycbpropylthb),5-Me 0 A-0841 H H H H H 0 H H 2-(cycbpropylthb),6-Me 0 A-0842 H H H H H 0 H H 2-C(=0)Me,3-F 0 A-0843 H H H H H 0 H H 2-C(=0)Me,4-F 0 A-0844 H H H H H 0 H H 2-C(=0)Me,5-F 0 A-0845 H H H H H 0 H H 2-C(=0)Me,6-F 0 A-0846 H H H H H 0 H H 2-C(=0)Me,3-M e 0 A-0847 H H H H H 0 H H 2-C(=0)Me,4-M e 0 A-0848 H H H H H 0 H H 2-C(=0)Me,5-M e 0 A-0849 H H HIH H 0 H H 2-C(=0)Me,6 -M e 0 A-0850 H FfH H H0 H H 3-C(=0)Me,2-F 0
[0141]
[Table 16]
com pound R' R2 R R A R R' (R)m p A-08b1 H H H H 0 H H 3-C(=0)Me,4-F 0 A-0852 H H H H 0 H H 3-C(=U)Me,b-F 0 A-0853 H H H H 0 H H 3-C(=0)Me,6-F W A-0854 H H H H i 0 H H 3-C(=U)Me,2-M e 0 A-08bb H H H H 0 H H 3-C(=0)Me,4-Me A-0856 H H H H 0 H H 3-C(=0)Me,b-M e 0 A-08b H H H H 0 H H 3-C(=0)Me,6--M e 0 A-08b8 H H H H 0 H H 2-C(=O)OMe,3-F 0 A-0859 H H H H 0 H H 2-C(=O)OMe,4-F 0 A-0860 H H H H H 0 H H 2-C(=0)OMe,b-F 0 A-0861 H H H H i 0 H H 2-C(=U)OMe,6-F 0 A-0862 H H H H 0 H H 2-C(=0)0Me,3-MA e 0 A-0863 H H H H 0 H H 2-C(=0)UMe,4-M e 0 A-0864 H H H H 0 H H 2-C(=0)0Me,b-MAe 0 A-0865 H H H H 0 H H 2-C(=0)0Me,6-MA e 0 A-0866 H H H H Hi0 H H 2-C(=0)UEt,3-F 0 A-086/ H H H H f0 H H 2-C(=0)UEt,4-F 0 A-0868 H H H H 0 H H 2-C(=0)0Etb-F 0 A-0869 H H H H Hi0 H H 2-C(=0)UEt,6-F 0 A-080 H H H H 0 H H 2-C(=0)0Et3-M e 0 A-08/1 H H H H 0 H H 2-C(=0)UEt4-Me 0 A-08/2 H H H H 0 H H 2-C(=0)UEtb-M e 0 A-08/3 H H H H 0 H H 2-C(=0)0Et6-M e 0 A-08/4 H H H H Hi0 H H 2-C(=0)NH 2,3-4 0 A-08b H H H H HD0 H H 2-C(=U)NH 2,4-F 0 A-08/6 H H H H f0 H H 2-C(=U)NH 2,b-H 0 A-08// H H H H f0 H H 2-C(=U)NH2,6- 0 A-08/8 H H H H i 0 H H 2-C(=0)NH 2 ,3-M e 0 A-08/9 H H H H 0 H H 2-C(=0)NH 2 ,4-M e 0 A-0880 H H H H 0 H H 2-C(=0)NH 2 ,b-M e 0 A-0881 H H H H 0 H H 2-C(=0)NH 2 ,6-M e 0 A-0882 H H H H 0 H H 2-C(=0)NHMe,3-F 0 A-0883 H H H H 0 H H 2-C(=0)NHMe,4-F 0 A-0884 H H H H 0 H H 2-C(=0)NHMe,b-F 0 A-088b H H H H 0 H H 2-C(=0)NHMe,6-F 0 A-0886 H H H H 0 H H 2-C(=0)NHMe,3-M e 0 A-088/ H H H H f0 H H 2-C(=0)NHMe,4-M e 0 A-0888 H H H H 0 H H 2-C(=0)NHMe,b-M e 0 A-0889 H H H H 0 H H 2-C(=0)NHMe,6-M e 0 A-0890 H H H H 0Di H H 2-C(=0)NMe 2 ,3-F 0 A-0891 H H H H 0 H H 2-C(=0)NMe 2 ,4-F 0 A-0892 H H H H 0 H H 2-C(=0)NMe 2 ,b-F 0 A-0893 H H H H f0 H H 2-C(=U)NMe 2 ,6- 0 A-0894 H H H H 0 H H 2-C(=U)NMe 2,3-M e 0 A-0895 H H H H 0 H H 2-C(=U)NMe 2,4-M e 0 A-0896 H H H H f0 H H 2-C(=U)NMe 2,b-M e 0 A-089/ H H H H 0 H H 2-C(=0)NMe 2,6-M e 0 A-0898 H H H H 0 H H 2-CH 2UH,3-F 0 A-0899 H H H H 0 H H 2-CH 2UH,4-F 0 A-0900 H H H H f0 H H 2-CH 2UNb-H 0 A-0901 H H H H 0 H H 2-CH 2UH,6-F 0 A-0902 H H H H f0 H H 2-CH 2UN,3-M e A-0903 H H H H f0 H H 2-CH 2UH,4-Me 0 A-0904 H H H H 0 H H 2-CH 2UH,b-M e 0 A-0905 H H H H f0 H H 2-CH 2UH,6-M e 0 A-0906 H HF FH 0 H H 2-GH 20H 3,3-F 0 A-090/ H fF HF i H H 2-CH 20H 3 ,4-F 0
[0142]
[Table 17]
com pound R' R2 R R A R R' (R)m p A-0908 H H H H 0 H H 2-0H 20H 3 ,b-F 0 A-0909 H H H H f0 H H 2-0H 20H 3 ,6-F F A-0910 H H H H 0 H H 2-0H 20H 3 ,3-M e 0 A-0911 H H H H if 0 H H 2-H 20H 3 ,4-M e A-0912 H H H H 0 H H 2-CH 20CH 3 ,b- e A-0913 H H H H 0 H H 2-0H 20H 3 ,6-MA e 0 A-0914 H H H H 0 H H 2-0H 20H 2 CH 3 ,3-F 0 A-0915 H H H H 0 H H 2-0H 20H 2 CH 3,4-F 0 A-0916 H H H H H 0 H H 2-0H 20H 2 CH 3 ,b-F 0 A-091/ i H HH H 0 H H 2-U2H0H2CH3,6- 0 A-0918 H H H H if 0 H H 2-H 20H 2CH 3 ,3-Me 0 A-0919 H H H H 0 E H H 2-H 20H 2CH 3,4-Me 0 A-0920 H H H H f0 H H 2-GH 20H 2CH 3 ,b-M e 0 A-0921 H H H H 0 H H 2-0H 20H 2CH 3 ,6-M e 0 A-0922 H H H H 0 H H 2-00= )GH 3 ,3-4 0 A-0923 H H H H H0 H H 2-0G0(= )GH 3 ,4- 0 A-0924 H H H H HD0 H H 2-0C= U)GH 3,b-H 0 A-0925 H H H H 0 H H 2-0C0(= )CH 3,6-F 0 A-0926 H H H H f0 H H 2-0C(=U)CH 3,3-Me 0 A-0927 H H H H 0 H H 2-0C (=0 )CH 3 ,4-Mve 0 A-0928 H H H H f0 H H 2-0 C= U)TH 3 ,b- e 0 A-0929 H H H H f0 H H 2-0C (=0 )CH 3 ,6-M e 0 A-0930 H H H H 0 H H 2-OS (=0 ) 2 H 3 ,3-4 0 A-0931 H H H H Hi0 H H 2-OS (=0 ) 2 H 3 ,4-F 0 A-0932 H H H H HD0 H H 2-OS =OUH3,b-H )2 0 A-0933 H H H H H 0 H H 2-OS =OUH)2 3 ,6- 0 A-0934 H H H H f0 H H 2-OS =O ) 2 CH 3,3-M e 0 A-0935 H H H H i 0 H H 2-OS(= 0) 2 H3,4-M e 0 A-0936 H H H H 0 H H 2-0S(= 0) 2 H 3,b-M e 0 A-0937 H H H H 0 H H 2-S(= 0) 2 GH 3,6-M e 0 A-0938 H H H H 0 H H 2-CH 2 SCH 3 ,3-4 0 A-0939 H H H H 0 H H 2-CH 2 SCH 3,4-F 0 A-0940 H H H H H 0 H H 2-CH 2 SCH 3 ,b-4 0 A-0941 H H H 0H E H H 2-CH 2SCH 3 ,6- 0 A-0942 H H H H 0 H H 2-CH 2SCH 3,3-M e 0 A-0943 H H H H 0 H H 2-CH 2SCH 3,4-M e 0 A-0944 H H H H f0 H H 2-CH 2SCH 3,b-M e 0 A-0945 H H H H 0 H H 2-CH 2SCH 3,6-M e 0 A-0946 H H H H 0 H H 2-CH 2SCF 3 ,3-F 0 A-0947 H H H H H 0 H H 2-CH 2SCF 3 ,4-F 0 A-0948 H H H H 0 H H 2-CH 2SCF 3 ,b-F 0 A-0949 H H H H 0 H H 2-CH 2SCF 3 ,6-F 0 A-0950 H H H H f0 H H 2-CH 2SCF 3 ,3-M e 0 A-0951 H H H H 0 H H 2-CH 2SCF 3 ,4-M e 0 A-0952 H H H H 0 H H 2-CH 2SCF 3 ,b-M e 0 A-0953 H H H H f0 H H 2-CH 2SCF 3 ,6-M e 0 A-0954 H H H H 0 H H 2-(benzy bxy),3-F 0 A-0955 H H H H 0 H H 2-(benzy bxy),4-F 0 A-0956 H H H H 0 H H 2-(benzy bxy),b-F 0 A-0957 H H H H E 0 H H 2-(benzybxy),6-F 0 A-0958 H H H H 0 H H 2-(benzyloxy),3-M e 0 A-0959 H H H H f0 H H 2-(benzyloxy),4-M e 0 A-0960 H H H H f0 H H 2-(benzyloxy),b-M e 0 A-0961 H H H H E 0 H H 2-(benzyloxy),6-M e 0 A-0962 H H H H f0 H H 2-NH 2,3- 0 A-0963 H H H H HD0 H H 2-NH 2,4- 0 A-0964 H H Hi H 0 H H 2-NH 2,b-4 0
[0143]
[Table 18]
com pound RI R2 R R R A R R' (R)m P A-0965 i H H H H H 0 H H 2-N2H,6-F 0 A-0966 H H H H H 0 H H 2-NH 2,3-MAe 0 A-0967 H H H H H 0 H H 2-NH 2,4-M e 0 A-0968 H H H H H 0 H H 2-NH 2,5-Me 0 A-0969 H H H H H 0 H H 2-NH 2,6-Me 0 A-0970 H H H H H 0 H H 2-NHMe,3-F 0 A-0971 H H H H H 0 H H 2-NHMe,4-F 0 A-0972 H H H H H 0 H H 2-NHMe,5-F 0 A-0973 H H H H H 0 H H 2-NHMe,6-F 0 A-0974 H H H H H 0 H H 2-NHMe,3-Me 0 A-0975 H H H H H 0 H H 2-NHMe,4-Me 0 A-0976 H H H H H 0 H H 2-NHMe,5-Me 0 A-0977 H H H H H 0 H H 2-NHMe,6-Me 0 A-0978 H H H H H 0 H H 2-NHEt,3-F 0 A-0979 H H H H H 0 H H 2-NHEt,4-F 0 A-0980 H H H H H 0 H H 2-NHEt,5-F 0 A-0981 H H H H H 0 H H 2-NHEt,6-F 0 A-0982 H H H H H 0 H H 2-NHEt,3-M e 0 A-0983 H H H H H 0 H H 2-NHEt,4-Me 0 A-0984 H H H H H 0 H H 2-NHEt,5-M e 0 A-0985 H H H H H 0 H H 2-NHEt,6-M e 0 A-0986 H H H H H 0 H H 2-NMe 2 ,3-F 0 A-0987 H H H H H 0 H H 2-NMe2,4-F 0 A-0988 H H H H H 0 H H 2-NMe 2 ,5-F 0 A-0989 H H H H H 0 H H 2-NMe 2 ,6-F 0 A-0990 H H H H H 0 H H 2-NMe 2 ,3-Me 0 A-0991 H H H H H 0 H H 2-NMe 2 ,4-Me 0 A-0992 H H H H H 0 H H 2-NMe 2 ,5-Me 0 A-0993 H H H H H 0 H H 2-NMe 2 ,6-Me 0 A-0994 H H H H H 0 H H 2-NEt2,3-F 0 A-0995 H H H H H 0 H H 2-NEt2,4-F 0 A-0996 H H H H H 0 H H 2-NEt2,5-F 0 A-0997 H H H H H 0 H H 2-NEt 2,6-F 0 A-0998 H H H H H 0 H H 2-NEt,3-e 0 A-0999 H H H H H 0 H H 2-NEt2,4-Me 0 A-1000 H H H H H 0 H H 2-NEt2,5-Me 0 A-1001 H H H H H 0 H H 2-NEt2,6-Me 0 A-1002 H H H H H 0 H H 2-CHO,3-F 0 A-1003 H H H H H 0 H H 2-CHOA-F 0 A-1004 H H H H H 0 H H 2-CHO,5-F 0 A-1005 H H H H H 0 H H 2-CHO,6-F 0 A-1006 H H H H H 0 H H 2-CHO,3-M e 0 A-1007 H H H H H 0 H H 2-CHO,4-MAe 0 A-1008 H H H H H 0 H H 2-CHO,5-M e 0 A-1009 H H H H H 0 H H 2-CHO,6-M e 0 A-101C0 H H H H H 0 H H 2-C (=0)OH,3-F 0 A-1011 H H H H H 0 H H 2-C (=0)OH,4-F 0 A-101 2 H H H H H 0 H H 2-C (=0)OH,5-F 0 A-101 3 H H H H H 0 H H 2-C (=0)OH,6-F 0 A-101 4 H H H H H 0 H H 2-C(=0)0H,3-M e 0 A-1015 H H H H H 0 H H 2-C(=0)0H,4-M e 0 A-1016 H H H H H 0 H H 2-C(=0)0H, 5-M e 0 A-1017 H H H H H 0 H H 2-C(=0)0H,6-M e 0 A-1018 H H H H H 0 H H 2-(1,3-dioxolan-2-yD,3-F 0 A-1019 H H H H H 0 H H 2-(1,3-dioxolan-2-yD,4-F 0 A-1020 H H H H H 0 H H 2-(1,3-dioxolan-2-yD,5-F 0 A-1021 H Hf H H 0 H H 2-(1,3-dioxolan-2-yl),6-F 0
[0144]
[Table 19]
com pound RI R2 R R R A R R' (R)m P A-1022 i H H H H H0 H H 2-(1,3-dbxolan-2-yD,3-M e 0 A-1023 H H H H H 0 H H 2-(1,3-dbxolan-2-yD,4-Me 0 A-1024 H H H H H 0 H H 2-(1,3-dbxolan-2-yD,5-Me A-1025 H H H H H 0 H H 2-(1,3-dbxolan-2-yD,6-M e 0 A-1026 H H H H H 0 H H 2-0,3-dbxan-2-yD,3-F 0 A-1027 H H H H H 0 H H 2-(1,3-dbxan-2-yD,4-F 0 A-1028 H H H H H 0 H H 2-0,3-dbxan-2-yD,5-F 0 A-1029 H H H H H 0 H H 2-0,3-dbxan-2-yD,6-F 0 A-1030 H H H H H 0 H H 2-(1,3-dioxan-2-yD,3-Me 0 A-1031 H H H H H 0 H H 2-(1,3-dioxan-2-yD,4-Me 0 A-1032 H H H H H 0 H H 2-(1,3-dioxan-2-yD,5-M e 0 A-1033 H H H H H 0 H H 2-(1,3-dioxan-2-yD,6-Me 0 A-1034 H H H H H 0 H H 2-(thiazol--2-yl),3-F 0 A-1035 H H H H H 0 H H 2-(thiazol--2-yD,4-F 0 A-1036 H H H H H 0 H H 2-(thiazol-2-y),5-F 0 A-1037 H H H H H 0 H H 2-(thiazol--2-yl),6-F 0 A-1038 H H H H H 0 H H 2-(thbzol-2-yD,3-M e 0 A-1039 H H H H H 0 H H 2-(thbzol-2-yD,4-Me 0 A-1040 H H H H H 0 H H 2-(thbzol-2-yD,5-M e 0 A-1041 H H H H H 0 H H 2-(thbzol-2-yD,6-Me 0 A-1042 H H H H H 0 H H 2-(oxazol-2-yD,3-F 0 A-1043 H H H H H 0 H H 2-(oxazol-2-yD,4-F 0 A-1044 H H H H H 0 H H 2-(oxazol-2-yD,5-F 0 A-1045 H H H H H 0 H H 2-(oxazol-2-yD,6-F 0 A-1046 H H H H H 0 H H 2-(oxazol-2-yD,3-M e 0 A-1047 H H H H H 0 H H 2-(oxazol-2-yD,4-Me 0 A-1048 H H H H H 0 H H 2-(oxazol-2-yD,5-M e 0 A-1049 H H H H H 0 H H 2-(oxazol-2-yD,6-M e 0 A-1050 H H H H H 0 H H 2-CH= NOH,3-F 0 A-1051 H H H H H 0 H H 2-CH= NOH,4-F 0 A-1052 H H H H H 0 H H 2-CH= NOH,5-F 0 A-1053 H H H H H 0 H H 2-CH= NOH,6-F 0 A-1054 H H H H H 0 H H 2-CH=N0H,3-M e 0 A-1055 H H H H H 0 H H 2-CH=N0H,4-M e 0 A-1056 H H H H H 0 H H 2-CH=N0H,5-Me 0 A-1057 H H H H H 0 H H 2-CH=N0H,6-M e 0 A-1058 H H H H H 0 H H 2-CH= NOM e,3-F 0 A-1059 H H H H H 0 H H 2-CH= NOM e,4-F 0 A-1060 H H H H H 0 H H 2-CH= NOM e,5-F 0 A-1061 H H H H H 0 H H 2-CH= NOM e,6-F 0 A-1062 H H H H H 0 H H 2-CH=N0Me,3-M e 0 A-1063 H H H H H 0 H H 2-CH=N0Me,4-M e 0 A-1064 H H H H H 0 H H 2-CH=N0Me,5-M e 0 A-1065 H H H H H 0 H H 2-CH=N0Me,6-M e 0 A-1066 H H H H H 0 H H 2-CN,3-F 0 A-1067 H H H H H 0 H H 2-CNA-F 0 A-1068 H H H H H 0 H H 2-CN,5-F 0 A-1069 H H H H H 0 H H 2-CN,6-F 0 A-1070 H H H H H 0 H H 2-CN,3-CI 0 A-1071 H H H H H 0 H H 2-CNA-CI 0 A-1072 H H H H H 0 H H 2-CN,5-CI 0 A-1073 H H H H H 0 H H 2-CN,6-CI 0 A-1074 H H H H H 0 H H 2-CN,3-Me 0 A-1075 H H H H H 0 H H 2-CN A-M e 0 A-1076 H H H H H 0 H H 2-CN,5-Me 0 A-1077 H H H H H 0 H H 2-CN,6-Me 0 A-1078 H H H H H0 H H 2-CN,3-U M e 0
[0145]
[Table 20]
com pound RI R2 R R R A R R' (R)m P A-1079 H H H H H 0 H H 2-CN,4-0 M e 0 A-1080 H H H H H 0 H H 2-CN,5-0 M e 0 A-1081 H H H H H 0 H H 2-CN,6-0Me A-1082 H H H H H 0 H H 3-CN,2-F 0 A-1083 H H H H H 0 H H 3-CNA-F 0 A-1084 H H H H H 0 H H 3-CN,5-F 0 A-1085 H H H H H 0 H H 3-CN,6-F 0 A-1086 H H H H H 0 H H 3-CN,2-C I 0 A-1087 H H H H H 0 H H 3-CN A- I 0 A-1088 H H H H H 0 H H 3-CN,5-CI 0 A-1089 H H H H H 0 H H 3-CN,6-C I 0 A-1090 H H H H H 0 H H 3-CN,2-M e 0 A-1091 H H H H H 0 H H 3-CN A- e 0 A-1092 H H H H H 0 H H 3-CN,5-M e 0 A-1093 H H H H H 0 H H 3-CN,6-M e 0 A-1094 H H H H H 0 H H 3-CN,2-0M e 0 A-1095 H H H H H 0 H H 3-CN,4-0 M e 0 A-1096 H H H H H 0 H H 3-CN,5-0 M e 0 A-1097 H H H H H 0 H H 3-CN,6-0 M e 0 A-1098 H H H H H 0 H H 4-CN,2-F 0 A-1099 H H H H H 0 H H 4-CN,3-F 0 A-1100 H H H H H 0 H H 4-CN,2-C I 0 A-1101 H H H H H 0 H H 4-CN,3-C I 0 A-1102 H H H H H 0 H H 4-CN,2-M e 0 A-1103 H H H H H 0 H H 4-CN,3-M e 0 A-1104 H H H H H 0 H H 4-CN,2-0M e 0 A-1105 H H H H H 0 H H 4-CN,3-0M e 0 A-1106 H H H H H 0 H H 2-N0 2 ,3-F 0 A-1107 H H H H H 0 H H 2-N02,4-F 0 A-1108 H H H H H 0 H H 2-N0 2 ,5-F 0 A-1109 H H H H H 0 H H 2-N0 2 ,6-F 0 A-1110 H H H H H 0 H H 2-A0 2,3-M e 0 A-1111 H H H H 0 H H H 2-A02,4-M e 0 A-1112 H H H H 0 H H H 2-N0 2,5-M e 0 A-1113 H H H H 0 H H H 2-N0 2,6-M e 0 A-1114 H H H H 0 H H H 2-M e,3,4- 2 0 A-1115 H H H H 0 H H H 2-M e,3,b- 2 0 A-1116 H H H H 0 H H H 2-M e,3,6-F2 0 A-1117 H H H H 0 H H H 2-M e,4,5-F2 0 A-1118 H H H H 0 H H H 2-0 M e,3,4-F 2 0 A-1119 H H H H 0 H H H 2-0M e,3,5-F 2 0 A-1120 H H H H 0 H H H 2-OM e,3,6-F2 0 A-1121 H H H H 0 H H H 2-M e,4,b-F 2 0 A-1122 H H H H H 0 H H 2-(0H 2 )3 -3 0 A-1123 H H H H H 0 H H 2-(0H 2) 4-3 0 A-1124 H H H H H 0 H H 2-(OCH 2CH2)-3 0 A-1125 H H H H H 0 H H 2-(0CH 2CH 2CH2)-3 0 A-1126 H H H H H 0 H H 2-(CH 2CH 20)-3 0 A-1127 H H H H H 0 H H 2-(CH 2CH 2CH 20)-3 0 A-1128 H H H H H 0 H H 3-(0H 2)3 -4 0 A-1129 H H H H H 0 H H 3-(0CH 2 4-4 0 A-1130 H H H H H 0 H H 3-(OCH 2CH2)-4 0 A-1131 H H H H H 0 H H 3-(OCH 2CH 2C2)-4 0 A-1132 H H H H H 0 H H 3-(CH 2CH 20)-4 0 A-1133 H H H H H 0 H H 3-(CH 2CH 2CH 20)-4 0 A-1134 H H H H H 0 H H 2-(OCH 20)-3 0 A-1135 H F FHIH 0 H H 3-(0CH20)-4 0
[0146]
[Table 21]
com pound RI R2 R R R A R R' (R)m P A-1136 H H H H H 0 H H 2-(0CH 2CH 20)-3 0 A-1137 H H H H H 0 H H 3-(0CH 2CH 20)-4 0 A-1138 H H H H H 0 H H 2-(0CF 2 0)-3 0 A-1139 H H H H H 0 H H 3-(00F 2 0)-4 0 A-1140 H H H H H 0 H H 2-M e,6-Et 0 A-1141 H H H H H 0 H H 2-CH 20TBS 0 A-1142 H H H H H 0 H H 2-cyclopropyl,3-0Me 0 A-1143 H H H H H 0 H H 2-cyclopropyl,4-0Me 0 A-1144 H H H H H 0 H H 2-cyclopropyl,5-0Me 0 A-1145 H H H H H 0 H H 2-cyclopropyl,6-0Me 0 A-1146 H H H H H 0 H H 2 -M e,3-0Me,6--M e 0 A-1147 H H H H H 0 H H 2-M e,4-0Me,6-M e 0 A-1148 H H H H H 0 H H 2-0Me,3-Me,6--M e 0 A-1149 H H H H H 0 H H 2-0Me,5-Me,6--M e 0 A-1150 H H H H H 0 H H 2-0Me,3-F,6-Me 0 A-1151 H H H H H 0 H H 2-0Me,5-F,6-Me 0 A-1152 H H H H H 0 H H 2-0Me,5-M e,6-F 0 A-1153 H H H H H 0 H H 2-CI,3-M e,6-F 0 A-1154 H H H H H 0 H H 2-C1,5-M e,6-F 0 A-1155 H H H H H 0 H H 2-C1,3-0Me,6-F 0 A-1156 H H H H H 0 H H 2-CI,5-0Me,6-F 0 A-1157 H H H H H 0 H H 2-M e,5-Et 0 A-1158 H H H H H 0 H H 2,6-Et 2 0 A-1159 H H H H H 0 H H 2-Et,6-F 0 A-1160 H H H H H 0 H H 2-CH 200H 3 ,6-CI 0 A-1161 H H H H H 0 H H 2-CH 200H 20H 3 ,6-CI 0 A-1162 H H H H H 0 H H 2-0Me,5-CH=N0Me 0 A-1163 H H H H H 0 H H 2-CH 2 NM e 2 0 A-1164 H H H H H 0 H H 2-CH 20CH 3 ,6-CF3 0 A-1165 H H H H H 0 H H 2-CHOC 0 A-1166 H H F H H 0 H H 2-M e 0 A-1167 H H H H H 0 CH3 H H 0 A-1168 H H H H H 0 CH3 H 2-F 0 A-1169 H H H H H 0 OH 3 H 2-Cl 0 A-1170 H H H H H 0 CH3 H 2-Br 0 A-1171 H H H H H 0 OH 3 H 2-OH 0 A-1172 H H H H H 0 OH 3 H 2-Me 0 A-1173 H H H H H 0 CH 3 H 2-Et 0 A-1174 H H H H H 0 CH 3 H 2-Pr 0 A-1175 H H H H H 0 CH 3 H 2-CF 3 0 A-1176 H H H H H 0 CH 3 H 2-CHF 2 0 A-1177 H H H H H 0 CH 3 H 2-CH 2F 0 A-1178 H H H H H 0 OH 3 H 2-CF 2CI 0 A-1179 H H H H H OH 3 H 2-cycbpropyl 0 A-1180 H H H H H 0 H3 H 2-cycobbutyl 0 A-1181 H H H H H 0 OH 3 H 2-cycobpentyl 0 A-1182 H H H H H 0 CH 3 H 2-etheny 1 0 A-1183 H H H H H 0 CH 3 H 2-aIlyl 0 A-1184 H H H H H 0 CH 3 H 2-(prop-1-en-1-y) 0 A-1185 H H H H H 0 OH 3 H 2-(triflioroethenyD 0 A-1186 H H H H H 0 CH 3 H 2-0M e 0 A-1187 H H H H H 0 OH 3 H 2-0Et 0 A-1188 H H H H H F0 H3 H 2-0Pr 0 A-1189 H H H H H 0 CH 3 H 2-0(/-Pr) 0 A-1190 H H H H H 0 CH 3 H 2-0CF3 0 A-1191 H H H H H 0 OH 3 H 2-0CHF 2 0 A-1192 H H H H H 0 OH 3 H 2-(cycbpropy bxy) 0
[0147]
[Table 22]
com pound RI R2 R R R A R R' (R)m P A-1193 i H H H H H 0 CH, H 2-(cycobbuty bxy) 0 A-1194 H H H H H 0 CH, H 2-(cycbpenty bxy) 0 A-1195 H H H H H 0 CH, H 2-((2,2-d ih brocycobpropy Doxy) 0 A-1196 H H H H H 0 OH, H 2-(oxiran-2-y D 0 A-1197 H H H H H 0 CH3 H 2-SM e 0 A-1198 H H H H H 0 CH3 H 3-SM e 0 A-1199 H H H H H 0 CH3 H 2-S (= )M e 0 A-1200 H H H H H 0 CH3 H 3-S (= )M e 0 A-1201 H H H H H 0 CH3 H 2-S (=0) 2M e 0 A-1202 H H H H H 0 OH 3 H 3-S (=0)2 M e 0 A-1203 H H H H H 0 OH 3 H 2-SOF 3 0 A-1204 H H H H H 0 OH 3 H 3-SOF 3 0 A-1205 H H H H H 0 OH 3 H 3-S (=U)G 3 0 A-1206 H H H H H 0 CH 3 H 3-SCF(CF 3) 2 0 A-1207 H H H H H 0 CH 3 H 2-(cycbpropy th b) 0 A-1208 H H H H H 0 OH 3 H 2-(cycbpropysu finy D 0 A-1209 H H H H H 0 OH 3 H 2-(cycbpropy u fony D 0 A-1210 H H H H H 0 CH 3 H 2-C (=0)M e 0 A-1211 H H H H H 0 OH 3 H 2-CH 20(=0 )CH3 0 A-1212 H H H H H 0 CH 3 H 2-CH 2C 0(= )CF3 0 A-1213 H H H H H 0 CH 3 H 2-CH 2 0H 0 A-1214 H H H H H 0 CH 3 H 2-CH 2 0CH 3 0 A-1215 H H H H H 0 CH 3 H 2-CH 2 0CH 2CH 3 0 A-1216 H H H H H 0 CH 3 H 2-CH 2SCH 3 0 A-1217 H H H H H 0 OH 3 H 2-CH 2 S(=30H3 0 A-1218 H H H H H 0 OH 3 H 2-CH 2 S(=O 2 H3 0 A-1219 H H H H H 0 OH 3 H 2-(benzy bxy) 0 A-1220 H H H H H 0 CH 3 H 2-NH 2 0 A-1221 H H H H H 0 CH 3 H 2-NH M e 0 A-1222 H H H H H 0 CH 3 H 2-N ( e)2 0 A-1223 H H H H H 0 CH 3 H 2-(1,3-d bxo an-2-y D 0 A-1224 H H H H H 0 CH 3 H 2-(1,3-d bxan-2-y D 0 A-1225 H H H H H 0 CH 3 H 2-(1H-im dazokE2-yD 0 A-1226 H H H H H 0 OH3 H 2-(thiazo -2-yl) 0 A-1227 H H H H H 0 CH 3 H 2-(oxazol-2-y D 0 A-1228 H H H H H CH 3 O H 2-CH= NOH 0 A-1229 H H H H H 0 OH 3 H 2-CH= NOM e 0 A-1230 H H H H H 0 CH 3 H 2-(4,5-dihydro-3-oxazo D 0 A-1231 H H H H H 0 CH 3 H 2-CN 0 A-1232 H H H H H 0 CH 3 H 2-N0 2 0 A-1233 H H H H H 0 CH 3 H 2-F,6-O 1 0 A-1234 H H H H H 0 CH 3 H 2-F,6-M e 0 A-1235 H H H H H CH 3 O H 3-F,6-M e 0 A-1236 H H H H H O 3 CH H 4-F,2-M e 0 A-1237 H H H H H 0 OH 3 H 2-F,6-0M e 0 A-1238 H H H H H 0 OH 3 H 3-F,6-0M e 0 A-1239 H H H H H 0 CH 3 H 2,6-C 0 A-1240 H H H H H 0 CH 3 H 2-C 1,6-M e 0 A-1241 H H H H H 0 CH 3 H 3-C 1,6-M e 0 A-1242 H H H H H 0 OH 3 H 4-C 1,2-M e 0 A-1243 H H H H H 0 CH 3 H 2-C I,5-CF3 0 A-1244 H H H H H 0 OH 3 H 2-0 ,6-GF 3 0 A-1245 H H H H H CH 3 O H 2-C 1,6-0M e 0 A-1246 H H H H H 0 CH 3 H 3-C 1,6-0M e 0 A-1247 H H H H H 0 CH 3 H 4-C 1,2-0 M e 0 A-1248 H H H H H 0 GH 3 H 2,4-M e 2 0 A-1249 H H H H H 0 OH 3 H 2,b-M e 2 0
[0148]
[Table 23]
com pound R' R2 R R A R R' (R)m p A-1250 H H H H 0 OH 3 H 2,6-M e 2 0 A-1251 H H H H 0 OH 3 H 2-M e,4-0F 3 0 A-1252 H H H H O 0H3 H 2-M e,b-CF3 0 A-1253 H H H H i 0 OH 3 H 2-M e,6-GH 3 0 A-1254 H H H H O 0H3 H 2-M e,4-0M e A-1255 H H H H 0 OH 3 H 2-M e,b-OM e 0 A-1256 H H H H D OH 3 H 2-M e,6-0M e 0 A-1257 H H H H 0 OH 3 H 3-M e,6-0M e 0 A-1258 H H H H H 0 OH 3 H 4-M e,2-0M e 0 A-1259 H H H HDif0H3 H 2,b-Me2 0
A-1260 H H H H i 0 OH 3 H 2,6-0M e 2 A-1261 H H H H 0 OH 3 H 2-1Me,6-GH 3 0 A-1262 H H H H f0 OH 3 H 2-CHH 2,b-H 0
A-1263 H H H H 0 OH 3 H 2-CHF 2,6-F 0 A-1264 H H H H 0 OH 3 H 2-CH F2,b-M e 0 A-1265 H H H H 0 OH 3 H 2-CH F 2,6-M e0 A-1266 H H H H GH O 3 H 2-cycbpropy 1,b-F 0 A-1267 H H H H 0 OH 3 H 2-cycbpropy 1,6-F 0 A-1268 H H H H GH O 3 H 2-cyclopropylb-M e 0 A-1269 H H H H 0 OH 3 H 2-cyclopropyl,6-M e 0 A-1270 H H H H O0H3 H 2-ethenyl,6-F 0 A-1271 H H H H O0 CH3 H 2-ethenyl,6- e 0 A-1272 H H H H 0 OH 3 H 2-0Etb-FHW A-1273 H H H H Hi0 OH 3 H 2-0Et6-F 0 A-1274 H H H H HDi OH 3 H 2-0Etb- CI 0 A-1275 H H H H Hi0 OH 3 H 2-OEt6-C I 0 A-1276 H H H H GH O 3 H 2-0Etb-M e 0 A-12// H H H H i 0 OH 3 H 2-OEt6-M e 0 A-1278 H H H H 0 OH 3 H 2-0)H F 2,b-F 0 A-12/9 H H H H 0 OH 3 H 2-0)H F 2,6-F 0 A-1280 H H H H O0H3 H 2-OHF2,b-Me 0 A-1281 H H H H 0 OH 3 H 2-0)H 12,6-M e 0 A-1282 H H H H O0H3 H 2-(cycobpropyloxy),b-F 0 A-1283 H H H H O 3 GH H 2-(cycobpropyloxy),6-F 0 A-1284 H H H H O0H3 H 2-(cyclopropybxy),b5- e 0 A-1285 H H H H 0 OH 3 H 2-(cyclopropybxy),6M e 0 A-1286 H H H H GH 3 O H 2-SM e,b-F 0 A-1287 H H H H 0 OH 3 H 2-SM e,6-F 0 A-1288 H H H H 0 OH 3 H 2-SM e,b-M e 0 A-1289 H H H H H 0 OH 3 H 2-SM e,6-M e 0 A-1290 H H H H 0 OH 3 H 2-S(=0)M e,b-F 0 A-1291 H H H H OD CH3 H 2-S(=0)Me,6-F 0 A-1292 H H H H GH 3 O H 2-S = )Me,5- e 0 A-1293 H H H H GH 3 O H 2-S = )Me,6Me A-1294 H H H H GH 3 O H 2-S (=) 2 M eb-H 0 A-1295 H H H H GH 3 O H 2-S(=U) 2Me,6-F A-1296 H H H H 0 OH 3 H 2-S(= 0) 2 M e,b- e 0 A-1297 H H H H 0 OH 3 H 2-S(= 0)2 Me,6--M e 0 A-1298 H H H H 0 OH 3 H 2-SCF 3 ,b-F 0 A-1299 H H H H f0 OH 3 H 2-SF 3 ,6-FF A-1300 H H H H O0H3 H 2-SGF,5-3 e 0 A-1301 H H H H GH O 3 H 2-SGF 3 ,6-M e 0 A-1302 H H H H HiF OH 3 H 2-S (=O)GF 3,b-F A-1303 H H H H 0 OH 3 H 2-S (=U)F3 ,6-F 0 A-1304 H H H H f0 OH 3 H 2-S =U)GF 3 ,b-Me 0 A-1305 H H H H f0 OH 3 H 2-S = )F 3 ,6-Me A-1306 H H H H f0 OH 3 H 2-S (=0)2 F 3 ,b-F 0
[0149]
[Table 24]
com pound R' R2 R R A R R' (R)m p A-130/ i H H H H 0 OH3 H 2-S (=U)20F3,6-F 0 A-1308 H H H H 0 OH 3 H 2-S(=D) 2OF 3 ,b5-e A-1309 H H H H O0H3 H 2-S(=D) 2OF3,6-Me A-1310 H H H H GH 3 O H 2-(cycobpropylth b),b-F 0 A-1311 H H H H O 0H3 H 2-(cycobpropylth b),6-F 0 A-1312 H H H H 0 OH 3 H 2-(cycbpropy thio),b-M e 0 A-1313 H H H H D OH 3 H 2-(cycbpropy thio),6-M e 0 A-1314 H H H H 0 OH 3 H 2- 0(= )M e,b-F 0 A-1315 H H H H H 0 OH 3 H 2- (=0)M e,6-F 0 A-1316 H H H H D if 0 H3 H 2-)(=0)M e,b-M e 0 A-1317 H H H H Ei 0 OH 3 H 2-O(= )Me,6-Me 0 A-1318 H H H H 0 OH 3 H 2-CH 2UH,b-H A-1319 H H H H f0 OH 3 H 2-CH 2UN,6-F A-1320 H H H H 0 OH 3 H 2-OH 2UH,b5-M e 0 A-1321 H H H H 0 OH 3 H 2-OH 2UH,6 -Me 0 A-1322 H H H H f0 OH 3 H 2-GH 20H 3 ,4-F 0 A-1323 H H H H f0 OH 3 H 2-GH 20H 3,b-H 0 A-1324 H H H H 0 OH 3 H 2-OH 20H 3,6-F 0 A-1325 H H H H f0 OH 3 H 2-CH 2UGH 3 ,4-M e 0 A-1326 H H H H 0 OH 3 H 2-OH 20H 3 ,b-i e 0 A-1327 H H H H 0 OH 3 H 2-OH 20H 3 ,6-Me 0 A-1328 H H H H f0 OH 3 H 2-0 C(= 0)CH 3 ,b-4 0 A-1329 H H H H 0 OH 3 H 2-O =0)H 3 ,6-F 0 A-1330 H H H H O 0H3 H 2-O=0)H3,b-M e 0 A-1331 H H H H 0 OH 3 H Z-(=U)GH 3,6-Me 0 A-1332 H H H H f0 OH 3 H Z-2S =OU 2 GH 3,b-H A-1333 H H H H Hi0 OH 3 H 2-OS (= ) 2 GH 3 ,6- 0 A-1334 H H H H i 0 OH 3 H 2-0S(= 0) 2 H 3,b-M e 0 A-1335 H H H H 0 OH 3 H 2-US(= 0) 2 H 3,6-M e 0 A-1336 H H H H 0 OH 3 H 2-OH 2 SOH 3 ,b-4 0 A-1337 H H H H 0 OH 3 H 2-OH 2 SOH 3 ,6-F 0 A-1338 H H H H 0 OH 3 H 2-OH 2SOH 3,b-M e 0 A-1339 H H H H H 0 OH 3 H 2-OH 2SOH 3,6-M e 0 A-1340 H H H H OH 3 H 2-AMe 2 ,b-H 0 A-1341 H H H H E 0 OH3 H 2-NMe 2 ,6-F 0 A-1342 H H H H f Df OH 3 H 2AM e 2 ,5-A e 0 A-1343 H H H H f0 OH 3 H 2-NM e 2 ,6-M e 0 A-1344 H H H H 0 OH 3 H 2-ON,4-F 0 A-1345 H H H H 0 OH 3 H 2-ONb-F 0 A-1346 H H H H H 0 OH 3 H 2-ON,6-F 0 A-1347 H H H H 0 OH 3 H 2-ON,6-M e 0 A-1348 H H H H 0 OH 3 H 2-ON,b-OM e 0 A-1349 H H H H GH O 3 H 2-ON,6-OM e 0 A-1350 H H H H GH O 3 H 3-ON,6-M e 0 A-1351 H H H H O GH 3 H 3-ON,6-OM e 0 A-1352 H H H H f0 OH 3 H 4-ON,2-Me 0 A-1353 H H H H D OH 3 H 4-N,2-OM e 0 A-1354 H H H H 0 OH 3 H 240 2,4-F 0 A-1355 H H H H 0 OH 3 H 2-N0 2 ,5-F 0 A-1356 H H H H f0 OH 3 H 240 2 ,6-F 0 A-1357 H H H H 0 OH 3 H 2-0 2,4-MvAe 0 A-1358 H H H H f0 OH 3 H 2-N 2,b-m e 0 A-1359 H H H H F OH 3 H 2A0 2,6 Ae 0 A-1360 H H H H 0 OH 3 H 2-M e,4,b-F 2 0 A-1361 H H H H f0 OH 3 H 2-M e,6-Et 0 A-1362 H H H H f0 OH 3 H 2-cyclopropyl,6-OM e 0 A-1363 H H H H f0 GH 3 H 2-M e,b-Et 0
[0150]
[Table 25]
com pound R' R2 R R A R R' (R)m p A-1364f H H H H 0 OH 3 H 2,6-Et 2 0 A-1365 H H H f0 H OH 3 H 2-Et,6-F 0 A-1366 H H H H 0 OH 3 H 2-0H 20H 3 ,6-CI I A-1367 H H H if 0 H GH 3 H 2-0H 20H 20H 3 ,6-CI1 A-1368 H H H O0H3 H H 2-CH2NMe2 0 A-1369 H H H D0 H2CH3 H H H 0 A-1370 H H H D0 H2CH3 H H 2-F 0 A-1371 H H H H 0 CH 2CH 3 H 2-Cl 0 A-1372 H H H H H 0 CH 2CH 3 H 2-Br 0 A-1373 H H H D 0GH20H3 H H 2-OH 0 A-1374 H H H H i 0 GH 20H 3 H 2-M e 0 A-1375 H H H H D GH 20H 3 H 2-Et 0 A-1376 H H H H GH 20H 3 H 2-Pr 0 A-13// H H H H 0 H 2CH 3 H 2-CF 3 0 A-1378 H H H H 0 OH 2CH 3 H 2-UH F 2 A-13/9 H H H H H0 GH 20H 3 H 2-CH 2F 0
A-1380 H H H H H0 GH 20 3 H 2-GH 2G1 0 A-1381 H H H D 0 H2CH3 H H 2-cycbpropy1 0 A-1382 H H H f0 H GH 20H 3 H 2-cycobbutyl 0 A-1383 H H H H 0 OH 2CH 3 H 2-cycbpenty 1 0 A-1384 H H H f0 H OH 2CH 3 H 2-ethenyl 0 A-1385 H H H f0 H OH 2CH 3 H 2-a ly 0 A-1386 H H H D 0 H2CH3 H H 2-(prop-l-en-1-y D 0 A-138 / H H H H i 0 OH 2CH 3 H 2-(trfboroethenyD 0 A-1388 H H H H GH 20H 3 H 2-M e 0 A-1389 H H H iH GH 20H 3 H 2-)Et 0 A-1390 H H H H GH 20H 3 H 2-UPr 0 A-1391 H H H H i 0 OH 2CH 3 H 2-0 (/-Pr) 0 A-1392 H H H H 0 OH 2CH 3 H 2-0GF 3 0 A-1393 H H H H 0 OH 2CH 3 H 2-0)H F 2 A-1394 H H H D 0 H2CH3 H H 2-(cycbpropy bxy) 0 A-1395 H H H H 0 OH 2CH 3 H 2-(cycobbuty loxy) 0 A-1396 H H H i 0 H OH 2CH 3 H 2-(cycbpenty bxy) 0 A-1397 H H H f0 H GH 20H 3 H 2-((2,2-d ich brocycbpropy )oxy) 0 A-1398 H H H D 0 H2CH3 H H 2-(oxiran-2-y D0 A-1399 H H H H D GH 20H 3 H 2-SMe 0 A-1400 H H H H GH 20H 3 H 3-SMe 0 A-1401 H H H H D 0 H2CH3 H 2-S(=0)Me 0 A-1402 H H H H 0 OH 2CH 3 H 3-S(=0)M e 0 A-1403 H H H H D 0 H2CH3 H 2-S (=0)2Me 0 A-1404 H H H H 0 OH 2CH 3 H 3-S (=0) 2 M e 0 A-1405 H H H H Ei0 H2CH 3 H 2-SOF 3 0 A-1406 H H H H H 0 GH 20H 3 H 3-SGH 3 A-140/ H H H H f0 GH 20H 3 H 3-S (= U)GH 3 A-1408 H H H H D GH 20H 3 H 3-SCF(GF 3) 2 A-1409 H H H H GH 20H 3 H 2-(cycbpropythb) 0 A-1410 H H H H 0 OH 2CH 3 H 2-(cycbpropylsu finy D 0 A-1411 H H H H 0 OH 2CH 3 H 2-(cycbpropy u fony D 0 A-1412 H H H H 0 OH 2CH 3 H 2-C (=0)M e 0 A-1413 H H H HIF GH 20H 3 H 2-GH 2 (= U)0H 3 A-1414 H H H H 0 OH 2CH 3 H 2-CH 2 (= 0)CF 3 A-1415 H H H H 0 GH 20H 3 H 2-CH 2 H 0 A-1416 H H H H 0 GH 20 3 H 2-H 2 UGH 3 A-141/ H H H H 0 OH 2CH 3 H 2-CH 20H 2CH 3 0
A-1418 H H H H H 0 H 2CH 3 H 2-CH 2SOH 3 0 A-1419 H H H H GH 20H 3 H 2-CH 2S = )GH 3 0
A-1420 H H H H 0 H 2OH 3 H 2-CH 2S(= 0) 2 H 3 0
[0151]
[Table 26]
com pound R' R2 R R A R R' (R)m p A-1421 H H H H 0 CH 2CH 3 H 2-(benzy bxy) 0 A-1422 H H H H f0 CH 2CH 3 H 2-NH 2 A-1423 H H H H D 0 H2CH3 H 2-NH M e A-1424 H H H H i 0 GH 20H 3 H 2 NM e)2 0 A-1425 H H H H D CH 2CH 3 H 2-0,3-d bxo an-2-y D A-1426 H H H H 0 CH 2CH 3 H 2-0,3-d bxan-2-y D 0 A-1427 H H H H 0 CH 2CH 3 H 2-(1H-m idazokE2-yD 0 A-1428 H H H H D 0 H 2CH3 H 2-(thiazo b-2-y) 0 A-1429 H H H H H 0 CH 2CH 3 H 2-(oxazol-2-y D 0 A-1430 H H H H D 0 GH20H3 H 2-GH=N0H 0 A-1431 H H H H i 0 GH 20H 3 H 2-CH= NUM e 0 A-1432 H H H H D GH 20H 3 H 2-(4,b-dihydro-3-soxazo yD 0 A-1433 H H H H H GH 20H 3 H 2-N 0 A-1434 H H H H 0 0H 2CH 3 H 2-NO 2 0
A-1435 H H H H 0 0H 2CH 3 H 2-F,6-GI 0 A-1436 H H H H f GH 20H 3 H 2-F,6-M e 0 A-1437 H H H H f0 GH 20H 3 H 3-F,6-M e 0 A-1438 H H H H D0 2HCH3 H 4-F,2-Me 0 A-1439 H H H H GH 20H 3 H 2-F,6-M e 0 A-1440 H H H H 0 0H 2CH 3 H 3-F,6-M e 0 A-1441 H H H H H0 0H 2CH 3 H 2,6-O 0 A-1442 H H H H f0 0H 2CH 3 H 2- 1,6-M e 0 A-1443 H H H H D0 2HCH3 H 3- 1,6-Me F A-1444 H H H H f0 0H 2CH 3 H 4- 1,2-M e 0 A-1445 H H H H 0 GH 20H 3 H 2-C ,b-CF3 0 A-1446 H H H H 0 GH 20H 3 H 2-C ,6-CF3 0 A-1447 H H H H GH 20H 3 H 2-G 1,6-0M e 0 A-1448 H H H H i 0 0H 2CH 3 H 3-G 1,6-0M e 0 A-1449 H H H H D 0 H2CH3 H 4-G1,2-0M e 0 A-1450 H H H H 0 0H 2CH 3 H 2,4-M e 2 0 A-1451 H H H H D0 H2CH3 H 2,5-Me2 0 A-1452 H H H H 0 0H 2CH 3 H 2,6-M e2 0
A-1453 H H H H H 0 0H 2CH 3 H 2-M e,4-0F 3 0 A-1454 H H H H f0 GH 20H 3 H 2-M e,b-CF 3 0 A-1455 H H H H 0 H2CH 3 H 2-M e,6-F 3 0
A-1456 H H H H D GH 20H 3 H 2 -Me,4-0Me A-1457 H H H H E 0 0G 2GH 3 H 2 -Me,b-UMe 0 A-1458 H H H H D 0 H2CH3 H 2-Me,6-0M e 0 A-1459 H H H H 0 0H 2CH 3 H 3-M e,6-0M e 0 A-1460 H H H H H 0 0H 2CH 3 H 4-M e,2-0M e 0 A-1461 H H H H 0 0H 2CH 3 H 2,b-M e 2 0
A-1462 H H H H D0 H2CH3 H 2,6-UMe2 0 A-1463 H H H H GH 20H 3 H 2-OMe,6-GH 3 0 A-1464 H H H H H GH 20H 3 H 2-CHH 2,b-H 0
A-1465 H H H H D GH 20H 3 H 2-CHH 2,6-F 0 A-1466 H H H H f0 GH 20H 3 H 2-CH H 2,b e 0 A-1467 H H H H D 0 H2CH3 H 2-GHF2,6-i e 0 A-1468 H H H H 0 0H 2CH 3 H 2-cycbpropy 1,b-F 0 A-1469 H H H H 0 0H 2CH 3 H 2-cycbpropy 1,6-F 0 A-1470 H H H H f0 GH 20H 3 H 2-cyclopropyLb-M e 0 A-1471 H H H H D 0 H2CH3 H 2-cyclopropyL,6-M e 0 A-1472 H H H H D GH 20H 3 H 2-ethenyl,6-F 0 A-1473 H H H H EF 0HGC 2GH 3 H 2-ethenyl,6-M e 0 A-1474 H H H H 0 0H 2CH 3 H 2-0Etb-F 0 A-1475 H H H H H0 0H 2CH 3 H 2-UEt6-F 0 A-1476 H H H H H0 GH 20H 3 H 2-U Eto-UI F A-1477 H H H I H10 GH 2 H 3 H 2-U Et6- I 0
[0152]
[Table 27]
com pound R' R2 R R A R R' (R)m p A-1478 H H H H 0 CH 2CH 3 H 2-Et,b-M e 0 A-1479 H H H H H 0 H 2CH 3 H 2-0Et,6-M e A-1480 H H H H 0 CH 2CH 3 H 2-UCH F 2,b-F W A-1481 H H H H i 0 GH 20H 3 H 2-UCH H 2,6-H 0 A-1482 H H H H D 0 H2CH3 H 2-OCHF2,b-M e 0 A-1483 H H H H 0 CH 2CH 3 H 2-0CH F 2 ,6-M e 0 A-1484 H H H H 0 CH 2CH 3 H 2-(cycbpropyloxy),b-F 0 A-1485 H H H H D 0 H2CH3 H 2-(cycbpropyloxy),6-F 0 A-1486 H H H H H 0 CH 2CH 3 H 2-(cyclopropybxy),b-M e 0 A-1487 H H H H i EH GH 2GH 3 H 2-(cyclopropybxy),6-M e 0 A-1488 H H H H i 0 GH 20H 3 H 2-SM e,b-F 0 A-1489 H H H H D GH 2 0H 3 H 2-SM e,6-F 0 A-1490 H H H H GH 20H 3 H 2-SM e,b-M e 0 A-1491 H H H H 0 0H CH 32 H 2-SM e,6-M e 0 A-1492 H H H H 0 0H CH 32 H 2-S(=0)Me,b-F 0 A-1493 H H H H 7 GH 20H 3 H 2-S(= 0)Me,6-F 0 A-1494 H H H H i 0 GH 20H 3 H 2-S = )Meb-M e 0 A-1495 H H H H 0 H CH 32 H 2-S (=0)Me,6-M e 0 A-1496 H H H H GH 20H 3 H 2-S =) 2 Me,b-H 0 A-1497 H H H H 0 0H 2CH 3 H 2-S(= 0)M e,6-F 0 A-1498 H H H H H 0 H 2CH 3 H 2-S(= 0) 2 M e,b-M e 0 A-1499 H H H H H 0 H 2CH 3 H 2-S (=0 )2 M e,6 -Me 0 A-lb00 H H H H 0 0H 2 CH 3 H 2-SCF3,b-F F A-1b01 H H H H Hi0 0H 2 CH 3 H 2-SCF 3 ,6-F 0 A-1502 H H H H GH 20H 3 H 2-SCF 3 ,b-Me 0 A-1503 H H H H GH 20H 3 H 2-SCF 3 ,6-M e 0 A-1504 H H H H GH 20H 3 H 2-S (=O)F 3 ,b-F A-l50b H H H H i 0 0H 2CH 3 H 2-S (=0)F3 ,6-F 0 A-1506 H H H H D0 H2CH3 H 2-S(=U)F3,b-Me 0 A-lb0/ H H H H 0 0H 2CH 3 H 2-S(=U)F 3 ,6-Me 0 A-lb08 H H H H 0 0H 2CH 3 H 2-S(=0)2 G3,b-F 0 A-1509 H H H H 0 0H 2CH 3 H 2-S(=0) 2 F 3 ,6-F 0 A-1510 H H H H 0 H 2CH 3 H 2-S(=0) 2 F 3 ,b-Me 0 A-1511 H H H H 0 H 20H 3 H 2-S(=U)2 F 3 ,6-Me 0 A-1512 H H H H 0 0H 2CH 3 H 2-(cycobpropy thb),b-F 0 A-1513 H H H H D GH 20H 3 H 2-(cycobpropy thb),6-F 0 A-1514 H H H H H GH 20H 3 H 2-(cycobpropythio),b-M e 0 A-ibi1 H H H H 0 0H 2CH 3 H 2-(cycobpropythio),6-M e 0 A-1516 H H H H 0 0H 2CH 3 H 2-C (=0)M e,-F 0 A-l 7 H H H H H 0 0H 2CH 3 H 2-C (=0)M e,6-F 0 A-ll8 H H H H 0 0H 2CH 3 H 2-C(= 0)M e,-M e 0 A-l l9 H H H H D H 2CH 3 H 2-C(= 0)M e,6M e 0 A-1520 H H H H f0 GH 20H 3 H 2-CH 2UH,b-H 0 A-1521 H H H H f0 GH 20H 3 H 2-CH 2UN,6-F A-1522 H H H H D GH 2 0H 3 H 2-CH 2 H,b-Me 0 A-1523 H H H H 0 GH 20H 3 H 2-CH 2 H,6-M e 0 A-1524 H H H H 0 0H 2CH 3 H 2-0H 20H 3 ,4-F 0 A-1525 H H H H 0 0H 2CH 3 H 2-0H 20H 3,5-F 0 A-1526 H H H H 0 0H 2CH 3 H 2-0H 20H 3 ,6-F 0 A-1527 H H H H 0 H 20H 3 H 2-CH 20H 3 ,4-M e 0 A-1528 H H H H 0 0H 2CH 3 H 2-0H 20H 3 ,-M e 0 A-1529 H H H H GH 20H 3 H 2-CH 20H 3,6-M e 0 A-1530 H H H H - GH 20H 3 H 2-0 C= U)0H 3,b-F A-1531 H H H H 0 0H 2 CH 3 H 2-0)C =0 )CH 3 ,6-F 0 A-1532 H H H jH j H 2CH 3 H 2-0C(=0)CH 3 ,5-M e 0 A-1533 H H H H E U GH 2GH 3 H 2-C0(=U)GH 3 ,6-M e A-lb34 H H H H Hf H 20H 3 H 2-US (= U)2 H 3 ,5-F 0
[0153]
[Table 28]
com pound R' R2 R R A R R' (R)m p A-1535 H H H H 0 CH 2CH 3 H 2-US (= 0) 2 H 3 ,6-F 0 A-1536 H H H H H 0 H 2CH 3 H 2-S(= 0) 2 CH 3,b-Me A-1537 H H H H 0 H 2CH 3 H 2-US(= 0) 2 H 3,6-Me A-1538 H H H H i 0 GH 20H 3 H 2-GH 2SCH 3 ,b-F 0
A-1539 H H H H 0 0H 2CH 3 H 2-OH 2 SCH 3 ,6-F 0 A-1540 H H H H 0 0H 2 CH 3 H 2-OH 2SCH 3,b-M e 0 A-1541 H H H H D0 H 2CH3 H 2-OH2SCH3,6-M e 0 A-1542 H H H H 0 0H 2CH 3 H 2-NM e 2 ,b-F 0 A-1543 H H H H 0 0H 2CH 3 H 2-NM e 2 ,6-F 0 A-1544 H H H H D 0H 20H 3 G H 2A Me 2 1--e 0 A-1545 H H H H i 0 GH 20H 3 H 2-NM e 2 ,6-M e 0 A-1546 H H H H D GH 20H 3 H 2-ON4-F 0 A-1547 H H H H GH 20H 3 H 2-ONb-F 0 A-1548 H H H H 0 0H 2CH 3 H 2-N,6-F 0 A-1549 H H H H 0 0H 2CH 3 H 2-ON,6-M e 0 A-1bb0 H H H H F GH 20H 3 H 2-ON,b-UM e 0 A-1bb1 H H H H 0 H 20H 3 H 2-ON,6-UM e 0 A-1552 H H H H D 0 H2CH3 H 3-ON,6-Me 0 A-1553 H H H H GH 20H 3 H 3-ON,6-OM e 0 A-1554 H H H H 0 0H 2CH 3 H 4-ON,2-M e 0 A-1bbb H H H H 0 H 2CH 3 H 4-ON,2-OM e 0 A-1556 H H H H f0 0H 2CH 3 H 2-N0 2,4-F 0 A-lb/ H H H H 0 0H 2CH 3 H 2-N0 2 ,b-F F A-1bb8 H H H H 0 0H 2CH 3 H 2-N0 2 ,64 0 A-1559 H H H H GH 20H 3 H 2A U 2,4-MA e 0 A-1560 H H H H GH 20H 3 H 2A U 2,b-Ae 0 A-1561 H H H H GH 20H 3 H 2-NU 2,6-Me 0 A-1562 H H H H i 0 0H 2CH 3 H 2-M e,4,b-F 2 0 A-1563 H H H H 0 0H 2CH 3 H 2-M e,6-Et 0 A-1564 H H H H 0 0H 2CH 3 H 2-cyclopropyl,6-OM e 0 A-1565 H H H H 0 0H 2CH 3 H 2-M e,b-Et 0 A-1566 H H H H 0 0H 2CH 3 H 2,6-Et 2 0 A-1567 H H H H H 0 0H 2CH 3 H 2-Et,6-F 0 A-1568 H H H H f0 GH 20H 3 H 2-GH 20H 3 ,6-C F A-1569 H H H H 0 0H 2CH 3 H 2-OH 20H 2 CH 3 ,6-OI 0 A-1b70 H H H H E D H 2GH 3 H 2-H 2 NMe 2 0 A-lb/ 1 H H H H H GH 20H 20H 3 H H 0 A-1b72 H H H H 0 0H 2CH 2CH 3 H 2-F 0 A-1b73 H H H H 0 0H 2CH 2CH 3 H 2-CI 0 A-1b74 H H H H H 0 0H 2CH 2CH 3 H 2-Br 0 A-lb/b H H H H 0 0H 2CH 2CH 3 H 2-OH 0 A-1b76 H H H H 0 0H 2CH 2CH 3 H 2-M e 0 A-lb// H H H H i GH 20H 20H 3 H 2-Et 0 A-ib/8 H H H H GH 20H 20H 3 H 2-Pr 0 A-lb/9 H H H H D GH 20H 20H 3 H 2-GH 3 0 A-ib80 H H H H i GH 20H 20H 3 H 2-GH F 2 A-b81 H H H H D 0H 2CH 2CH 3 H 2-OH 2F 0
A-lb82 H H H H 0 0H 2CH 2CH 3 H 2-OF 2C I 0 A-lb83 H H H H 0 0H 2CH 2CH 3 H 2-cycbpropy 1 0 A-lb84 H H H H f0 GH 20H 20H 3 H 2-ycobbutyl 0 A-ibb H H H H 0 0H 2CH 2CH 3 H 2-cycbpenty I F A-lb86 H H H H f0 GH 20H 20H 3 H 2-ethenyl 0 A-lb8 H H H H GH 20H 20H 3 H 2-allyl A-lb88 H H H H 0 0H 2CH 2CH 3 H 2-(prop-i-en-1-y D 0 A-ib89 H H H H f0 0H 2CH 2CH 3 H 2-(trffboroetheny D 0 A-lb90 H H H H H GH 20H 20H 3 H 2-0M e A-lb91 H H H H H0f 0H 20H 20H 3 H 2-ULt 0
[0154]
[Table 29]
com pound R' R2 R R A R R' (R)m p A-1592 H H H H 0 0H 2CH 2CH 3 H 2-OPr 0 A-1593 H H H H H 0 0H 2CH 2CH 3 H 2-0 (/-Pr) A-1594 H H H H 0 0H 2CH 2CH 3 H 2-4)H3 A-1595 H H H H i 0 GH 20H 20H 3 H 2-0CH 2 0
A-1596 H H H H 0 0H 2CH 2CH 3 H 2-(cycbpropy bxy) 0 A-1597 H H H H 0 0H 2CH 2CH 3 H 2-(cycbbuty bxy) 0 A-1598 H H H H 0 0H 2CH 2CH 3 H 2-(cycbpenty bxy) 0 A-1599 H H H H 0 0H 2CH 2CH 3 H 2-((2,2-d ih brocycbpropy Doxy) 0 A-1600 H H H H 0 0H 2CH 2CH 3 H 2-(oxiran-2-y D0 A-1601 H H H H D G 0H20H20H3 H 2-SMe 0 A-1602 H H H H i 0 GH 20H 20H 3 H 3-SMe 0 A-1603 H H H H D GH 20H 20H 3 H 2-S(=0)M e 0 A-1604 H H H H GH 20H 20H 3 H 3-S =0 )M e 0 A-1605 H H H H 0 0H 2CH 2CH 3 H 2-S(= 0)2 M e 0 A-1606 H H H H 0 0H 2CH 2CH 3 H 3-S(= 0) 2M e 0 A-1607 H H H H 0 GH 20H 20H 3 H Z-SCF3 A-1608 H H H HIF0 GH 20H 2 0H 3 H 3-SG 3 0 A-1609 H H H H 0 0H 2CH 2CH 3 H 3-S (=0)F 3 A-1610 H H H H I GH 20H 20H 3 H 3-SCF(G 3 )2 0
A-1611 H H H H 0 0H 2CH 2CH 3 H 2-(cycbpropy thb) 0 A-1612 H H H H f0 0H 2CH 2CH 3 H 2-(cycbpropy Isu finy D 0 A-1613 H H H H f0 0H 2CH 2CH 3 H 2-(cycbpropy u fony D 0 A-1614 H H H H D 0 H2CH2CH 3 H 2-G (=0)Me 0 A-1615 H H H H H0 0H 2CH 2CH 3 H 2-GH 2C (= )0H3 0 A-1616 H H H H GH 2 0H2 0 3 H Z-GH 2G =OU 3 A-1617 H H H H H0 GH 20H 20H 3 H 2-CH 2 H 0 A-1618 H H H H H0 GH 20H 20H 3 H 2-GH 20H 3 0
A-1619 H H H H H if 0 0H 20H 2CH 3 H 2-0H 2 0H CH 3 2 0 A-1620 H H H H D0 CH0H2H2H3 H 2-OH2SCH3 0 A-1621 H H H H 0 0H 2CH 2CH 3 H 2-H 2S (=0 )H 3 0
A-1622 H H H H D0 CH 0H2H2H3 H 2CH 2-GH 2S(= 0) 3 A-1623 H H H H 0 0H 2CH 2CH 3 H 2-(benzy bxy) 0 A-1624 H H H H H 0 0H 2CH 2CH 3 H 2-NH 2 0 A-1625 H H H H f0 GH 20H 20H 3 H 2-NH M e A-1626 H H H H 0 0H 2CH 2CH 3 H 2 N e) 2 0 A-1627 H H H H D GH 20H 20H 3 H 2-0,3-d bxolan-2-yD 0 A-1628 H H H H f0 GH 20H 20H 3 H 2-0,3-d bxan-2-y D A-1629 H H H H 0 0H 2CH 2CH 3 H 2-(lH-m idazokE2-yD A-1630 H H H H 0 0H 2CH 2CH 3 H 2-(thiazo -2-y) 0 A-1631 H H H H H 0 0H 2CH 2CH 3 H 2-(oxazol-2-yD 0 A-1632 H H H H 0 0H 2CH 2CH 3 H 2-GH= N0H 0 A-1633 H H H H 0 0H 2CH 2CH 3 H 2-CH= NOM e 0 A-1634 H H H H ii f CH2CH20H3 H 2-(4,b-dihydro-3-soxazoD 0F A-1635 H H H H GH 20H 20H 3 H 2-N 0 A-1636 H H H H D GH 20H 20H 3 H 2-NO 2 0
A-1637 H H H H i GH 20H 20H 3 H 2-F,6-GI 0 A-1638 H H H H D 0 H2CH2CH3 H 2-F,6-M e 0 A-1639 H H H H 0 0H 2CH 2CH 3 H 3-F,6-M e 0 A-1640 H H H H 0 0H 2CH 2CH 3 H 4-F,2-M e 0 A-1641 H H H H f0 GH 20H 20H 3 H 2-F,6-UM e A-1642 H H H H 0 0H 2CH 2CH 3 H 3-F,6-0M e A-1643 H H H H Hi0 GH 20H 20H 3 H 2,6-C 0 A-1644 H H H H GH 20H 20H 3 H 2-G 1,6-M e 0 A-1645 H H H H 0 0H 2CH 2CH 3 H 3-01,6-M e 0 A-1646 H H H H f0 0H 2CH 2CH 3 H 4-01,2-M e 0 A-1647 H H H H H0f GH 20H 20H 3 H 2-Cb-CF 3 0 A-1648 H H H H H 0 H 20H 20H 3 H 2-G,6-0F 3 0
[0155]
[Table 30]
com pound R' R2 R R A R R' (R)m p A-1649 i H H H H 0 0H2CH2CH3 H 2-C ,6-0M e 0 A-1650 H H H H 0 H 2 CH 2CH 3 H 3-C 1,6-0M e F A-1651 H H H H 0 H 2CH 2CH 3 H 4-C 1,2-0M e F A-1652 H H H H i 0 GH 20H 20H 3 H 2,4-M e 2 0 A-1653 H H H H D 0H2CH2CH3 H 2,b-ie2 0 A-1654 H H H H 0 0H 2 CH 2CH 3 H 2,6-M e 2 0 A-1655 H H H H D 0H 2 CH 2CH 3 H 2-M e,4-CF 3 0 A-1656 H H H H D 0H 2 CH 2CH 3 H 2-M e,b-CF 3 0 A-1657 H H H H H 0 0H 2 CH 2CH 3 H 2-M e,6-CF 3 0 A-1658 H H H H D 0 GH20H20H 3 H 2-M e,4-0M e A-1659 H H H H i 0 GH 20H 20H 3 H 2-M e,b-OM e A-1660 H H H H D GH 2 0H 20H 3 H 2-M e,6-OM e 0 A-1661 H H H H GH 2 0H 20H 3 H 3-M e,6-OM e 0 A-1662 H H H H 0 0H 2 CH 2CH 3 H 4-M e,2-OM e 0 A-1663 H H H H 0 0H 2 CH 2CH 3 H 2,b-M e 2 0 A-1664 H H H H H GH 20H 20H 3 H 2,6-0M e 2 A-1665 H H H H GH 20H 20H 3 H 2-UM e,6-GH 3 0 A-1666 H H H H 0 0H 2CH 2CH 3 H 2-CH ' 2,b-F 0 A-1667 H H H H iif GH20H20H 3 H 2-CH 2,6- 0 A-1668 H H H H 0 0H 2CH 2CH 3 H 2-CH F 2,b-M e 0 A-1669 H H H H H 0 H 2CH 2CH 3 H 2-CH F 2,6-M e 0 A-1670 H H H H H 0 H 2CH 2CH 3 H 2-cycobpropy 1,b-F 0 A-1671 H H H H D 0 H2CH2CH3 H 2-cycobpropy 1,6-F 0 A-1672 H H H H H 0 H 2CH 2CH 3 H 2-cyclopropylb-M e 0 A-1673 H H H H 0G 20H 2 H 3 H 2-cyclopropyl,6-M e 0 A-1674 H H H H f0 GH 2 0H 20 3 H 2-ethenyl,6-F 0 A-1675 H H H H GH 20H 20H 3 H 2-ethenyl,6-M e 0 A-1676 H H H H i 0 0H 2CH 2CH 3 H 2-0Etb-F 0 A-1677 H H H H 0 0H 2CH 2CH 3 H 2-OEt6-F 0 A-1678 H H H H 0 0H 2CH 2CH 3 H 2-0Etb-CI 0 A-1679 H H H H 0 0H 2CH 2CH 3 H 2-OEt6-C I 0 A-1680 H H H H 0 0H 2CH 2CH 3 H 2-0Etb--M e 0 A-1681 H H H H H 0 0H 2 CH 2CH 3 H 2-OEt6-M e 0 A-1682 H H H H f0 GH 2 0H 20H 3 H 2-0CH H2,b-F 0
A-1683 H H H H 0 0H 2 CH 2CH 3 H 2-0CH F 2,6-F 0 A-1684 H H H H D CH 2CH 2CH 3 H 2-OCH F2 ,b-M e A-1685 H H H H f0 CH 2CH 2CH 3 H 2-OCH H2 ,6-M e 0 A-1686 H H H H 0 0H 2CH 2CH 3 H 2-(cycbpropyloxy),b-F W A-1687 H H H H 0 H 2CH 2CH 3 H 2-(cycbpropyloxy),6-F 0 A-1688 H H H H H 0 CH 2CH 2CH3 H 2-(cyclopropy bxy),b-M e 0 A-1689 H H H H 0 0H 2CH 2CH 3 H 2-(cyclopropy bxy),6-M e 0 A-1690 H H H H 0 0H 2CH 2CH 3 H 2-SM e,b-F 0 A-1691 H H H H CH 2CH 2CH 3 H 2-SM e,6-F 0 A-1692 H H H H CH 2CH 2CH 3 H 2-SM e,b-M e 0 A-1693 H H H H f Di CH 2CH 2CH 3 H 2-SM e,6-M e 0 A-1694 H H H H H CH 2CH 2CH 3 H 2-S =0 )M e,b-F 0 A-1695 H H H H 0 0H 2CH 2CH 3 H 2-S(=0)M e,6-F 0 A-1696 H H H H H 0 0H 2CH 2CH 3 H 2-S(=0)Me,b-M e 0 A-1697 H H H H 0 0H 2CH 2CH 3 H 2-S(= 0)Me,6-M e 0 A-1698 H H H H f0 CH 2CH 2CH 3 H 2-S =) 2 Me,b-F A-1699 H H H H D0 H 2CH2CH3 H 2-S(= 0)e,6-F 2M F A-1700 H H H H 0 CH 2CH 2CH 3 H 2-S = ) 2 Me,b-M e 0 A-1/l H H H H F CH 2CH 2CH 3 H 2-S = ) 2 Me,6--M e 0 A-1702 H H H H 0 0H 2CH CH 3 2 H 2-SCF3,b-F 0 A-1703 H H H H Hi0 0H 2CH CH 3 2 H 2-SCF 3 ,6-F 0 A-1704 H H H H H GH 2 ;H 2 ;H 3 H 2-SCF 3 ,b-M e 0 A-170b H H H H f 0H 20H 20H 3 H 2-SCF 3 ,6-M e 0
[0156]
[Table3 1]
cornpound RI R2 R A R6Rt Wm p A-17 06 if H if H if 0 0H 20H 2 0H3 H 2-S (=0)0F 3,b-F 0 A-1707 HfH ifH if0 0H 20H 2 0H 3 H 2-S (=0)0F3 ,6-F0 A-l708 ifH Hif if0 0H 20H 2 0H 3 H 2-S (=0)F3 ,-vleW A-1709 if H if H if 0 0H 20H 2 0H 3 H 2-S (=O)F 3 ,6-vle 0 A -1l 71f0 H ifH Hif0 CH 20H 2 0H 3 H 2-S=0 )20F 3,b-F 0 A -ll 71f1 H ifHiHif0 CH 20H 2 0H 3 H 2-S=0 ) 20F 3,6-F 0 A-1712 ifIHifIHif-0 0H 20H 20H 3 H 2-S=0 )2 F3,-vle 0 A-1713 ifH HfH Hf0 0H 20H 20H 3 H 2-S=0 )2 F3,6-vle 0 A-1714 if H if H if 0 0H 20H 2 0H 3 H 2-(oy opropylIthbi),b-F 0 A-ill5 if H if H if 0F H 20H 20H 3 H 2-(oy opropylIthbi),6-F 0 A-171 6 if H if H if 0 0H 20H 20H 3 H 2-(oy opropy th io),b-vle 0 A-ill] if H if H if 0 H 20H 2 0H 3 H 2-(oy opropy th io),6-vle 0 A-ibi8 ifiHifiHif0 H 20H 20H 3 H 2-C0A)e,5-F 0 A-171 9 ifH HfH if0 0H 20H 20H 3 H 2-C0A)e,6-F 0 A-1720 ifH HfH if0 0H 20H 20H 3 H 2-0(=0)M e,-ve 0 A-1721 if H if iF if 0 0H 20H 20H 3 H 2-0(=0)M e,6-vle 0 A-1722 HiH HiH FF 0HI 20H 20H 3 H 2-CH 2 UH b-F 0 A-1723 HfH ifH if0 0H 20H 20H 3 H 2-OH 2 0H,6-F 0 A-1724 ifi Hifi -CFi0 H20H 20H 3 H 2-CH 2 0H 5-M e 0 A-1725 ifI HfI Hf0 0H 20H 20H 3 H 2-0H 20 H6-Mve 0 A-1b726 HfH HfH Hf0 0H 20H 20H 3 H 2-OH 20CH 3,4-F 0 A-1l727 HfH HfH Hf0 0H 20H 20H 3 H 2-OH 20CH 3,S-F 0 A-1728 HfH ifH if0 0H 20H 20H 3 H 2-OH 20CH 3,6-F 0 A-1729 ifi ifi if0 0H 20H 20H 3 H 2-OH 200H 3 ,4-vle 0 A-1b730 ifi ifi if0 H2 H 20H 3 H 2 C 3 b-ie 0 A-1731 ifi ifi if0 H20H 20H 3 H 2 C 3 6-ie 0 A-1732 HfH HfH Hf0 0H 20H 20H 3 H 2-0 C(0)C0H 3 ,b-F 0 A-1733 H H if H if 0 0H 2 0H 20H 3 H 2-0 C=0 )C0H 3 ,6-F 0 A-1734 ifH ifi if0 0H 2 0H 20H 3 H 2-0 C(0 )H 3,-Mvle 0 A-1735 ifI HfI if0 0H 2 0H 20H 3 H 2-OC(=0 )H 3,6-Mvle 0 A-11736 HfH HfH if0 0H 20H 20H 3 H 2-OS=0 )20H 3,b-F 0 A-11737 HfI HfI if0 0H 20H 20H 3 H 2-OS=0 )20H 3,6-F 0 A-1738 ifH ifH if0 0H 20H 20H 3 H 2-0 S=0 )2 H 3,-vle 0 A-1739 ifH ifH if0 0H 20H 20H 3 H 2-0 S(=O) 2 CH 3,6-M e 0 A-1740 HfH HfH if0 0H 20H 20H 3 H 2-OH 2 SCH 3,S-F 0 A-11741 HfiHiHiHiH CH 2CH 2CH 3 H 2-CH 2 SCH 3,6-F 0 A-1742 ifiHifiHif0 H20H 20H 3 H 2-CH 2SCH 3,5-M e 0 A-1743 ifi ifi if0 0H 20H 20H 3 H 2-OH 2 SCH 3,6-MvleW A-1744 ifI HfI if0 0H 2 0H 20H 3 H 2-NM e2,S-F 0 A-1745 H H H H H 0 0H 2 0H 20H 3 H 2-NM e 2 ,6-F 0 A-1746 HfI HfI if0 0H 2 0H 20H 3 H 2-NM e2 S-ve 0 A-1747 ifi ifi if0 0H 2 0H 2 0H 3 H 2-NM e2 ,6-vle 0 A-1748 HfH HfH Hf0 0H 2 0H 20H 3 H 2-ON,4-F 0 A-1749 HiH ifHif0 0H 2 0H 20H 3 H 2-ON,S-F 0 A-175O HfH ifH ifW H2 H2 CH,3 H 2-ON,6-F 0 A-1751 ifi ifi if0 0H 2 0H 20H 3 - H 2-ON 6-Mvie 0 A-1752 ifI HfI if0 0H 2 0H 20H 3 H 2-ON 5-OM e 0 A-1753 ifH HfH HfW 0H 20H 20H 3 H 2-ON,6-OM e 0 A-1754 ifH HfH if0 0H 2 0H 20H 3 H 3-ON 6-Mvie 0 A-1755 ifH ifH if0 0H 2 0H 20H 3 H 3-ON,6-OM e 0 A-1b756 ifi ifi if0 0H 2 0H 20H 3 H 4-ON 2-Mve 0 A-l~ if7iH ifHiHif0 CH 20H 2 0H 3 H 4-ON,2-OM e 0 A-1758 HiH HiH Hif0 0H 20H 2 0H 3 H 2-AN0 2 14-F 0 A-1759 HfH ifH Hf0 0H 2 0H 20H 3 H 2-N 02 ,S-F 0 A-1b760 HfH HfH Hf0 0H 2 0H 20H 3 H 2-N 0 2 ,6-F 0 A-1761 ifi Hifi H if0 0H 2H3 H 2 A O2A4-A e 0 A-1762 ifi ifi if0 CH 20;H 20;H 3 H 2-N 02,S-vle 0
[0157]
[Table 32]
com pound RI R2 R R R A R R' (R)m P A-1763 i H H H H H 0 CH2CH2CH, H 2-N02,6-Me 0 A-1764 H H H H H 0 CH 2CH 2CH, H 2-M e,4,5-F2 0 A-1765 H H H H H 0 CH 2CH 2CH, H 2-M e,6-Et 0 A-1766 H H H H H 0 0H 20H 20H 3 H 2-cyclopropyl,6-OM e 0 A-1767 H H H H H 0 CH 2CH 2CH, H 2-M e,5-Et 0 A-1768 H H H H H 0 CH 2CH 2CH, H 2,6-Et 2 0 A-1769 H H H H H 0 CH 2CH 2CH, H 2-Et,6-F 0 A-1770 H H H H H 0 CH 2CH 2CH, H 2-CH 20CH ,6-Cl 0 A-1771 H H H H H 0 CH 2CH 2CH, H 2-CH 20CH 2 CH ,6-C| 0 A-1772 H H H H H 0 H 2CH 2CH 3 H 2-CH 2 NM e2 A-1773 H H H H H 0 cycobpropy H H 0 A-1774 H H H H H 0 cycobpropy H 2-F 0 A-1775 H H H H H 0 cycobpropy H 2-Cl 0 A-1776 H H H H H 0 cycobpropy H 2-Br 0 A-1777 H H H H H 0 cycobpropyl H 2-OH 0 A-1778 H H H H H 0 cycobpropyl H 2-M e 0 A-1779 H H H H H 0 cycbpropyl H 2-Et 0 A-1780 H H H H H 0 cycbpropyl H 2-Pr 0 A-1781 H H H H H 0 cycbpropyl H 2-GF 3 0 A-1782 H H H H H 0 cycbpropyl H 2-CH F 2 0 A-1783 H H H H H 0 cycbpropyl H 2-CH 2F 0 A-1784 H H H H H 0 cycbpropyl H 2-CF 2C1 0 A-1785 H H H H H 0 cycbpropyl H 2-cycbpropy 1 0 A-1786 H H H H H 0 cycbpropyl H 2-cycobbutyl 0 A-1787 H H H H H 0 cycbpropyl H 2-cycbpenty 1 0 A-1788 H H H H H 0 cycbpropyl H 2-etheny 1 0 A-1789 H H H H H 0 cycbpropyl H 2-a llyl 0 A-1790 H H H H H 0 cycobpropyl H 2-(prop-1-en-1-y D 0 A-1791 H H H H H 0 cycobpropyl H 2-(trifforoetheny D 0 A-1792 H H H H H 0 cycbpropyl H 2-0M e 0 A-1793 H H H H H 0 cycbpropyl H 2-0Et 0 A-1794 H H H H H 0 cycbpropyl H 2-0Pr 0 A-1795 H H H H H 0 cycbpropyl H 2-0 (/-Pr) 0 A-1796 H H H H H 0 cycbpropyl H 2-00G 0 A-1797 H H H H H 0 cycbpropyl H 2-0CH F 2 0 A-1798 H H H H H 0 cycbpropyl H 2-(cycbpropy bxy) 0 A-1799 H H H H H 0 cycbpropyl H 2-(cycobbuty loxy) 0 A-1800 H H H H H 0 cycbpropyl H 2-(cycbpenty bxy) 0 A-1801 H H H H H 0 cycbpropyl H 2-((2,2-d ih brocycbpropy Doxy) 0 A-1802 H H H H H 0 cycbpropyl H 2-(oxiran-2-y D 0 A-1803 H H H H H 0 cycbpropyl H 2-SM e 0 A-1804 H H H H H 0 cycbpropyl H 3-SM e 0 A-1805 H H H H H 0 cycbpropyl H 2-S (=0)M e 0 A-1806 H H H H H 0 cycbpropyl H 3-S (=0)M e 0 A-1807 H H H H H 0 cycbpropyl H 2-S (=0)2 Me 0 A-1808 H H H H H 0 cycbpropyl H 3-S(=0) 2M e 0 A-1809 H H H H H 0 cycbpropyl H 2-SCF3 0 A-1810 H H H H H 0 cycbpropyl H 3-SCF 3 0 A-1811 H H H H H 0 cycbpropyl H 3-S (=0)CF3 0 A-1812 H H H H H 0 cycbpropyl H 3-SCF(CF 3 ) 2 0 A-1813 H H H H H 0 cycbpropyl H 2-(cycbpropy th b) 0 A-1814 H H H H H 0 cycbpropyl H 2-(cycbpropy Isu finyD 0 A-1815 H H H H H 0 cycbpropyl H 2-(cycbpropy u fonyD 0 A-1816 H H H H H 0 cycbpropy H 2-C (=0)M e 0 A-1817IH H H H H 0 cycbpropy H 2-CH 2C(=0)CH3 0 A-1818 H H H H H 0 cycbpropyl H 2-0H 20(= 0)G 3 0 A-1819 HH H H H 0 cycbpropy H 2-CH20H 0
[0158]
[Table 33]
com pound RI R2 R R R A R R' (R)m P A-1820 H H H H H 0 cycbpropyl H 2-CH 2 0CH3 0 A-1821 H H H H H 0 cycbpropyl H 2-CH 2 0CH 2 CH3 0 A-1822 H H H H H 0 cycbpropyl H 2-CH 2SCH3 0 A-1823 H H H H H 0 cycbpropyl H 2-CH 2S (= 0CH, 0 A-1824 H H H H H 0 cycbpropyl H 2-CH 2S(= 0) 2 CH 0 A-1825 H H H H H 0 cycbpropyl H 2-(benzy bxy) 0 A-1826 H H H H H 0 cycbpropyl H 2-NH 2 0 A-1827 H H H H H 0 cycbpropyl H 2-NH M e 0 A-1828 H H H H H 0 cycbpropyl H 2-N ( e)2 0 A-1829 H H H H H 0 cycbpropyl H 2-(1,3-d bxo an-2-y D 0 A-1830 H H H H H 0 cycbpropyl H 2-(1,3-d bxan-2-yl 0 A-1831 H H H H H 0 cycbpropy H 2-(1H-im dazokE2-yD 0 A-1832 H H H H H 0 cycbpropyl H 2-(thiazo -2-yl) 0 A-1833 H H H H H 0 cycbpropyl H 2-(oxazol1-2-y D 0 A-1834 H H H H H 0 cycbpropy H 2-CH= N0H 0 A-1835 H H H H H 0 cycbpropy H 2-CH= NOM e 0 A-1836 H H H H H 0 cycbpropy H 2-(4,5-d ihydro-3-oxazo ly D 0 A-1837 H H H H H 0 cycbpropy H 2-CN 0 A-1838 H H H H H 0 cycbpropy H 2-NO 2 0 A-1839 H H H H H 0 cycobpropy H 2-F,6-O 1 0 A-1840 H H H H H 0 cycobpropy H 2-F,6-M e 0 A-1841 H H H H H 0 cycbpropy H 3-F,6-M e 0 A-1842 H H H H H 0 cycbpropy H 4-F,2-M e 0 A-1843 H H H H H 0 cycbpropy H 2-F,6-0M e 0 A-1844 H H H H H 0 cycbpropy H 3-F,6-0M e 0 A-1845 H H H H H 0 cycbpropy H 2,6-Cl 0 A-1846 H H H H H 0 cycbpropy H 2-C 1,6-M e 0 A-1847 H H H H H 0 cycbpropy H 3-C 1,6-M e 0 A-1848 H H H H H 0 cycbpropy H 4-C 1,2-M e 0 A-1849 H H H H H 0 cycbpropy H 2-C 1,5-CF, 0 A-1850 H H H H H 0 cycbpropy H 2-C 1,6-CF, 0 A-1851 H H H H H 0 cycbpropy H 2-C 1,6-0M e 0 A-1852 H H H H H 0 cycbpropy H 3-C 1,6-0M e 0 A-1853 H H H H H 0 cycbpropy H 4-C 1,2-0 M e 0 A-1854 H H H H H 0 cycbpropy H 2,4-M e 2 0 A-1855 H H H H H 0 cycbpropyl H 2,b-M e 2 0 A-1856 H H H H H 0 cycbpropyl H 2,6-M e2 0 A-1857 H H H H H 0 cycbpropyl H 2-M e,4-CF 3 0 A-1858 H H H H H 0 cycbpropyl H 2-M e,b-CF 3 0 A-1859 H H H H H 0 cycobpropy H 2-M e,6-CF 3 0 A-1860 H H H H H 0 cycobpropyl H 2-M e,4-0M e 0 A-1861 H H H H H 0 cycobpropyl H 2-M e,5-0M e 0 A-1862 H H H H H 0 cycobpropyl H 2-M e,6-0M e 0 A-1863 H H H H H 0 cycobpropyl H 3-M e,6-0M e 0 A-1864 H H H H H 0 cycobpropyl H 4-M e,2-0M e 0 A-1865 H H H H H 0 cycobpropy H 2,b-OMe 2 0 A-1866 H H H H H 0 cycobpropy H 2,6-0M e 2 0 A-1867 H H H H H 0 cycobpropy H 2-OM e,6-CF3 0 A-1868 H H H H H 0 cycobpropy H 2-CH F2,b-F 0 A-1869 H H H H H 0 cycbpropyl H 2-CH F 2,6-F 0 A-1870 H H H H H 0 cycbpropyl H 2-CH F 2,b-i e 0 A-1871 H H H H H 0 cycbpropyl H 2-CH F2,6 Ae 0 A-1872 H H H H H 0 cycbpropyl H 2-cycbpropy lb-F 0 A-1873 H H H H H 0 cycbpropyl H 2-cycbpropy 1,6-F 0 A-1874 H H H H H 0 cycbpropyl H 2-cyclopropyL,5-M e 0 A-1875 H H H H H 0 cycbpropyl H 2-cyclopropyL,6-M e 0 A-1876 H H H H H 0 cycbpropyl H 2-ethenyL,6-F 0
[0159]
[Table 34]
com pound RI R2 R R R A R R' (R)m P A-187 H H H H H 0 cycbpropyl H 2-ethenyl,6-M e 0 A-1878 H H H H H 0 cycbpropyl H 2-0Et,5-F 0 A-1879 H H H H H 0 cycbpropyl H 2-0Et,6-F 0 A-1880 H H H H H 0 cycbpropyl H 2-0Et,5-CI 0 A-1881 H H H H H 0 cycbpropyl H 2-0Et,6-CI 0 A-1882 H H H H H 0 cycbpropyl H 2-0Et,5-Me 0 A-1883 H H H H H 0 cycbpropyl H 2-0Et,6-M e 0 A-1884 H H H H H 0 cycbpropyl H 2-0CHF 2,5-F 0 A-1885 H H H H H 0 cycbpropyl H 2-0CHF 2,6-F 0 A-1886 H H H H H 0 cycbpropyl H 2-0CHF 2,b-MAe 0 A-1887 H H H H H 0 cycbpropyl H 2-0CHF 2 ,6-MAe 0 A-1888 H H H H H 0 cycbpropyl H 2-(cycbpropyloxy),5-F 0 A-1889 H H H H H 0 cycbpropyl H 2-(cycbpropyloxy),6-F 0 A-1890 H H H H H 0 cycbpropyl H 2-(cyclopropybxy),5-M e 0 A-1891 H H H H H 0 cycbpropyl H 2-(cyclopropybxy),6-M e 0 A-1892 H H H H H 0 cycbpropyl H 2-SMe,5-F 0 A-1893 H H H H H 0 cycbpropyl H 2-SMe,6-F 0 A-1894 H H H H H 0 cycbpropyl H 2-SMe,5-M e 0 A-1895 H H H H H 0 cycbpropyl H 2-SMe,6-M e 0 A-1896 H H H H H 0 cycbpropyl H 2-S(=0)Me,5-F 0 A-1897 H H H H H 0 cycbpropyl H 2-S (0)M e,6-F 0 A-1898 H H H H H 0 cycbpropyl H 2-S(=0)Me,5-M e 0 A-1899 H H H H H 0 cycbpropyl H 2-S(=0)Me,6-M e 0 A-1900 H H H H H 0 cycbpropyl H 2-S(=0)2 Me,5-F 0 A-1901 H H H H H 0 cycbpropyl H 2-S(=0)2 Me,6-F 0 A-1902 H H H H H 0 cycbpropyl H 2-S(=0) 2Me,b-Me 0 A-1903 H H H H H 0 cycbpropyl H 2-S(=0) 2Me,6-Me 0 A-1904 H H H H H 0 cycbpropyl H 2-SCF,,5-F 0 A-1905 H H H H H 0 cycbpropyl H 2-SCF,6-F 0 A-1906 H H H H H 0 cycbpropyl H 2-SCF3 ,b-M e 0 A-1907 H H H H H 0 cycbpropyl H 2-SCF,6-M e 0 A-1908 H H H H H 0 cycbpropyl H 2-S (=0)CF3 ,5-F 0 A-1909 H H H H H 0 cycbpropyl H 2-S (=0)CF3 ,6-F 0 A-1910 H H H H H 0 cycbpropyl H 2-S(=0)CF 3 ,b-Me 0 A-1911 H H H H H 0 cycbpropyl H 2-S(=0)CF,6-Me 0 A-1912 H H H H H 0 cycbpropyl H 2-S(=0) 20F3 ,b-F 0 A-1913 H H H H H 0 cycbpropyl H 2-S(=0) 20F 3 ,6-F 0 A-1914 H H H H H 0 cycbpropyl H 2-S(=0) 2 CF 3 ,b-M e 0 A-1915 H H H H H 0 cycbpropyl H 2-S(=0) 2 CF3 ,6-Me 0 A-1916 H H H H H 0 cycbpropyl H 2-(cycobpropylthb),5-F 0 A-1917 H H H H H 0 cycbpropyl H 2-(cycobpropylthb),6-F 0 A-1918 H H H H H 0 cycbpropyl H 2-(cycobpropylthio),5-M e 0 A-1919 H H H H H 0 cycbpropyl H 2-(cycobpropylthio),6-M e 0 A-1920 H H H H H 0 cycbpropyl H 2-C(=0)Me,5-F 0 A-1921 H H H H H 0 cycbpropyl H 2-C (=0)M e,6-F 0 A-1922 H H H H H 0 cycbpropyl H 2-C(=0)Me,5-M e 0 A-1923 H H H H H 0 cycbpropyl H 2-C(=0)Me,6-M e 0 A-1924 H H H H H 0 cycbpropyl H 2-CH 20H,5-F 0 A-1925 H H H H H 0 cycbpropyl H 2-CH 20H,6-F 0 A-1926 H H H H H 0 cycbpropyl H 2-CH 20H,b5e 0 A-1927 H H H H H 0 cycobpropyl H 2-CH 20H,6-M e 0 A-1928 H H H H H 0 cycobpropyl H 2-3H 200H3 ,4-F 0 A-1929 H H H H H 0 cycobpropyl H 2-3H 200H3 ,b-F 0 A-1930 H H H H H 0 cycobpropy H 2-CH 20CH 3 ,6-F 0 A-1931 H H H H H 0 cycobpropyl H 2-CH 20CH,4-M e 0 A-1932 H H H H H 0 cycobpropyl H 2-CH 200H,b-M e 0 A-1933 H H fH H H 0 cycbpropyl H 2-CH 20CHA,6-Me 0
[0160]
[Table 35]
com pound RI R2 R A R R R R' (R)m P A-1934f H H H 0 H H cycbpropyl H 2-OC (=O)CH,5-F 0 A-1935 H H H 0 H H cycbpropyl H 2-OC (=O)CH,6-F 0 A-1936 H H H 0 H H cycbpropyl H 2-0C (=0)CH 3 ,5-Me A-1937 H H H 0 H H cycbpropyl H 2-0C(= 0)H3 ,6-M e 0 A-1938 H H H 0 H H cycbpropyl H 2-OS (= )2CH3 ,5-F 0 A-1939 H H H 0 H H cycbpropyl H 2-OS (= ) 2CH3 ,6-F 0 A-1940 H H H H H 0 cycbpropyl H 2-OS (= ) 2CH 3 ,5-M e 0 A-1941 H H H H H 0 cycbpropyl H 2-OS (= ) 2CH 3 ,6-M e 0 A-1942 H H H H H 0 cycbpropyl H 2-CH 2 SCH 3 ,5-F 0 A-1943 H H H H H 0 cycbpropyl H 2-CH 2 S0H ,6-F 0 A-1944 H H H H H 0 cycbpropyl H 2-CH 2SCH 3,b-M e 0 A-1945 H H H H H 0 cycbpropyl H 2-CH 2SCH 3,6-Me A-1946 H H H H H 0 cycbpropyl H 2-NM e 2 ,5-F 0 A-1947 H H H H H 0 cycbpropyl H 2-NM e 2 ,6-F 0 A-1948 H H H H H 0 cycbpropyl H 2-AM e 2 ,5-M e 0 A-1949 H H H H H 0 cycbpropyl H 2-NM e 2 ,6-M e 0 A-1950 H H H H H 0 cycbpropyl H 2-CN,4-F 0 A-1951 H H H H H 0 cycbpropyl H 2-CN,5-F 0 A-1952 H H H H H 0 cycbpropyl H 2-CN,6-F 0 A-1953 H H H H H 0 cycbpropyl H 2-CN,6-M e 0 A-1954 H H H H H 0 cycbpropyl H 2-CN,5-OM e 0 A-1955 H H H H H 0 cycbpropyl H 2-CN,6-OM e 0 A-1956 H H H H H 0 cycbpropyl H 3-CN,6-M e 0 A-1957 H H H H H 0 cycbpropyl H 3-CN,6-OM e 0 A-1958 H H H H H 0 cycbpropyl H 4-CN 2-M e 0 A-1959 H H H H H 0 cycbpropyl H 4-CN,2-OM e 0 A-1960 H H H H H 0 cycbpropyl H 2-N0 2 ,4-F 0 A-1961 H H H H H 0 cycbpropyl H 2-N0 2 ,5-F 0 A-1962 H H H H H 0 cycbpropyl H 2-N0 2 ,6-F 0 A-1963 H H H H H 0 cycbpropyl H 2-A0 2,4-M e 0 A-1964 H H H H H 0 cycbpropyl H 2-A0 2,5-M e 0 A-1965 H H H H H 0 cycbpropyl H 2-N0 2,6--M e 0 A-1966 H H H H H 0 cycbpropyl H 2-M e,4,5-F2 0 A-1967 H H H H H 0 cycbpropyl H 2-M e,6-Et 0 A-1968 H H H H H 0 cycbpropyl H 2-cyclopropyl,6-OM e 0 A-1969 H H H H H 0 cycbpropyl H 2-M e,5-Et 0 A-1970 H H H H H 0 cycbpropyl H 2,6-Et2 0 A-1971 H H H H H 0 cycbpropyl H 2-Et,6-F 0 A-1972 H H H H H 0 cycbpropyl H 2-CH 20CH 3 ,6-C I 0 A-1973 H H H H H 0 cycbpropyl H 2-CH 20CH 2CH 3 ,6-C| 0 A-1974 H H H H H 0 cycbpropyl H 2-CH 2 NM e 2 0 A-1975 H H H H H 0 cycbhexyl H H 0 A-1976 H H H H H 0 cycbhexyl H 2-F 0 A-1977 H H H H H 0 cycbhexyl H 2-C1 0 A-1978 H H H H H 0 cycbhexyl H 2-Br 0 A-1979 H H H H H 0 cycbhexyl H 2-OH 0 A-1980 H H H H H 0 cycbhexyl H 2-M e 0 A-1981 H H H H H 0 cycbhexyl H 2-Et 0 A-1982 H H H H H 0 cycbhexyl H 2-Pr 0 A-1983 H H H H H 0 cycbhexyl H 2-GO 3 0 A-1984 H H H H H 0 cycbhexyl H 2-CH F 2 0 A-1985 H H H H H 0 cycbhexyl H 2-CHf 0 A-1986 H H H H H 0 cycbhexyl H 2-OF 2CI 0 A-1987 H H H H H 0 cyobhexyl H 2-cycbpropy 1 0 A-1988 H H H H H 0 cycbhexyl H 2-cycobbutyl 0 A-1989 H H H H H 0 cyobhexyl H 2-cycbpentyl 0 A-1990 H H IHIH H0 cycbhexyl H 2-ethenyl 0
[0161]
[Table 36]
com pound RI R2 R R R A R R' (R)m P A-1991 H H H H H 0 cycbhexyl H 2-allyl 0 A-1992 H H H H H 0 cycbhexyl H 2-(prop-1-en-1-yl 0 A-1993 H H H H H 0 cycbhexyl H 2-(trifforoethenyD A-1994 H H H H H 0 cycbhexyl H 2-0M e 0 A-1995 H H H H H 0 cycbhexyl H 2-0Et 0 A-1996 H H H H H 0 cycbhexyl H 2-0Pr 0 A-1997 H H H H H 0 cycbhexyl H 2-0(/-Pr) 0 A-1998 H H H H H 0 cycbhexyl H 2-0CF, 0 A-1999 H H H H H 0 cycbhexyl H 2-0CH F 2 0 A-2000 H H H H H 0 cycbhexyl H 2-(cycbpropy bxy) 0 A-2001 H H H H H 0 cycbhexyl H 2-(cycobbutybxy) 0 A-2002 H H H H H 0 cycbhexyl H 2-(cycbpentybxy) 0 A-2003 H H H H H 0 cycbhexyl H 2-((2,2-dichbrocycbpropy)oxy) 0 A-2004 H H H H H 0 cycbhexyl H 2-(oxiran-2-yD 0 A-2005 H H H H H 0 cycbhexyl H 2-SMe 0 A-2006 H H H H H 0 cycbhexyl H 3-SMe 0 A-2007 H H H H H 0 cycbhexyl H 2-S(=0)Me 0 A-2008 H H H H H 0 cycbhexyl H 3-S(0)Me 0 A-2009 H H H H H 0 cycbhexyl H 2-S(=0)Me 0 A-2010 H H H H H 0 cycbhexyl H 3-S(=0) 2Me 0 A-2011 H H H H H 0 cycbhexyl H 2-SCF, 0 A-2012 H H H H H 0 cycbhexyl H 3-SCF, 0 A-2013 H H H H H 0 cycbhexyl H 3-S(=0)CF, 0 A-2014 H H H H H 0 cycbhexyl H 3-SCF(CFI) 2 0 A-2015 H H H H H 0 cycbhexyl H 2-(cycbpropythio) 0 A-2016 H H H H H 0 cycbhexyl H 2-(cycbpropylsulfinyD 0 A-2017 H H H H H 0 cycbhexyl H 2-(cycbpropylsulfonyl 0 A-2018 H H H H H 0 cycbhexyl H 2-C(=0)Me 0 A-2019 H H H H H 0 cycbhexyl H 2-CH 2C(=0)CH3 0 A-2020 H H H H H 0 cycbhexyl H 2-CH 2C(=0)CF 0 A-2021 H H H H H 0 cycbhexyl H 2-CH 2 0H 0 A-2022 H H H H H 0 cycbhexyl H 2-CH 2 0CH 3 0 A-2023 H H H H H 0 cycbhexyl H 2-CH 2 0CH 2CH 3 0 A-2024 H H H H H 0 cycbhexyl H 2-CH 2SCH 3 0 A-2025 H H H H H 0 cycbhexyl H 2-CH 2S(=0)CH 3 0 A-2026 H H H H H 0 cycbhexyl H 2-CH 2S(=0)2CH 3 0 A-2027 H H H H H 0 cycbhexyl H 2-(benzybxy) 0 A-2028 H H H H H 0 cycbhexyl H 2-NH 2 0 A-2029 H H H H H 0 cycbhexyl H 2-NH M e 0 A-2030 H H H H H 0 cycbhexyl H 2-N (Me2 0 A-2031 H H H H H 0 cycbhexyl H 2-(1,3-dioxolan-2-yD 0 A-2032 H H H H H 0 cycbhexyl H 2-(1,3-dioxan-2-yD 0 A-2033 H H H H H 0 cycbhexyl H 2-(1H--m idazol-2-yD 0 A-2034 H H H H H 0 cycbhexyl H 2-(thiazol-2-y) 0 A-2035 H H H H H 0 cycbhexyl H 2-(oxazo-2-yID 0 A-2036 H H H H H 0 cycbhexyl H 2-CH=N0H 0 A-2037 H H H H H 0 cycbhexyl H 2-CH= NOM e 0 A-2038 H H H H H 0 cycbhexyl H 2-(4,5-dihydro-3-isoxazolyD 0 A-2039 H H H H H 0 cycbhexyl H 2-CN 0 A-2040 H H H H H 0 cycbhexyl H 2-N0 2 0 A-2041 H H H H H 0 cycbhexyl H 2-F,6-CI 0 A-2042 H H H H H 0 cycbhexyl H 2-F,6-Me 0 A-2043 H H H H H 0 cycbhexyl H 3-F,6-Me 0 A-2044 H H H H H 0 cycbhexyl H 4-F,2-Me 0 A-2045 H H H H H 0 cycbhexyl H 2-F,6-OMe 0 A-2046 H H HIH H 0 cycbhexyl H 3-F,6-OMe 0 A-2047 i fHH H H 0 cycbhexyl H 2,6-Cl 0
[0162]
[Table 37]
com pound RI R2 R R R A R R' (R)m P A-2048 Hif8- H H H H 0 cycbhexyl H 2-CI,6-Me 0 A-2049 H H H H H 0 cycbhexyl H 3-CI,6-Me 0 A-2050 H H H H H 0 cycbhexyl H 4-CI,2-Me A-2051 H H H H H 0 cycbhexyl H 2-CIb-CF, 0 A-2052 H H H H H 0 cycbhexyl H 2-C1,6-CF, 0 A-2053 H H H H H 0 cycbhexyl H 2-C1,6-0Me 0 A-2054 H H H H H 0 cycbhexyl H 3-C1,6-0Me 0 A-2055 H H H H H 0 cycbhexyl H 4-CI,2-0Me 0 A-2056 H H H H H 0 cycbhexyl H 2,4-M e 2 0 A-2057 H H H H H 0 cycbhexyl H 2,b-M e 2 0 A-2058 H H H H H 0 cycbhexyl H 2,6-M e 2 0 A-2059 H H H H H 0 cycbhexyl H 2-M e,4-CF 3 0 A-2060 H H H H H 0 cycbhexyl H 2-M e,b-CF 3 0 A-2061 H H H H H 0 cycbhexyl H 2-Me,6-CF3 0 A-2062 H H H H H 0 cycbhexyl H 2-Me,4-0Me 0 A-2063 H H H H H 0 cycbhexyl H 2-Me,5-0Me 0 A-2064 H H H H H 0 cycbhexyl H 2-Me,6-0Me 0 A-2065 H H H H H 0 cycbhexyl H 3-Me,6-0Me 0 A-2066 H H H H H 0 cycbhexyl H 4-Me,2-0Me 0 A-2067 H H H H H 0 cycbhexyl H 2,5-0Me 2 0 A-2068 H H H H H 0 cycbhexyl H 2,6-0Me 2 0 A-2069 H H H H H 0 cycbhexyl H 2-0Me,6-CF3 0 A-2070 H H H H H 0 cycbhexyl H 2-CHF2,5-F 0 A-2071 H H H H H 0 cycbhexyl H 2-CHF 2,6-F 0 A-2072 H H H H H 0 cycbhexyl H 2-CHF 2,b-MAe 0 A-2073 H H H H H 0 cycbhexyl H 2-CHF 2 ,6-Me 0 A-2074 H H H H H 0 cycbhexyl H 2-cycbpropyl,5-F 0 A-2075 H H H H H 0 cycbhexyl H 2-cycbpropyl,6-F 0 A-2076 H H H H H 0 cycbhexyl H 2-cyclopropyl,5-Me 0 A-2077 H H H H H 0 cycbhexyl H 2-cyclopropyl,6-Me 0 A-2078 H H H H H 0 cycbhexyl H 2-ethenyl,6-F 0 A-2079 H H H H H 0 cycbhexyl H 2-ethenyl,6-Me 0 A-2080 H H H H H 0 cycbhexyl H 2-0Et,5-F 0 A-2081 H H H H H 0 cycbhexyl H 2-0Et,6-F 0 A-2082 H H H H H 0 cycbhexyl H 2-0Et,5-CI 0 A-2083 H H H H H 0 cycbhexyl H 2-0Et,6-CI 0 A-2084 H H H H H 0 cycbhexyl H 2-0Et,5-Me 0 A-2085 H H H H H 0 cycbhexyl H 2-0Et,6-Me 0 A-2086 H H H H H 0 cycbhexyl H 2-0CHF 2,5-F 0 A-2087 H H H H H 0 cycbhexyl H 2-0CHF 2,6-F 0 A-2088 H H H H H 0 cycbhexyl H 2-OCHF 2 ,b-Me 0 A-2089 H H H H H 0 cycbhexyl H 2-0CHF 2 ,6-MAe 0 A-2090 H H H H H 0 cycbhexyl H 2-(cycobpropyloxy),5-F 0 A-2091 H H H H H 0 cycbhexyl H 2-(cycobpropyloxy),6-F 0 A-2092 H H H H H 0 cycbhexyl H 2-(cyclopropyloxy),5-M e 0 A-2093 H H H H H 0 cycbhexyl H 2-(cyclopropybxy),6-M e 0 A-2094 H H H H H 0 cycbhexyl H 2-SMe,5-F 0 A-2095 H H H H H 0 cycbhexyl H 2-SMe,6-F 0 A-2096 H H H H H 0 cycbhexyl H 2-SMe,5-Me 0 A-2097 H H H H H 0 cycbhexyl H 2-SMe,6-Me 0 A-2098 H H H H H 0 cycbhexyl H 2-S(0)Me,5-F 0 A-2099 H H H H H 0 cycbhexyl H 2-S(0)Me,6-F 0 A-2100 H H H H H 0 cycbhexyl H 2-S(=0)Me,5-M e 0 A-2101 H H H H H 0 cyobhexyl H 2-S(=0)Me,6-M e 0 A-2102 H H H H H 0 cyobhexyl H 2-S(=0) 2Me,5-F 0 A-2103 f H H H H 0 cycbhexyl H 2-S(=0) 2Me,6-F 0 A-2104 IH H IH H H 0 cycbhexyl H 2-S(0) 2 Me,5-Me 0
[0163]
[Table 38]
com pound R' R2 R R A R R' (R)m p A-2105 H H H H 0 cycbhexyl H 2-S(=U) 2 Me,6-M e 0 A-2106 H H H H cyc bhexyl H 2-SCH3,b-F 0 A-2107 H H H H D cyc bhexyl H 2-SCF 3 ,6-F 0 A-2108 H H H H if cy cbhexyl H 2-SCF 3 ,b-M e 0 A-2109 H H H H 0 cycbhexyl H 2-SGF 3 ,6-Me 0 A-2110 H H H H 0 cycbhexyl H 2-S(=U)G3,b-F 0 A-2111 H H H H f Di cycbhexyl H 2-S(=U)CF 3 ,6-F 0 A-2112 H H H H 0 cycbhexyl H 2-S(=U)CF 3 ,b-M e 0 A-2113 H H H H D i cyc bhexyl H 2-S(=U)CF 3,6-M e 0 A-2114 H H H H D i cyc bhexyl H 2-S(=0) 20F 3,-F A-2115 iH H H H Hi cyc bhexyl H 2-S =0) 20F3,6- 0 A-2116 H H H H D cycbhexyl H 2-S(=0) 2C F 3,b--e 0 A-2117 H H H H 0 cycbhexyl H 2-S(=0) 2CF 3 ,6-M e 0 A-2118 H H H H 0 cycbhexyl H 2-(cycobpropylthb),b-F 0 A-2119 H H H H 0 cycbhexyl H 2-(cycobpropylthb),6-F 0 A-2120 H H H H cycbhexyl H 2-(cyclopropylthio),b-Me 0 A-2121 H H H H cycbhexyl H 2-(cyclopropylthio),6-Me 0 A-2122 H H H H D cycbhexyl H 2-(=0)Me,b-F 0 A-2123 H H H H cycbhexyl H 2-0(=0)Me,6-F 0 A-2124 H H H H 0 cycbhexyl H 2-0(=O)Me,b-Me 0 A-2125 H H H H cycbhexyl H 2-0(=0)Me,6-Me 0 A-2126 H H H H cycbhexyl H 2-OH 2UH,b-F 0 A-2127 H H H H cyc bhexyl H 2-OH 2UH,6-F 0 A-2128 H H H H cycbhexyl H 2-CH 2UH,b-M e 0 A-2129 H H H H cycbhexyl H 2-CH 20,6-M e 0 A-2130 H H H H cycbhexyl H -GH 2UH 3,4- 0 A-2131 H H H H cycbhexyl H Z-GH 2UGH 3,b-H 0 A-2132 H H H H H cyc hbhexyl H 2-OH 20H 3 ,6-F 0 A-2133 H H H H D cycbhexyl H 2-OH 2OCH 3 ,4-Me 0 A-2134 H H H H D cycbhexyl H 2-OH 2OCH 3 ,b-Me 0 A-2135 H H H H cyc bhexyl H 2-OH 2 CH 3 ,6-MAe 0 A-2136 H H H H D cycbhexyl H 2-0(=U)0H 3,b-F 0 A-2137 H H H H cyc bhexyl H 2-0C(=U)0H 3 ,6-F 0 A-2138 H H H H cycbhexyl H 2-00(=0)CH 3 ,b-M e 0 A-2139 H H H H D cycbhexyl H 2-0(=U)CH 3 ,6-M e 0 A-2140 H H H H D cycbhexyl H 2-US(=U) 2 0H3,-F A-2141 H H H H cycbhexyl H 2-OS(=0) 2CH 3 ,6- 0 A-2142 H H H H D cycbhexyl H 2-OS(=U) 2CH 3,b-M e 0 A-2143 H H H H 0 cycbhexyl H 2-OS(=U) 2CH 3,6-Me 0 A-2144 H H H H H 0 cycbhexyl H 2-OH 2 SCH 3 ,b-4 0 A-2145 H H H H 0 cycbhexyl H 2-OH 2 SCH 3,6-F 0 A-2146 H H H H D cycbhexyl H 2-OH 2S0H 3,b-Me A-2147 H H H H 0 cycbhexyl H 2-CH 2SCH 3,6-M e 0 A-2148 H H H H cycbhexyl H 2-NM e 2 ,b-F A-2149 H H H H D cycbhexyl H 2-NM e 2 ,6-F 0 A-2150 H H H H cycbhexyl H 2-NM e 2 ,b-A e 0 A-2151 H H H H 0 cycbhexyl H 2-NMe 2 ,6-Me 0 A-2152 H H H H 0 cycbhexyl H 2-ON,4-F 0 A-2153 H H H H 0 cycbhexyl H 2-ONb-F 0 A-2154 H H H H cycbhexyl H 2-ON,6-F 0 A-2155 H H H H 0 cycbhexyl H 2-ON,6-Me F A-2156 H H H H cycbhexyl H 2-ONS5-OM e 0 A-2157 H H H H cycbhexyl H 2-ON,6-OMe 0 A-2158 H H H H D cycbhexyl H 3-ON,6-Me 0 A-2159 H H H H cycbhexyl H 3-ON,6-OM e 0 A-2160 H H H H cycbhexyl H 4-GN,2-M e 0 A-2161 H f F IFH cycbhexyl H 4-GN,2-UMe 0
[0164]
[Table 39]
com pound RI R2 R R R A R R' (R)m P A-2162 iH H H H H 0 cycbhexyl H 2-N02,4-F 0 A-2163 H H H H H 0 cycbhexyl H 2-N0 2 ,5-F 0 A-2164 H H H H H 0 cycbhexyl H 2-N0 2 ,6-F 0 A-2165 H H H H H 0 cycbhexyl H 2-N0 2,4-MAe 0 A-2166 H H H H H 0 cycbhexyl H 2-N0 2,5-Me 0 A-2167 H H H H H 0 cycbhexyl H 2-N0 2,6-Me 0 A-2168 H H H H H 0 cycbhexyl H 2-Me,4,5-F 2 0 A-2169 H H H H H 0 cycbhexyl H 2-Me,6-Et 0 A-2170 H H H H H 0 cycbhexyl H 2-cyclopropyl,6-OMe 0 A-2171 H H H H H 0 cycbhexyl H 2-M e,5-Et 0 A-2172 H H H H H 0 cycbhexyl H 2,6-Et2 0 A-2173 H H H H H 0 cycbhexyl H 2-Et,6-F 0 A-2174 H H H H H 0 cycbhexyl H 2-CH 200H3 ,6-CI 0 A-2175 H H H H H 0 cycbhexyl H 2-CH 20CH 2 CH 3 ,6-CI 0 A-2176 H H H H H 0 cycbhexyl H 2-CH 2 NMe 2 0 A-2177 H H H H H 0 allyl H H 0 A-2178 H H H H H 0 allyl H 2-F 0 A-2179 H H H H H 0 allyl H 2-Cl 0 A-2180 H H H H H 0 allyl H 2-Br 0 A-2181 H H H H H 0 allyl H 2-OH 0 A-2182 H H H H H 0 allyl H 2-M e 0 A-2183 H H H H H 0 allyI H 2-Et 0 A-2184 H H H H H 0 allyI H 2-Pr 0 A-2185 H H H H H 0 allyl H 2-CF, 0 A-2186 H H H H H 0 allyI H 2-CHF 2 0 A-2187 H H H H H 0 allyI H 2-CH2F 0 A-2188 H H H H H 0 allyl H 2-0F 2C1 0 A-2189 H H H H H 0 allyl H 2-cycbpropyl 0 A-2190 H H H H H 0 allyl H 2-cycobbutyl 0 A-2191 H H H H H 0 allyl H 2-cycbpentyl 0 A-2192 H H H H H 0 allyl H 2-ethenyl 0 A-2193 H H H H H 0 allyl H 2-aIlyl 0 A-2194 H H H H H 0 allyl H 2-(prop-1-en-1-yD 0 A-2195 H H H H H 0 allyl H 2-(trifboroethenyD 0 A-2196 H H H H H 0 allyl H 2-0Me 0 A-2197 H H H H H 0 allyl H 2-0Et 0 A-2198 H H H H H 0 allyl H 2-0Pr 0 A-2199 H H H H H 0 allyl H 2-0(/-Pr) 0 A-2200 H H H H H 0 allyI H 2-0CF 0 A-2201 H H H H H 0 allyl H 2-0CHF 2 0 A-2202 H H H H H 0 allyl H 2-(cycbpropybxy) 0 A-2203 H H H H H 0 allyl H 2-(cycobbutyloxy) 0 A-2204 H H H H H 0 allyl H 2-(cycbpentybxy) 0 A-2205 H H H H H 0 allyl H 2-((2,2-dichbrocycbpropyl)oxy) 0 A-2206 H H H H H 0 allyl H 2-(oxiran-2-y) 0 A-2207 H H H H H 0 allyl H 2-SMe 0 A-2208 H H H H H 0 allyl H 3-SMe 0 A-2209 H H H H H 0 allyl H 2-S(=0)Me 0 A-2210 H H H H H 0 allyl H 3-S(=0)Me 0 A-2211 H H H H H 0 allyl H 2-S(=0) 2Me 0 A-2212 H H H H H 0 allyl H 3-S(=0) 2Me 0 A-2213 H H H H H 0 allyI H 2-SCF3 0 A-2214 H H H H H 0 allyl H 3-S03 0 A-2215 H H H H H 0 allyl H 3-S(=0)CF3 0 A-2216 H H H H H 0 alyI H 3-SCF(CF3) 2 0 A-2217 H H H H H 0 allyl H 2-(cycbpropylthio) 0 A-2218 H Hf H H 0 allyl H 2-(cycbpropysulfinyD 0
[0165]
[Table 40]
com pound RI R2 R R R A R R' (R)m P A-2219 i H H H H H 0 all H 2-(cycbpropylsulfonyD 0 A-2220 H H H H H 0 alhI H 2-4(=0)Me 0 A-2221 H H H H H 0 alll H 2-CH 2C(=O)CH3 0 A-2222 H H H H H 0 alll H 2-CH 20(=O)0F3 0 A-2223 H H H H H 0 alll H 2-CH 2 0H 0 A-2224 H H H H H 0 alll H 2-CH 2 0CH, 0 A-2225 H H H H H 0 alll H 2-CH 2 0CH 2 CH3 0 A-2226 H H H H H 0 alll H 2-CH 2SCH3 0 A-2227 H H H H H 0 alll H 2-CH 2S(=0)CH, 0 A-2228 H H H H H 0 alll H 2-CH 2S(=0H 3 0 A-2229 H H H H H 0 alll H 2-(benzybxy) 0 A-2230 H H H H H 0 alll H 2-NH 2 0 A-2231 H H H H H 0 alll H 2-NHMe 0 A-2232 H H H H H 0 alll H 2-N(e) 2 0 A-2233 H H H H H 0 alll H 2-(1,3-dbxolan-2-y) 0 A-2234 H H H H H 0 alll H 2-(1,3-dbxan-2-yD 0 A-2235 H H H H H 0 alll H 2-(1H-in idazol-2-yD 0 A-2236 H H H H H 0 alll H 2-(thiazol-2-yl) 0 A-2237 H H H H H 0 alll H 2-(oxazol-2-yD 0 A-2238 H H H H H 0 alll H 2-CH=N0H 0 A-2239 H H H H H 0 alh'I H 2-CH= NOM e 0 A-2240 H H H H H 0 all H 2-(4,5-dihydro-3-soxazolyD 0 A-2241 H H H H H 0 alll H 2-CN 0 A-2242 H H H H H 0 alb'I H 2-N0 2 0 A-2243 H H H H H 0 alll H 2-F,6-CI 0 A-2244 H H H H H 0 alll H 2-F,6-M e 0 A-2245 H H H H H 0 alll H 3-F,6-M e 0 A-2246 H H H H H 0 alll H 4-F,2-M e 0 A-2247 H H H H H 0 alll H 2-F,6-0Me 0 A-2248 H H H H H 0 alll H 3-F,6-0Me 0 A-2249 H H H H H 0 alll H 2,6-Cl2 0 A-2250 H H H H H 0 alll H 2-CI,6-M e 0 A-2251 H H H H H 0 alll H 3-CI,6-M e 0 A-2252 H H H H H 0 alll H 4-CI,2-M e 0 A-2253 H H H H H 0 alll H 2-C1,5-CF, 0 A-2254 H H H H H 0 alll H 2-01,6-0F 3 0 A-2255 H H H H H 0 alll H 2-C1,6-0Me 0 A-2256 H H H H H 0 alll H 3-C1,6-0Me 0 A-2257 H H H H H 0 alll H 4-CI,2-0Me 0 A-2258 H H H H H 0 alll H 2,4-M e 2 0 A-2259 H H H H H 0 alIl H 2,5-M e 2 0 A-2260 H H H H H 0 alll H 2,6-M e 2 0 A-2261 H H H H H 0 alll H 2-M e,4-F3 0 A-2262 H H H H H 0 alll H 2-M e,b-F3 0 A-2263 H H H H H 0 alll H 2-M e,6-F3 0 A-2264 H H H H H 0 allI H 2-M e,4-0Me 0 A-2265 H H H H H 0 allI H 2-M e,5-0Me 0 A-2266 H H H H H 0 allyl H 2-M e,6-OMe 0 A-2267 H H H H H 0 allyl H 3-M e,6-OMe 0 A-2268 H H H H H 0 allyl H 4-M e,2-OMe 0 A-2269 H H H H H 0 allyl H 2,5-0Me 2 0 A-2270 H H H H H 0 alll H 2,6-0Me 2 0 A-2271 H H H H H 0 alll H 2-OMe,6-F3 0 A-2272 H H H H H 0 alll H 2-CHF 2,5-F 0 A-2273 H H H H H 0 alll H 2-CHF 2,6-F 0 A-2274 H H H H H 0 alll H 2-CHF 2,b-MAe 0 A-2275 H f F H IH 0 allI H 2-CHF 2,6-Me 0
[0166]
[Table 41]
com pound RI R2 R R R A R R' (R)m P A-2276 H H H H H 0 allyl H 2-cycbpropyl,5-F 0 A-2277 H H H H H 0 allyl H 2-cycbpropyl,6-F 0 A-2278 H H H H H 0 allyl H 2-cyclopropyl,5-Me A-2279 H H H H H 0 allyl H 2-cyclopropyl,6-Me 0 A-2280 H H H H H 0 allyl H 2-ethenyl,6-F 0 A-2281 H H H H H 0 allyl H 2-ethenyl,6-M e 0 A-2282 H H H H H 0 allyl H 2-0Et,5-F 0 A-2283 H H H H H 0 allyl H 2-0Et,6-F 0 A-2284 H H H H H 0 allyl H 2-0Et,5-CI 0 A-2285 H H H H H 0 allyl H 2-0Et,6-CI 0 A-2286 H H H H H 0 allyl H 2-0Et,5-M e 0 A-2287 H H H H H 0 allyl H 2-0Et,6-M e 0 A-2288 H H H H H 0 allyl H 2-0CH2,b-F 0 A-2289 H H H H H 0 allyl H 2-0CHF 2,6-F 0 A-2290 H H H H H 0 allyl H 2-0CHF 2 ,b -Me 0 A-2291 H H H H H 0 allyl H 2-0CHF 2 ,6 -M e 0 A-2292 H H H H H 0 allyl H 2-(cycobpropyloxy),5-F 0 A-2293 H H H H H 0 allyl H 2-(cycobpropyloxy),6-F 0 A-2294 H H H H H 0 allyl H 2-(cyclopropyloxy),5-M e 0 A-2295 H H H H H 0 allyl H 2-(cyclopropyloxy),6-M e 0 A-2296 H H H H H 0 allyl H 2-SMe,5-F 0 A-2297 H H H H H 0 allyl H 2-SMe,6-F 0 A-2298 H H H H H 0 allyl H 2-SMe,5-M e 0 A-2299 H H H H H 0 allyl H 2-SMe,6-M e 0 A-2300 H H H H H 0 allyl H 2-S(=0)Me,5-F 0 A-2301 H H H H H 0 allyl H 2-S(=0)Me,6-F 0 A-2302 H H H H H 0 allyl H 2-S(=0)Me,5-M e 0 A-2303 H H H H H 0 allyl H 2-S(=0)Me,6-M e 0 A-2304 H H H H H 0 allyl H 2-S(=0) 2 Me,5-F 0 A-2305 H H H H H 0 allyl H 2-S(=0) 2 Me,6-F 0 A-2306 H H H H H 0 allyl H 2-S(=0) 2 Me,5-M e 0 A-2307 H H H H H 0 allyl H 2-S(=0) 2 Me,6--M e 0 A-2308 H H H H H 0 allyl H 2-SCF,b-F 0 A-2309 H H H H H 0 allyl H 2-SCF,,6-F 0 A-2310 H H H H H 0 allyl H 2-SCF 3 ,b-Me 0 A-2311 H H H H H 0 allyl H 2-SCF 3 ,6-M e 0 A-2312 H H H H H 0 allyl H 2-S (=O)CF 3 ,b-F 0 A-2313 H H H H H 0 allyl H 2-S (=0)CF 3 ,6-F 0 A-2314 H H H H H 0 allyl H 2-S(=0)CF 3 ,b-Me 0 A-2315 H H H H H 0 allyl H 2-S(=0)CF 3 ,6-M e 0 A-2316 H H H H H 0 allyl H 2-S(=0) 2CF3 ,b-F 0 A-2317 H H H H H 0 allyl H 2-S(=0) 2CF 3 ,6-F 0 A-2318 H H H H H 0 allyl H 2-S(=0) 2CF 3 ,b-Me 0 A-2319 H H H H H 0 allyl H 2-S(=0) 2CF 3 ,6-Me A-2320 H H H H H 0 allyl H 2-(cycobpropylthb),5-F 0 A-2321 H H H H H 0 allyl H 2-(cycobpropylthb),6-F 0 A-2322 H H H H H 0 allyl H 2-(cycobpropythio),5-M e 0 A-2323 H H H H H 0 allyl H 2-(cycobpropylthio),6-M e 0 A-2324 H H H H H 0 allyl H 2-C(=0)Me,5-F 0 A-2325 H H H H H 0 allyl H 2-C(=0)Me,6-F 0 A-2326 H H H H H 0 allyl H 2-C(=0)Me,5-M e 0 A-2327 H H H H H 0 allyl H 2-C(=0)Me,6-Me 0 A-2328 H H H H H 0 allyl H 2-CH20H,b-F 0 A-2329 H H H H H 0 allyl H 2-CH 20H,6-F 0 A-2330 H H H H H 0 allyI H 2-CH 20H, 5-M e 0 A-2331 H H H H H 0 allyl H 2-CH20H,6-M e 0 A-2332 H f F H IH 0 alyI H 2-CH 20CH 3 ,4-F 0
[0167]
[Table 42]
com pound R' R2 R R A R R' (R)m p A-2333 H H H H 0 aly| H 2-0H 20H 3 ,b-F 0 A-2334 H H H H H 0 alh'I H 2-0H 20H 3 ,6-F 0 A-2335 H H H H 0 alh'I H 2-CH 20H 3 ,4-Me 0 A-2336 H H H H i 0 alhI H 2-CH 2UCH 3 ,b5-Me A-233/ iH H H H 0 alhl H 2-CH 20H 3 ,6-MeA A-2338 H H H H 0 alhl H 2)-00= 0)0H 3 ,b-F 0 A-2339 H H H H 0 alhl H 2)-0C= 0)CH 3 ,6-F 0 A-2340 H H H H 0 alhI H 2-00(=0)GH 3 ,b-Me 0 A-2341 H H H H 0 al lI H 2-00C(= 0)CH 3 ,6-M e 0 A-2342 H H H H 0 alhl H 2-OS( = ) 2 H 3 ,5-4 A-2343 H H H H i 0 alhl H 2-OS( = ) 2 H3 ,6- 0 A-2344 H H H H 0 alhl H 2-OS(= ) 2 CH 3,b-Me 0 A-2345 H H H H 0 alhl H 2-O S= U)2 CH 3,6-M e 0 A-2346 H H H H 0 alhl H 2-CH 2SCH 3 ,b-4 0 A-2347 H H H H 0 alhl H 2-CH 2SOH 3 ,6-F 0 A-2348 H H H H 0 alhl H 2-CH 2SCH 3,b-M e 0 A-2349 H H H H 0 alIl H 2-CH 2SCH 3,6-M e 0 A-2350 H H H H 0 alI| H 2-NM e 2 b-F 0 A-2351 H H H H 0 alI| H 2-NM e 2 ,6-F 0 A-2352 H H H H 0 alhl H 2AM e 2 ,b-M e 0 A-2353 H H H H 0 alh'| H 2-NM e 2 ,6-M e 0 A-2354 H H H H 0 albI H 2-ON4-F 0 A-2355 H H H H 0 albI H 2-CN,b-F 0 A-2356 H H H H 0 alb'l H 2-CN,6-F 0 A-2357 H H H H 0 al/I H 2-CN,6-Me 0 A-2358 H H H H 0 aly| H 2-CN,b-OM e 0 A-2359 H H H H 0 aly| H 2-CN,6-OM e 0 A-2360 H H H H i 0 al/I H 3-CN,6-Me 0 A-2361 H H H H 0 alb'l H 3-CN,6-OM e 0 A-2362 H H H H 0 albI H 4-CN,2-Me 0 A-2363 H H H H 0 alb'l H 4-CN,2-OM e 0 A-2364 H H H H 0 alh'| H 2A0214-F 0 A-2365 H H H H H 0 alh'I H 2-N0 2 ,b-F 0 A-2366 H H H H 0 alh'| H 240 2 ,6-F 0 A-2367 H H H H 0 alll H 2-N0 2,4 -M e 0 A-2368 H H H H 0 alhl H 2-NU 2,5-M e 0 A-2369 H H H H 0 alhl H 2-NU 2,6-M e 0 A-2370 H H H H 0 alhl H 2-M e,4,b-F 2 0 A-2371 H H H H 0 alb'l H 2-M e,6-Et 0 A-2372 H H H H H 0 alb'l H 2-cyclopropyl,6-OM e 0 A-2373 H H H H 0 albl H 2-M e,b-Et 0 A-2374 H H H H 0Di alll H 2,6-Et2 0 A-2375 H H H H 0 albl H 2-Et,6-F 0 A-2376 H H H H 0 alhl H 2-UH 20H 3 ,6-I1 A-2377 H H H H 0 alh'l H 2-GH 20H 2CH 3,6-C 1 0 A-2378 H H H H 0 al/I H 2-UH 2 NMe 2 0 A-2379 H H H H 0 1-cycbhexylethy I H H 0 A-2380 H H H H 0 1-cycbhexylethy I H 2-F 0 A-2381 H H H H 0 1-cycobhexylethy I H 2-C l 0 A-2382 H H H H 0 1-cycobhexylethyl H 2-Br 0 A-2383 H H H H 0 1-cycobhexylethyl H 2-OH 0 A-2384 H H H H 1-cy lobhexylethyl H 2-M e 0 A-2385 H H H H 0 1-cycbhexylethyl H 2-Et 0 A-2386 H H H H 0 1-cycbhexylethy I H 2-Pr 0 A-2387 H H H H 0 1-cycbhexylethy I H 2-CF 3 0 A-2388 H H H H E0 -ycbhexylethyl H 2-GHF 2 0 A-2389 H H H H 0 1-cycbhexylethyl H 2-CH 2F 0
[0168]
[Table 43]
com pound RI R2 R R R A R R' (R)m P A-2390 H H H H H 0 1-cycbhexylethyl H 2-CF 2C1 0 A-2391 H H H H H 0 1-cycbhexylethyl H 2-cycbpropyl 0 A-2392 H H H H H 0 1-cycbhexylethyl H 2-cycobbutyl 0 A-2393 H H H H H 0 1-cycbhexylethyl H 2-cycbpentyl 0 A-2394 H H H H H 0 1-cycbhexylethyl H 2-ethenyl 0 A-2395 H H H H H 0 1-cycbhexylethyl H 2-allyl 0 A-2396 H H H H H 0 1-cycobhexylethyl H 2-(prop-1-en-1-yD 0 A-2397 H H H H H 0 1-cycobhexylethyl H 2-(trifboroethenyD 0 A-2398 H H H H H 0 1-cycbhexylethyl H 2-0Me 0 A-2399 H H H H H 0 1-cycbhexylethyl H 2-0Et 0 A-2400 H H H H H 0 1-cycbhexylethyl H 2-0Pr 0 A-2401 H H H H H 0 1-cycbhexylethyl H 2-0 (/-Pr) 0 A-2402 H H H H H 0 1-cycbhexylethyl H 2-00F 0 A-2403 H H H H H 0 1-cycbhexylethyl H 2-0CHF 2 0 A-2404 H H H H H 0 1-cycbhexylethyl H 2-(cycbpropybxy) 0 A-2405 H H H H H 0 1-cycbhexylethyl H 2-(cycobbutyloxy) 0 A-2406 H H H H H 0 1-cycbhexylethyl H 2-(cycbpentybxy) 0 A-2407 H H H H H 0 1-cycbhexylethyl H 2-((2,2-dichbrocycbpropy)oxy) 0 A-2408 H H H H H 0 1-cycbhexylethyl H 2-(oxiran-2-yl 0 A-2409 H H H H H 0 1-cycbhexylethyl H 2-SMe 0 A-2410 H H H H H 0 1-cycbhexylethyl H 3-SMe 0 A-2411 H H H H H 0 1-cycbhexylethyl H 2-S(=0)Me 0 A-2412 H H H H H 0 1-cycbhexylethyl H 3-S(=O)Me 0 A-2413 H H H H H 0 1-cycbhexylethyl H 2-S(=0) 2Me 0 A-2414 H H H H H 0 1-cycbhexylethyl H 3-S(0) 2Me 0 A-2415 H H H H H 0 1-cycbhexylethyI H 2-SCF3 0 A-2416 H H H H H 0 1-cycbhexylethyI H 3-SCF3 0 A-2417 H H H H H 0 1-cycbhexylethyl H 3-S(=0)CF3 0 A-2418 H H H H H 0 1-cycbhexylethyI H 3-SCF(CF3) 2 0 A-2419 H H H H H 0 1-cycbhexylethyl H 2-(cycbpropylthio) 0 A-2420 H H H H H 0 1-cycbhexylethyl H 2-(cycbpropylsulfinyD 0 A-2421 H H H H H 0 1-cycbhexylethyl H 2-(cycbpropylsulfonyD 0 A-2422 H H H H H 0 1-cycbhexylethyl H 2-C(=0)Me 0 A-2423 H H H H H 0 1-cycbhexylethyl H 2-CH 20(=0)0H 3 0 A-2424 H H H H H 0 1-cycbhexylethyl H 2-CH 2C0(=)CF 3 0 A-2425 H H H H H 0 1-cycbhexylethyl H 2-CH 2OH 0 A-2426 H H H H H 0 1-cycbhexylethyl H 2-CH 2 00H 3 0 A-2427 H H H H H 0 1-cycbhexylethyl H 2-CH 2 0CH 2CH 3 0 A-2428 H H H H H 0 1-cycbhexylethyl H 2-CH 2SCH 3 0 A-2429 H H H H H 0 1-cycbhexylethyl H 2-CH 2S(=0)CH 3 0 A-2430 H H H H H 0 1-cycbhexylethyl H 2-CH 2S(=0) 2 CH3 0 A-2431 H H H H H 0 1-cycbhexylethyl H 2-(benzybxy) 0 A-2432 H H H H H 0 1-cycbhexylethyl H 2-NH 2 0 A-2433 H H H H H 0 1-cycbhexylethyl H 2-NHMe 0 A-2434 H H H H H 0 1-cycbhexylethyl H 2-N (Me) 2 0 A-2435 H H H H H 0 1-cycbhexylethyl H 2-(1,3-dioxolan-2-yD 0 A-2436 H H H H H 0 1-cycbhexylethyl H 2-(1,3-dioxan-2-y D 0 A-2437 H H H H H 0 1-cycbhexylethyl H 2-(1H--m idazol-2-yD 0 A-2438 H H H H H 0 1-cycbhexylethyl H 2-(thiazol-2-y) 0 A-2439 H H H H H 0 1-cycbhexylethyl H 2-(oxazol-2-yl 0 A-2440 H H H H H 0 1-cycbhexylethyl H 2-CH=N0H 0 A-2441 H H H H H 0 1-cycbhexylethyl H 2-CH=NOMe 0 A-2442 H H H H H 0 1-cycbhexylethyI H 2-(4,5-dihydro-3-isoxazolyD 0 A-2443 H H H H H 0 1-cycbhexylethyl H 2-CN 0 A-2444 H H H H H 0 1-cycbhexylethyl H 2-N0 2 0 A-2445 H H H H H 0 1-cycbhexylethyl H 2-F,6-CI 0 A-2446 H f IF H 0 1-cycbhexylethy I H 2-F,6-Me 0
[0169]
[Table 44]
com pound RI R2 R R R A R R' (R)m P A-2447 Hif7- H H H H 0 1-cycbhexylethyI H 3-F,6-Me 0 A-2448 H H H H H 0 1-cycbhexylethyI H 4-F,2-Me 0 A-2449 H H H H H 0 1-cycbhexylethyl H 2-F,6-0Me A-2450 H H H H H 0 1-cycbhexylethyl H 3-F,6-0Me 0 A-2451 H H H H H 0 1-cycbhexylethyl H 2,6-Cl2 0 A-2452 H H H H H 0 1-cycbhexylethyl H 2-CI,6-M e 0 A-2453 H H H H H 0 1-cycbhexylethyl H 3-CI,6-M e 0 A-2454 H H H H H 0 1-cycbhexylethyl H 4-CI,2-M e 0 A-2455 H H H H H 0 1-cycbhexylethyI H 2-CL,5-CF 0 A-2456 H H H H H 0 1-cycbhexylethyI H 2-C1,6-0F 3 0 A-2457 H H H H H 0 1-cycbhexylethyl H 2-C1,6-0Me 0 A-2458 H H H H H 0 1-cycbhexylethyl H 3-C1,6-0Me 0 A-2459 H H H H H 0 1-cycbhexylethyl H 4-C,2-0Me 0 A-2460 H H H H H 0 1-cycbhexylethyl H 2,4-M e 2 0 A-2461 H H H H H 0 1-cycbhexylethyl H 2,5-M e 2 0 A-2462 H H H H H 0 1-cycbhexylethyl H 2,6-Me 2 0 A-2463 H H H H H 0 1-cycbhexylethyl H 2-Me,4-0F 3 0 A-2464 H H H H H 0 1-cycbhexylethyI H 2-Me,5-CF3 0 A-2465 H H H H H 0 1-cycobhexylethyI H 2-Me,6-0F 3 0 A-2466 H H H H H 0 1-cycobhexylethyl H 2-Me,4-0Me 0 A-2467 H H H H H 0 1-cycobhexylethyl H 2-Me,5-0Me 0 A-2468 H H H H H 0 1-cycobhexylethyl H 2-Me,6-0Me 0 A-2469 H H H H H 0 1-cycobhexylethyl H 3-Me,6-0Me 0 A-2470 H H H H H 0 1-cycobhexylethyl H 4-Me,2-0Me 0 A-2471 H H H H H 0 1-cycobhexylethyl H 2,b-0Me 2 0 A-2472 H H H H H 0 1-cycobhexylethyl H 2,6-0Me 2 0 A-2473 H H H H H 0 1-cycobhexylethyI H 2-0Me,6-GF 3 0 A-2474 H H H H H 0 1-cycobhexylethyI H 2-CHF2,5-F 0 A-2475 H H H H H 0 1-cycbhexylethyI H 2-CHF 2,6-F 0 A-2476 H H H H H 0 1-cycbhexylethyI H 2-CHF 2,5-Me 0 A-2477 H H H H H 0 1-cycbhexylethyI H 2-CHF 2,6-Me 0 A-2478 H H H H H 0 1-cycbhexylethyl H 2-cycbpropyl,5-F 0 A-2479 H H H H H 0 1-cycbhexylethyl H 2-cycbpropyl,6-F 0 A-2480 H H H H H 0 1-cycbhexylethyl H 2-cyclopropyl,5-Me 0 A-2481 H H H H H 0 1-cycbhexylethyl H 2-cyclopropyl,6-Me 0 A-2482 H H H H H 0 1-cycbhexylethyl H 2-ethenyl,6-F 0 A-2483 H H H H H 0 1-cycbhexylethyl H 2-ethenyl,6-M e 0 A-2484 H H H H H 0 1-cycbhexylethyl H 2-0Et,5-F 0 A-2485 H H H H H 0 1-cycbhexylethyl H 2-0Et,6-F 0 A-2486 H H H H H 0 1-cycbhexylethyl H 2-0Et,5-CI 0 A-2487 H H H H H 0 1-cycbhexylethyl H 2-0Et,6-CI 0 A-2488 H H H H H 0 1-cycbhexylethyl H 2-0Et,5-M e 0 A-2489 H H H H H 0 1-cycbhexylethyl H 2-0Et,6-M e 0 A-2490 H H H H H 0 1-cycbhexylethyI H 2-2CH2,b-F 0 A-2491 H H H H H 0 1-cycbhexylethyl H 2-OCHF 2,6-F 0 A-2492 H H H H H 0 1-cycbhexylethyI H 2-OCHF 2 ,b-Me 0 A-2493 H H H H H 0 1-cycbhexylethyI H 2-0CHF 2 ,6-Me 0 A-2494 H H H H H 0 1-cycbhexylethyl H 2-(cycbpropyloxy),5-F 0 A-2495 H H H H H 0 1-cycbhexylethyl H 2-(cycbpropyloxy),6-F 0 A-2496 H H H H H 0 1-cycbhexylethyl H 2-(cyclopropyloxy),5-M e 0 A-2497 H H H H H 0 1-cycbhexylethyl H 2-(cyclopropybxy),6-M e 0 A-2498 H H H H H 0 1-cycbhexylethyl H 2-SMe,5-F 0 A-2499 H H H H H 0 1-cycbhexylethyI H 2-SMe,6-F 0 A-2500 H H H H H 0 1-cycbhexylethyl H 2-SMe,5-M e 0 A-2501 H H H H H 0 1-cycbhexylethyl H 2-SMe,6-M e 0 A-2502 f H H H H 0 1-cycbhexylethyl H 2-S(=0)Me,5-F 0 A-2b03 IH H IH IH H 0 1-cycbhexylethyl H 2-S(0)Me,6-F 0
[0170]
[Table 45]
com pound R' R2 R R A R R' (R)m p A-2504-iH H H H 0 1-cycbhexylethyl H 2-S(0)Me,b-Me 0 A-2505 H H H H 1-cycbhexylethyl H 2-S(=0)Me,6-Me A-2506 H H H H 0 1-cycbhexylethyl H 2-S(=U) 2Me,b-F W A-2507 H H H H i 0 1-cycobhexylethyl H 2-St=U) 2Me,6-H 0 A-2508 H H H H 0 1-cycobhexylethyI H 2-S(=U) 2 Me,b-Me A-2509 H H H H 0 1-cycobhexylethyI H 2-S(=U) 2 Me,6-Me 0 A-2510 H H H H f Di 1-cycobhexylethyl H 2-SGH3,b-F 0 A-2511 H H H H 0 1-cycobhexylethyl H 2-SF 3 ,6-F 0 A-2512 H H H H H 0 1-cycobhexylethyI H 2-SGF 3 ,b-M e 0 A-2513 H H H H 0 1-cycbhexylethyI H 2-SCF 3 ,6-M e 0 A-2514 H H H H i 0 1-cycbhexylethyI H 2-S (O)F 3 ,b-H 0 A-2515 H H H H 0 1-cycbhexylethyI H 2-S (O)F 3,6- 0 A-2516 H H H H 0 1-cycbhexylethyI H 2-S(=O)CF 3 ,b-M e 0 A-251 7 H H H H 0 1-cycbhexylethyI H 2-S(=U)0F 3 ,6-M e 0 A-2518 H H H H 0 1-cycbhexylethyI H 2-S(=0) 20%3,5-F 0 A-2519 H H H H 0 1-cycbhexylethyI H Z-S(=U) 20F 3 ,6- 0 A-2520 H H H H 0 1-cycbhexylethyI H Z-S(=U) 2CF 3,b-m e 0 A-2521 H H H H 0 1-cycbhexylethyl H 2-S(=0) 20F 3 ,6-M e 0 A-2522 H H H H 1-cycbhexylethyl H 2-(cycbpropyltho),5-F 0 A-2523 H H H H 0 1-cycbhexylethyl H 2-(cycobpropylthb),6-F 0 A-2524 H H H H 1-cycbhexylethyl H 2-(cycbpropylthio),5-M e 0 A-2525 H H H H 0 1-cycbhexylethyl H 2-(cycbpropylthio),6-M e 0 A-2526 H H H H 0 1-cycbhexylethyI H 2-(00)MeS-F 0 A-2527 H H H H 0 1-cycbhexylethyI H 2-0C0)Me,6-F 0 A-2528 H H H H 1-cycbhexylethyl H 2-0C(=)Me,5-Me 0 A-2529 H H H H 1-cycbhexylethyl H 2-0C(=)Me,6-Me 0 A-2530 H H H H 1-cycbhexylethyl H 2-GH 2UNb-H 0 A-2531 H H H H i 0 1-cycbhexylethyl H 2-OH 2 0H,6-F 0 A-2532 H H H H 0 1-cycbhexylethyl H 2-0H 20H,5-M e 0 A-2533 H H H H 0 1-cycbhexylethyl H 2-0H 20H,6-M e 0 A-2534 H H H H 0 1-cycbhexylethyl H 2-OH 20H 3 ,4-F 0 A-2535 H H H H 0 1-cycbhexylethyl H 2-OH 20H 3,5-F 0 A-2536 H H H H H 0 1-cycbhexylethyl H 2-OH 20H 3 ,6-F 0 A-2537 H H H H 1-cycbhexylethyI H 2-GH 2UCH 3 ,4-M e 0 A-2538 H H H H 0 1-cycbhexylethyI H 2-OH 20H 3 ,5-Me 0 A-2539 H H H H 0 1-cycbhexylethyI H 2-GH 2 CH 3 ,6-M e 0 A-2540 H H H H 0 1-cycbhexylethyI H 2-0G0U)GH 3 ,b-H 0 A-2541 H H H H 0 1-cycbhexylethyI H 2-00C(0)CH 3 ,6-F 0 A-2542 H H H H 0 1-cycbhexylethyl H 2-0(=0)GH 3,5-Me 0 A-2543 H H H H 0 1-cycbhexylethyl H 2-0(=0)CH 3 ,6-M e 0 A-2544 H H H H 0 1-cycbhexylethyI H 2-OS =0) 20H 3 ,5-F 0 A-2545 H H H H 0 1-cycbhexylethyI H 2-OS =0) 2CH 3 ,6-F 0 A-2546 H H H H 0 1-cycbhexylethyl H 2-UOS=U) 2CH 3,b-M e 0 A-2547 H H H H 0 1-cycbhexylethyl H 2-OS(=U) 2CH 3,6-e A-2548 H H H H 0 1-cycbhexylethyI H -H 2 S0H 3,b A-2549 H H H H 0 1-cycbhexylethyI H -H 2 0H 3,6- 0 A-2550 H H H H 0 1-cycbhexylethyI H 2-OH 2SCH 3,5-Me 0 A-2551 H H H H 0 1-cycbhexylethyI H 2-OH 2SOH 3 ,6-MAe 0 A-2552 H H H H 0 1-cycbhexylethyI H 2-NM e 2 ,5-F 0 A-2553 H H H H 1-cycbhexylethyI H 2-NM e 2 ,6-F 0 A-2554 H H H H 0 1-cycbhexylethyl H 2-NMe 2 ,5-Me 0 A-2555 H H H H 0 1-cycbhexylethyl H 2-NMe 2 ,6-e 0 A-2556 H H H H 1-cycbhexylethyl H 2-ON,4-F 0 A-2557 H H H H 0 1-cycbhexylethyI H 2-ON 5-F 0 A-2558 H H H H 0 1-cycbhexylethyI H 2-ON,6-F 0 A-2559 fH H H H 1-cycbhexylethyl H 2-ON,6-Me 0 A-2560 H H I IHH 1-cycbhexylethyl H 2-ON,5-OMe 0
[0171]
[Table 46]
com pound R' R2 R R A R R' (R)m p A-2561 H H H H 0 1-cycbhexylethyl H 2-GN,6-OM e 0 A-2562 H H H H 0 1-cycbhexylethyl H 3-ON,6-Me A-2563 H H H H 0 1-cycbhexylethyl H 3-GN,6-OMe A-2564 H H H H i 0 1-cycbhexylethyl H 4-ON,2-M e 0 A-2565 H H H H 0 1-cycbhexylethyl H 4-N,2-OM e 0 A-2566 H H H H 0 1-ycbhexylethyl H 240 2,4-F 0 A-2567 H H H H f Di 1-ycbhexylethyl H 240 2 ,5-F 0 A-2568 H H H H 0 1-cycbhexylethyl H 2-N0 2 ,64 0 A-2569 H H H H H 0 1-cycbhexylethy I H 2-N0 2,4iAe 0 A-2570 H H H H 0 1-cycbhexylethy I H 2-NU 2,b e 0 A-2571 H H H H i 0 1-cycbhexylethy I H 2-NU 2,6-M e 0 A-2572 H H H H 0 1-cycbhexylethy I H 2-M e,4,b-F 2 0 A-2573 H H H H H 1-ycbhexylethyI H 2-M e,6-Et 0 A-2574 H H H H 0 1-cycbhexylethy I H 2-cyclopropyl,6-OM e 0 A-2575 H H H H 0 1-cycbhexylethyI H 2- e,b-Et 0 A-2576 H H H H 0 E -ycbhexylethyl H 2,6-t2 0 A-2577 H H H H 0 1-cycbhexylethy I H 2-Et,6-F 0 A-2578 H H H H 0 1-cycbhexylethyI H 2-GH 20H 3,6- I 0 A-2579 H H H H 1-cy lobhexylethyI H 2 H 2GH2H 3 0 A-2580 H H H H 0 1-cycobhexylethy I H 2-GH 2 NM e 2 0 A-2581 H H H H H 0 H 2C=UH H H 0 A-2582 H H H H HD0 CH 2C =H H 2-F 0 A-2583 H H H H 0 CH 2C =H H 2-Cl 0 A-258 Hf4 H H H i 0 CH 2OEUH H 2-Br 0 A-2585 H H H H f0 GH 2GECH H 2-OH 0 A-2586 H H H H H GH 2GEUH H 2-M e 0 A-2587 H H H H H0f GH2GEH H 2-Et 0 A-2588 H H H H i 0 CH 2 G=H H 2-Pr 0 A-2589 H H H H 0 CH 2CEUH H 2-F 3 0 A-2590 H H H H 0 CH 2CEUH H 2-H F 2 A-2591 H H H H 0 CH 2CEUH H 2-GH 2F 0
A-2592 H H H H 0 CH 2OEUH H 2-GF 2O I 0 A-2593 H H H H H 0 CH 2C =H H 2-cycbpropy1 0 A-2594 H H H H H CH 2CCH H 2-ycobbutyl 0 A-2595 H H H H 0 CH 2C =H H 2-cycbpentyl 0 A-2596 H H H H D E CH 2GEUH H 2-ethenyl1 A-2597 H H H H ifEf H2GEUH H 2-alyl 0 A-2598 H H H H D0 H 2C=UH H 2-(prop-1-en-1-y D 0 A-2599 H H H H 0 CH 2 G=H H 2-(trifLloroethenyD 0 A-2600 H H H H H 0 CH 2CEUH H 2-0M e 0 A-2601 H H H HD 0H 2C=UH H 2-OEt 0 A-2602 H H H HD 0H 2C=UH H 2-OPr 0 A-2603 H H H H f0 CH 2GECH H 2-0 (/-Pr) 0 A-2604 H H H H H CH 2GECH H 2-0GH3 A-2605 H H H H WD0i GH 2GUH H 2-CHH 2 0
A-2606 H H H H f0 GH 2GCS'N H 2-(cycbpropy bxy) 0 A-2607 H H H H 0 OH20=UH H 2-(cycobbuty bxy) 0 A-2608 H H H H 0 CH 2CGUH H 2-(cycbpenty bxy) 0 A-2609 H H H H O 0H20EUH H 2-((2,2-d bh brocycbpropy I)oxy) 0 A-2610 H H H H H CH 2CCH H 2-(oxiran-2-y D 0 A-2611 H H H H D0H 2C=H H 2-SMe 0 A-2612 H H H H f0 GH 2GECH H 3-SMe 0 A-2613 H H H H f0 GH 2GECH H 2-S(= 0)Me 0 A-2614 H H H H D0H 2C=UH H 3-S(=0)M e 0 A-2615 H H H H H 0 H 2C==H H 2-S(= 0) 2Me 0 A-2616 H H H H 0 E CH 2CUH H 3-S =0) 2Me 0 A-261/ H H H H 7Uif f 2 =H UH H 2-SOF 3 0
[0172]
[Table 47]
com pound R' R2 R R A R R' (R)m p A-2618 H H H H 0 CH 2OEUH H 3-S0CF A-2619 H H H H H 0 H 2C=UH H 3-S (= 0)CF3 0 A-2620 H H H H O 0H20=UH H 3-SCF(F32 0 A-2621 H H H H H CH 2CCH H 2-(cycbpropy th) 0 A-2622 H H H H 0 CH 2C=UH H 2-(cycbpropylsu finy D 0 A-2623 H H H H O 0H20==H H 2-(cycbpropybu fonyD 0 A-2624 H H H H D0H 2C=UH H 2-G (=0)M e 0 A-2625 H H H H 0 CH 2C=UH H 2-GH C = )H 3 2 0 A-2626 H H H H 0 CH 2OEUH H 2-GH 2C (= )0F 3 A-2627 H H H H DF if GH2G=CH H 2-CH 2H F A-2628 H H H H i 0 CH 2CCH H 2-GH 20H 3 A-2629 H H H H Ei CD H 2CCH H 2-H 20H 2CH 3 0
A-2630 H H H H H CH 2CCH H 2-CH 2SCH 3 0 A-2631 H H H H D0H 2C=UH H 2-GH2S=0 )H3 0
A-2632 H H H H 0 H 2C=UH H 2-GH 2 S(= 0) 2 CH 3 A-2633 H H H H i 0 CH 2CEH H 2-(benzy bxy) 0 A-2634 H H H H H0 GH 2GECH H 2-NH 2 A-2635 H H H H 0 CH 20=UH H 2-NH Me A-2636 H H H H f0 GH 2GECH H 2 NM e) 2 0 A-2637 H H H H 0 CH 2C =H H 2-0,3-d bxoan-2-yD 0 A-2638 H H H H H 0 H 2C=UH H 2-0,3-dbxan-2-y D 0 A-2639 H H H H f0 0H 20EUH H 2-1H -i idazo 2-yD 0 A-2640 H H H H 0 0H 20EGH H 2-(thiazob-2-y) 0 A-2641 H H H H i 0 0H 20EUH H 2-(oxazo1-2-yD 0 A-2642 H H H H H0 GH 2GECH H 2-GH= N0H 0 A-2643 H H H H f0 GH 2GECH H 2-0H= NUM e 0 A-2644 H H H H H GH2G =CH H 2-(4,b-dihydro-3-soxazo' 0 A-2645 H H H H i 0 CH 2 0EUH H 2-N 0 A-2646 H H H HD 0H 2 H C==H 2-N2O 0 A-2647 H H H H 0 CH 2C =H H 2-F,6-GI 0 A-2648 H H H H D0H2C=UH H 2-F,6-Me 0 A-2649 H H H H D0 H 2C=UH H 3-F,6-Me 0 A-2650 H H H H H 0 CH 2C=UH H 4-F,2-M e 0 A-2651 H H H H 0 CH 2CCH H 2-F,6-UMe 0 A-2652 H H H H 0 H 20EUH H 3-F,6-M e 0 A-2653 H H H H E D CH 2CCH H 2,6-C A-2654 H H H H H CH 2CCH H 2-L1,6-M e 0 A-2655 H H H H 0 CH 2C=UH H 3- I,6-M e 0 A-2656 H H H H D0 H 2C=UH H 4-I,2-M e 0 A-2657 H H H H H 0 CH 2C =H H 2- Ib-F 3 0 A-2658 H H H H D0H2C==H H 2-G I,6-GF 3 0 A-2659 H H H H D0H2C=UH H 2- I,6-0M e 0 A-2660 H H H H H CH 2CCH H 3-1,6-0Me 0 A-2661 H H H H E F CH 2CCH H 4-1,2-0Me 0 A-2662 H H H H E D CH 2CCH H 2,4-M e 2 0 A-2663 H H H H H CH 2C =CH H Z,b-M e 2 0
A-2664 H H H HD 0H C=UH 2 H 2, 6 - Me2 0 A-2665 H H H H 0 CH 2C =H H 2-M e,4-GF 3 0 A-2666 H H H H D0H 2C=UH H 2-M e,b-UF3 0 A-2667 H H H H E0 C H 2CCH H 2-M e,6-F 3 0 A-2668 H H H H 0H2C==H H D 2-M e,4-0Me A-2669 H H H H H CH 2CCH H 2-M e,b-OMe 0 A-2670 H H H H H CH 2CCH H 2-M e,6-OMe 0 A-2671 H H H H E D CH 2C=UH H 3-M e,6-OMe 0 A-2672 H H H H H 0 H 2C==H H 4-M e,2-OMe 0 A-2673 H H H H H CH 2G=CH H 2,5-UMe 2 0 A-2674 H H H H H 0 H 2GEUH H 2,6-0M e 2 0
[0173]
[Table 48]
com pound R' R2 R R A R R' (R)m p A-2675 H H H H 0 0H 20 =H H 2-UMe,6-F 3 0 A-2676 H H H H H 0 H 2C =H H 2-CHF 2,b-F 0 A-2677 H H H H 0 CH 2C =H H 2-CHF 2,6-F 0 A-2678 H H H H i 0 CH 2C CH H 2-CHF 2,b-M e 0 A-2679 H H H H D 0H2C=H H 2-CHF2,6-Me 0 A-2680 H H H H D 0 H2C=H H 2-cycbpropylb-F 0 A-2681 H H H H ifD= H20 H H 2-cycbpropyl,6-F 0 A-2682 H H H H O 0H20 =H H 2-cyclopropylb-Me 0 A-2683 H H H H H 0 OH20 =H H 2-cyclopropyl,6-Me 0 A-2684 H H H H D if 0 GH2CH H 2-ethenyl,6-F 0 A-2685 H H H H 0 CH 2C CH H 2-ethenyl,6-Me 0 A-2686 H H H H D f 0 GH2CCH H 2-OEt,b-F A-2687 H H H H i CH 2C CH H 2-Et,6-F 0 A-2688 H H H H D0H 2C =H H 2-OEt,b-CI 0 A-2689 H H H H D0H 2C =H H 2-OEt,6-CI 0 A-2690 H H HHif0f GH2GGH H 2-UEt,b-Me 0 A-2691 H H H H f0 GH 2G GH H 2-UEt,6-Me 0 A-2692 H H H H D0 H 20 =H H 2-CH2,b-F 0 A-2693 H H H H i0 GH 2G GH H 2-CHH 2,6- 0 A-2694 H H H H 0 CH 2C H H 2-CH F 2 ,b-M e 0 A-269b H H H H i i0 CH2C H H 2-UCHF2,6-M e 0 A-2696 H H H H f0 OH20 =H H 2-(cycobpropyloxy),b-F 0 A-2697 H H H H 0 OH20 H H 2-(cycbpropyloxy),6-F 0 A-2698 H H H H f0 OH20 =H H 2-(cyclopropybxy),b-M e 0 A-2699 H H H H GH2 CH O H 2-(cyclopropybxy),6-M e 0 A-2700 H H H H iff GH2CCH H 2-SMe,b-F 0 A-2701 H H H H iff CH2CH H 2-SMe,6-F 0 A-2702 H H H H H0iH20 ==GH H 2-SMe,b-Me 0 A-2703 H H H H D 0H 2C =H H 2-SMe,6-M e 0 A-2704 H H H H D 0H2C=H H 2-S(=0)Me,b-F 0 A-2705 H H H H iff CH2H H 2-S(=0)Me,6-F 0 A-2706 H H H H D 0 H2C=H H 2-S(=0)Me,b-Me 0 A-2707 H H H H f0 0H 2C =H H 2-S(=0)Me,6-Me 0 A-2708 H H H H H CH 2C CH H 2-S(=U) 2Me,b-F A-2709 H H H H D0H 2C =H H 2-S(=0) 2Me,6-F 0 A-2710 H H H H D CH 2C CH H 2-S(=U) 2 Me,5-M e 0 A-2711 H H H H 0 CH 2C CH H 2-S(=U) 2 Me,6-M e 0 A-2712 H H H HD 0H 2C =H H 2-SC3,b-F 0 A-2713 H H H H D0 H 2C =H H 2-SC13,6-F 0 A-2714 H H H H H 0 CH 2C =H H 2-S0F 3 ,b-M e 0 A-271b H H H H 0 CH 2C =H H 2-S0F 3 ,6-Me 0 A-2716 H H H H 0 0H 2C =H H 2-S(=0)03,b-F 0 A-2717 H H H H i CH 2C CH H 2-S(=U)GF 3 ,6-F 0 A-2718 H H H H H CH 2C CH H 2-S(=U)CF 3 ,b-M e 0 A-2719 H H H H D CH 2C CH H 2-S =U)CF 3,6-M e 0 A-2720 H H H H H CH 2C CH H 2-S(=U) 203,b-F A-2721 H H H H D0H 2C =H H 2-S(=0)20F3,6-F 0 A-2722 H H H H D0 H 2C =H H 2-S(=0)20F3,b-M e 0 A-2723 H H H H D0 H 2C =H H 2-S(=U) 20F 3,6-M e 0 A-2724 H H H H O GH2 CH H 2-(cycbpropylthlo),b-F 0 A-272b H H H H 0 OH20 =H H 2-(cycbpropylthb),6-F F A-2726 H H H H H GH 2 CH H 2-(cycbpropylthio),b-M e 0 A-2727 H H H H iff GH2CH H 2-(cycbpropylthio),6-M e 0 A-2728 H H H H O 0H2O =H H 2-C(=0)Me,b-F 0 A-2729 H H H H f0 OH 2 =CH H 2-C(=0)Me,6-F 0 A-2730 H H H H f0 GH 2G GH H 2-C(=U)Me,b-M e 0 A-2731 H H H H H 0 H 2G H H 2-U(=0)Me,6-M e 0
[0174]
[Table 49]
com pound R' R2 R R A R R' (R)m p A-2732 H H H H 0 CH 2C=H H 2-OH 2 OHb-F 0 A-2733 H H H H H 0 CH 2C=H H 2-OH 2UH,6-F 0 A-2734 H H H H 0 CH 2C=H H 2-CH 2OH,b-Me 0 A-2735 H H H H i 0 GH 2 CH H 2-GH 2UN,6-M e 0 A-2736 H H H H 0 CH 2C=H H 2-OH 20H 3 ,4-F 0 A-2737 H H H H 0 CH 2C H H 2-OH 20H 3 ,b-F 0 A-2738 H H H H D CH 2C =H H 2-OH 20H 3 ,6-F 0 A-2739 H H H H D CH 2C =H H 2-OH 2OCH 3 ,4-Me 0 A-274 0 H H H H 0 CH 2C =H H 2-OH 2OCH 3 ,b-Me 0 A-2741 H H H H D GH 2 CH H 2-CH 2U0H 3 ,6-M e 0 A-2742 H H H H i 0 GH 2 CH H 2-00(=U)GH 3 ,b-H A-2743 H H H H D CH 2C CH H 2-0(=U)GH 3,6-F 0 A-2744 H H H H H CH 2C CH H 2-00(=U)GH 3 ,b-M e 0 A-2745 H H H H 0 CH 2C H H 2-0(=U)CH 3 ,6-M e 0 A-2746 H H H H D CH 2C =H H 2-OS(=O) 2CH 3 ,b- 0 A-2747 H H H H H0= H 2G GH H 2-OS(=U) 2CH3,6-F 0 A-2748 H H H H H GH 2G GH H 2-OS(=U) 2CH 3,b-M e 0 A-2749 H H H H D CH 2C =H H 2-OS(=U) 2CH 3,6-M e 0 A-2750 H H H H f0 GH 2G GH H 2-GH 2S0H 3,b-H 0 A-2751 H H H H 0 CH 2C H H 2-OH 2 SCH 3 ,6-F 0 A-2752 H H H H f0 CH 2C H H 2-OH 2SCH 3,b-Me 0 A-2753 H H H H H CH 2C =H H 2-OH 2SCH 3,6-Me 0 A-2754 H H H H D CH 2C =H H 2-NM e 2 ,b-F 0 A-2755 H H H H f0 CH 2C H H 2-NM e 2 ,6-F 0 A-2756 H H H H F GH 2 CH H 2-NMe 2 ,b-M e 0 A-2757 H H H H iff GH2CH H 2-NMe2,6-M e 0 A-2758 H H H H H7f GH 2 CH H 2-ON,4-F 0 A-2759 H H H H i 0 CH 2C=H H 2-ONb-F 0 A-2760 H H H H D CH 2C=H H 2-ON,6-F 0 A-2761 H H H H 0 CH 2C H H 2-ON,6-M e 0 A-2762 H H H H D CH 2C =H H 2-ON5-0Me 0 A-2763 H H H H D CH 2C=H H 2-ON,6-0Me 0 A-2764 H H H H H 0 CH 2C=H H 3-ON,6-M e 0 A-2765 H H H H f0 GH 2 CH H 3-ON,6-OMe 0 A-2766 H H H H D CH 2C=H H 4-ON,2-M e 0 A-2767 H H H H GH 2 CH H 4-ON,2-OMe 0 A-2768 H H H H H GH 2 CH H 2-N0 2 ,4-F 0 A-2769 H H H H D CH 2C =H H 2-N0 2 ,b-F 0
A-2770 H H H H D CH 2C =H H 2-N0 2,6-F 0 A-2//1 H H H H H 0 CH 2C=H H 2-N0 2,4-M e 0 A-2772 H H H H D CH 2C =H H 2-NU 2,b-Me 0 A-2773 H H H H D CH 2C =H H 2-NU 2,6-Me 0 A-2774 H H H H GH 2 CH H 2-M e,4,b-F 2 A-277b H H H H GH 2 CH H 2-Me,6-Et 0 A-2776 H H H H OH 2G CH H 2-cyclopropyl,6-OMe 0 A-2777 H H H H iff GH2CH H 2-Me,b-Et 0 A-2778 H H H H D CH 2C =H H 2,6-Et2 0 A-2779 H H H H D CH 2C=H H 2-Et,6-F 0 A-2780 H H H H D CH 2C =H H 2-OH 20H 3 ,6-I 0 A-2781 H H H H H GH 2 CH H 2-GH 20H 2CH 3 ,6-C 1F A-2782 H H H H D CH 2C =H H 2-OH 2 NMe 2 0 A-2783 H H H H H OH H H 0 A-2784 H H H H H OH H 2-F 0 A-278b H H H H D OH H 2-C 0 A-2786 H H H H H OH H 2-Br 0 A-2787 H H H H HD0 OH H 2-OH 0 A-2788 H f FIFH OH H 2-M e
[0175]
[Table 50]
com pound RI R2 R R R A R R' (R)m P A-2789 i H H H H H0 OH H 2-Et 0 A-2790 H H H H H 0 OH H 2-Pr 0 A-2791 H H H H H 0 OH H 2-C F, A-2792 H H H H H 0 OH H 2-CHF 2 0 A-2793 H H H H H 0 OH H 2-CH 2F 0 A-2794 H H H H H 0 0H H 2-CF 2C1 0 A-2795 H H H H H 0 0H H 2-cycbpropyl 0 A-2796 H H H H H 0 0H H 2-cycobbutyl 0 A-2797 H H H H H 0 0H H 2-cycbpentyl 0 A-2798 H H H H H 0 0H H 2-ethenyl 0 A-2799 H H H H H 0 0H H 2-allyl 0 A-2800 H H H H H 0 0H H 2-(prop-1-en-1-y) 0 A-2801 H H H H H 0 0H H 2-(trifloroethenyl 0 A-2802 H H H H H 0 OH H 2-0Me 0 A-2803 H H H H H 0 OH H 2-0Et 0 A-2804 H H H H H 0 0H H 2-0Pr 0 A-2805 H H H H H 0 0H H 2-0(/-Pr) 0 A-2806 H H H H H 0 0H H 2-0CF3 0 A-2807 H H H H H 0 0H H 2-OCHF 2 0 A-2808 H H H H H 0 0H H 2-(cycbpropy bxy) 0 A-2809 H H H H H 0 0H H 2-(cycbbutybxy) 0 A-2810 H H H H H 0 0H H 2-(cycbpentybxy) 0 A-2811 H H H H H 0 0H H 2-((2,2-dichbrocycobpropyl)oxy) 0 A-2812 H H H H H 0 0H H 2-(oxiran-2-yl 0 A-2813 H H H H H 0 0H H 2-SMe 0 A-2814 H H H H H 0 0H H 3-SMe 0 A-2815 H H H H H 0 0H H 2-S(=0)Me 0 A-2816 H H H H H 0 0H H 3-S(=0)Me 0 A-2817 H H H H H 0 0H H 2-S(=0) 2Me 0 A-2818 H H H H H 0 0H H 3-S(=0) 2Me 0 A-2819 H H H H H 0 0H H 2-SCF3 0 A-2820 H H H H H 0 0H H 3-SCF3 0 A-2821 H H H H H 0 0H H 3-S(=0)CF3 0 A-2822 H H H H H 0 0H H 3-SCF(CF 3 ) 2 0 A-2823 H H H H H 0 0H H 2-(cycobpropylthio) 0 A-2824 H H H H H 0 0H H 2-(cycbpropylsulfinyD 0 A-2825 H H H H H 0 0H H 2-(cycbpropylsulfonyl) 0 A-2826 H H H H H 0 0H H 2-C(=0)Me 0 A-2827 H H H H H 0 0H H 2-CH 2C(=0)CH 3 0 A-2828 H H H H H 0 0H H 2-CH 2C(=0)CF 3 0 A-2829 H H H H H 0 0H H 2-CH 2 0H 0 A-2830 H H H H H 0 0H H 2-CH 2 0CH 3 0 A-2831 H H H H H 0 0H H 2-CH 2 00H 20H 3 0 A-2832 H H H H H 0 0H H 2-CH 2SCH 3 0 A-2833 H H H H H 0 OH H 2-0H2 S(=O0H 3 0 A-2834 H H H H H 0 OH H 2-2H 2S(=0 3 0 A-2835 H H H H H 0 OH H 2-(benzybxy) 0 A-2836 H H H H H 0 OH H 2-NH 2 0 A-2837 H H H H H 0 OH H 2-NH M e 0 A-2838 H H H H H 0 OH H 2-NMe) 2 0 A-2839 H H H H H 0 OH H 2-(1,3-dioxolan-2-y) 0 A-2840 H H H H H 0 OH H 2-(1,3-dioxan-2-yl 0 A-2841 H H H H H 0 OH H 2-(1H-in idazol-2-yD 0 A-2842 H H H H H 0 OH H 2-(thiazol-2-yl) 0 A-2843 H H H H H 0 OH H 2-(oxazol-2-yD 0 A-2844 H H HIH H 0 OH H 2-CH=N0H 0 A-2845 ifHFH H H 0 OH H 2-CH= NOM e 0
[0176]
[Table 51]
com pound RI R2 R R R A R R' (R)m P A-2846 H H H H H 0 0H H 2-(4,5-dihydro-3-isoxazolyD 0 A-2847 H H H H H 0 0H H 2-CN 0 A-2848 H H H H H 0 0H H 2-N0 2 A-2849 H H H H H 0 0H H 2-F,6-CI 0 A-2850 H H H H H 0 0H H 2-F,6-Me 0 A-2851 H H H H H 0 OH H 3-F,6-Me 0 A-2852 H H H H H 0 OH H 4-F,2-Me 0 A-2853 H H H H H 0 0H H 2-F,6-0Me 0 A-2854 H H H H H 0 0H H 3-F,6-0Me 0 A-2855 H H H H H 0 0H H 2,6-01 0 A-2856 H H H H H 0 0H H 2-C,6-Me 0 A-2857 H H H H H 0 0H H 3-C,6-Me 0 A-2858 H H H H H 0 0H H 4-C,2-Me 0 A-2859 H H H H H 0 0H H 2-C 1,5-CF, 0 A-2860 H H H H H 0 0H H 2-CI,6-CF, 0 A-2861 H H H H H 0 0H H 2-C,6-0Me 0 A-2862 H H H H H 0 0H H 3-C1,6-0Me 0 A-2863 H H H H H 0 0H H 4-CI,2-0Me 0 A-2864 H H H H H 0 0H H 2,4-Me 2 0 A-2865 H H H H H 0 0H H 2,5-M e 2 0 A-2866 H H H H H 0 0H H 2,6-M e 2 0 A-2867 H H H H H 0 0H H 2-M e,4-CF 3 0 A-2868 H H H H H 0 OH H 2-M e,5-CF3 0 A-2869 H H H H H 0 OH H 2-Me,6-CF3 0 A-2870 H H H H H 0 OH H 2-M e,4-0Me 0 A-2871 H H H H H 0 0H H 2-M e,5-0Me 0 A-2872 H H H H H 0 0H H 2-M e,6-0Me 0 A-2873 H H H H H 0 0H H 3-M e,6-0Me 0 A-2874 H H H H H 0 0H H 4-M e,2-0Me 0 A-2875 H H H H H 0 0H H 2,5-Me 2 0 A-2876 H H H H H 0 0H H 2,6-0Me 2 0 A-2877 H H H H H 0 0H H 2-0Me,6-CF3 0 A-2878 H H H H H 0 0H H 2-CHF 2,5-F 0 A-2879 H H H H H 0 0H H 2-CHF 2,6-F 0 A-2880 H H H H H 0 0H H 2-CHF 2,5-M e 0 A-2881 H H H H H 0 0H H 2-CHF 2,6-M e 0 A-2882 H H H H H 0 0H H 2-cycbpropyL,5-F 0 A-2883 H H H H H 0 0H H 2-cycbpropyL,6-F 0 A-2884 H H H H H 0 0H H 2-cyclopropyL,5-Me 0 A-2885 H H H H H 0 OH H 2-cyclopropyL,6-Me 0 A-2886 H H H H H 0 OH H 2-ethenyl,6-F 0 A-2887 H H H H H 0 OH H 2-ethenyl,6-Me 0 A-2888 H H H H H 0 OH H 2-0Et,5-F 0 A-2889 H H H H H 0 0H H 2-0Et,6-F 0 A-2890 H H H H H 0 0H H 2-0Et,5-CI 0 A-2891 H H H H H 0 0H H 2-0Et,6-CI 0 A-2892 H H H H H 0 0H H 2-0Et,5-Me 0 A-2893 H H H H H 0 0H H 2-0Et,6-M e 0 A-2894 H H H H H 0 0H H 2-0CHF 2,5-F 0 A-2895 H H H H H 0 0H H 2-0CHF 2,6-F 0 A-2896 H H H H H 0 0H H 2-OCHF 2 ,5-M e 0 A-2897 H H H H H 0 0H H 2-OCHF 2 ,6-Me 0 A-2898 H H H H H 0 0H H 2-(cycbpropyloxy),5-F 0 A-2899 H H H H H 0 OH H 2-(cycobpropyloxy),6-F 0 A-2900 H H H H H 0 OH H 2-(cyclopropyoxy),5-M e 0 A-2901 H H H H H 0 OH H 2-(cyclopropyloxy),6-M e 0 A-2902 H H H H 0 OH H 2-SMe,5-F 0
[0177]
[Table 52]
com pound R' R2 R R A R R' (R)m p A-2903 H H H H 0 0H H 2-SMe,6-F 0 A-2904 H H H H H 0 OH H 2-SMe,b-Me 0 A-2905 H H H H 0 OH H 2-SMe,6-Me A-2906 H H H H i 0 OH H 2-S(=U)Me,b-F 0 A-2907 H H H H 0 OH H 2-S(=0)Me,6-F 0 A-2908 H H H H 0 OH H 2-S(=0)Me,b-M e 0 A-2909 H H H H D OH H 2-S(=0)Me,6-M e 0 A-2910 H H H H 0 0H H 2-S(=U) 2Me,b-F 0 A-2911 H H H H 0 H OH 2-S(=U) 2Me,6-F 0 A-2912 H H H H 0 H OH 2-S(=0) 2 Meeb-Me 0 A-2913 H H H H i 0 H OH Z-S(=U) 2Me,6-e 0 A-2914 H H H H D H OH 2-SC3,b- A-2915 H H H H f0 H OH 2-SCF 3 ,6-F 0 A-2916 H H H H D H OH 2-SCF 3 ,b-M e 0 A-2917 H H H H 0 H OH 2-SCF 3 ,6-M e 0 A-2918 H H H H f0 H OH 2-St=U)GF 3 ,b-H 0 A-2919 H H H H f0 H OH 2-S=U)GF 3,6-F A-2920 H H H H O 0H H 2-S(=0)CF3,b-MAe 0 A-2921 H H H H 0 OH H Z-=U)GH 3,6-Me 0 A-2922 H H H H 0 OH H 2-S(=U) 2 0%3,b-F 0 A-2923 H H H H H 0 OH H 2-S(=U) 20F 3 ,6-F 0 A-2924 H H H H f0 OH H 2-S (=) 2 CF 3 ,b-M e 0 A-2925 H H H H 0 OH H 2-S(=U) 2CF 3 ,6-M e 0 A-2926 H H H H 0 OH H 2-(cycobpropylthb),b-F A-2927 H H H Hi i f OH H 2-(cycobpropylthb),6-F A-2928 H H H H i if OH H 2-(cycbpropylthio),b-M e 0 A-2929 H H H H i if OH H 2-(cycbpropylthio),6-M e 0 A-2930 H H H H i 0 OH H 2-C(=U)Me,b-F 0 A-2931 H H H H DOH H 2-C(=0)Me,6-F 0 A-2932 H H H H D OH H 2-C(=O)Me,b-M e 0 A-2933 H H H H DOH H 2-C(=O)Me,6-M e 0 A-2934 H H H H 0 0H H 2-CH 2UH,b-F 0 A-2935 H H H H H 0 OH H 2-CH 2UH,6-F 0 A-2936 H H H H OH H Z-GH 2 ,b-Me 0 A-2937 H H H H 0 OH H 2-CH 2UH,6-M e 0 A-2938 H H H H D OH H 2-GH 20H 3 ,4-F 0 A-2939 H H H H f0 OH H 2-GH 20H 3 ,b- 0 A-2940 H H H H D OH H 2-0H 20H 3 ,6-F 0 A-2941 H H H H D OH H 2-CH 20CH 3 ,4-Me 0 A-2942 H H H H H 0 OH H 2-CH 2UCH 3 ,b-Me 0 A-2943 H H H H D OH H 2-CH 2UCH 3 ,6-Me 0 A-2944 H H H H D OH H 2-U0(=U)0H 3 ,b-F 0 A-2945 H H H H f0 OH H 2-UG(=U)GH 3 ,6-F 0 A-2946 H H H H O UH H 2-00(=0)CH 3 ,b-M e F A-2947 H H H H D OH H 2-0G0(=U)CH 3,16-M e 0 A-2948 H H H H f0 OH H 2-UOS=0) 2 03,b-H 0 A-2949 H H H H D OH H 2-OS(=U) 2CH 3 ,6-F 0 A-2950 H H H H D OH H 2-OS(=U) 2CH 3,b-M e 0 A-2951 H H H H D OH H 2-OS(=U) 2CH 3,6-M e 0 A-2952 H H H H i OH H 2-CH 2SCH 3 ,b-H 0 A-2953 H H H H 0 0H H 2-CH 2 SCH 3 ,6-F 0 A-2954 H H H H HOH H 2-CH 2S0H 3,b-M e 0 A-2955 H H H H OH H 2-CH 2S0H 3,6-M e 0 A-2956 H H H H D OH H 2-NMe 2 ,b-F 0 A-2957 H H H H 0 H H 2-NMe 2 ,6-F 0 A-2958 H H H H O UH H 2-NMe 2 ,b-e A-2959 H H HIH 0 OH H 2-NMe 2 ,6-MAe 0
[0178]
[Table 53]
com pound R' R2 R R A R R' (R)m p A-2960 i H H HH 0 0H H 2-ON4-F 0 A-2961 H H H H H 0 OH H 2-Nb-F 0 A-2962 H H H H D OH H 2-ON,6-F A-2963 H H H H i 0 OH H 2-GN,6-Me 0 A-2964 H H H H 0 OH H 2-ON,b-OMe 0 A-2965 H H H H D OH H 2-ON,6-OMe 0 A-2966 H H H H D OH H 3-GN,6-Me 0 A-2967 H H H H 0 0H H 3-ON,6-OMe 0 A-2968 H H H H 0 OH H 4-GN,2-Me 0 A-2969 H H H H H 0 OH H 4-ON,2-OMe 0 A-2970 H H H H O UH H -N 2,4- 0 A-2971 H H H H D OH H -NU 2,b-H A-2972 H H H H i 0 OH H Z-U 2,- 0 A-2973 H H H H D OH H 2-N0 2,4-MvAe 0 A-2974 H H H H D OH H 2-N0 2,b-M e 0 A-2975 H H H H 0 H H 2-NU 2,6-e 0 A-2976 H H H H O UH H 2-M e,4,b-F 2 0 A-2977 H H H H 0 OH H 2-M e,6-Et 0 A-2978 H H H H OH H 2-cyclopropyl,6-OMe 0 A-2979 H H H H 0 OH H 2-M e,b-Et 0 A-2980 H H H H HD0 OH H 2,6-Et2 0 A-2981 H H H H f0 OH H 2-Et,6-F 0 A-2982 H H H H 0 OH H 2-OH 20H 3 ,6-I 0 A-2983 H H H H f0 OH H 2-OH 20H 2CH 3 ,6-OI 0 A-2984 H H H H HOH H 2-CH 2 NMe 2 0 A-2985 H H H H f0 0GH 20H 3 H H 0 A-2986 H H H H I UGH 20H 3 H 2-F 0 A-2987 H H H H Hif 0 UGH2CH3 H 2-CI 0 A-2988 H H H H D 0H 2 CH 3 H 2-Br 0 A-2989 H H H H 0 0GH 2 CH 3 H 2-OH 0 A-2990 H H H H D 0H 2 CH 3 H 2-M e 0 A-2991 H H H H 0 0H 2 CH 3 H 2-Et 0 A-2992 H H H H H 0 0H 2 CH 3 H 2-Pr 0 A-2993 H H H H F 0H 20H 3 H 2-GH 3 0
A-2994 H H H H 0 0H 2 CH 3 H 2-UHF 2 0
A-2995 H H H H D0 0 2 CH3 UCH H 2-GH 2F 0
A-2996 H H H H H UGH 20C 3 H 2-GH 201 0 A-2997 H H H H ifDf UGH2H3 H 2-cycbpropyl 0 A-2998 H H H H D 0H 2 CH 3 H 2-cycbbutyl 0 A-2999 H H H H H 0 0GH 2 CH 3 H 2-cycbpentyl 0 A-3000 H H H H D 0H 2 CH 3 H 2-ethenyl 0 A-3001 H H H H D 0 H 2 CH 3 H 2-allyl A-3002 H H H H H 0H 20H 3 H 2-(prop-1-en-1-yD A-3003 H H H H H UGH 2 0H 3 H 2-(trffbioroethenyD A-3004 H H H H D 0GH 20H 3 H 2-0Me A-3005 H H H H i 0GH 20H 3 H 2-UEt 0 A-3006 H H H H 0 0GH 2 CH 3 H 2-OPr 0 A-3007 H H H H 0 0GH 2 CH 3 H 2-0 (/-Pr) 0 A-3008 H H H H 0 0GH 2 CH 3 H 2-0G3 A-3009 H H H H Hi0 0GH 20H 3 H 2-CHF 2 A-3010 H H H H 0 0GH 2 CH 3 H 2-(cycbpropybxy) 0 A-3011 H H H H f0 0GH 20H 3 H 2-(cycobbutyloxy) 0 A-3012 H H H H H 0H 20H 3 H 2-(cycbpentybxy) 0 A-3013 H H H H 0 0GH 2 CH 3 H 2-((2,2-dichbrocycbpropy)oxy) 0 A-3014 H H H H f0 0GH 2 CH 3 H 2-(oxiran-2-yD 0 A-3015 H H H H f0 0H 20H 3 H 2-SMe 0 A-3016 H H H H f0 UGH 20H 3 H 3-SMe 0
[0179]
[Table 54]
com pound R' R2 R R A R R' (R)m p A-3017 H H H H 0 UGH 2 CH 3 H 2-S (=0)M e 0 A-3018 H H H H 0 UH 2 CH 3 H 3-S (=U)Me A-3019 H H H H 0 UH 2 CH 3 H 2-S(= 0) 2M e A-3020 H H H H i 0 UGH 20H 3 H 3-S = ) 2 M e A-302 Hf1 H H H 0 UGH 2 CH 3 H 2-SGC3 A-3022 H H H H 0 UGH 2 CH 3 H 3-SGC3 A-3023 H H H H D UGH 2 CH 3 H 3-S (= 0) C3 A-3024 H H H H 0 UGH 2 CH 3 H 3-SCF(CF3) 2 A-3025 H H H H H 0 UGH 2 CH 3 H 2-(cycobpropy thb) 0 A-3026 H H H H D F 0 UGH20H 3 H 2-(cycbpropylsu finy D 0 A-3027 H H H H i 0 0GH 20H 3 H 2-(cycobpropy u fony D 0 A-3028 H H H H D 0H 20H 3 H 2-C (= 0)M e 0 A-3029 H H H H H 0H 20H 3 H 2-GH 2 0(= )H 3 0
A-3030 H H H H D 0H 2 CH 3 H 2-GH 2 (=0)CF U 3 A-3031 H H H H D 0H 2 CH 3 H 2-CH 2 UH 0 A-3032 H H H H f0 UH 20H 3 H 2-GH 20H 3 0
A-3033 H H H H H GH 20 3 H -GH 2 UGH2 0 3 A-3034 H H H H 0 0GH 2 CH 3 H 2-CH 2SCH 3 0 A-3035 H H H H f0 UH 0 3 2 H 2-CH 2S (= )H 3 0
A-3036 H H H H 0 0GH 2 CH 3 H 2-CH 2S(= 0) 2 CH 3 A-3037 H H H H 0 0H 2 CH 3 H 2-(benzy bxy) 0 A-3038 H H H H f0 0GH 2 CH 3 H 2-NH 2 0 A-3039 H H H H D 0H 2 CH 3 H 2-NH M e A-3040 H H H H f0 0GH 2 CH 3 H 2 MN e)2 0 A-3041 H H H H H 0H 20H 3 H 2-(1,3-d bxoan-2-yD 0 A-3042 H H H H H 0H 20H 3 H 2-0,3-dbxan-2-y D F A-3043 H H H H H 0H 20H 3 H 2-(1H- idazokE2-yD 0 A-3044 H H H H i 0 UGH 2 CH 3 H 2-(thiazo b-2-y1 0 A-3045 H H H H 0 H 2 CH 3 H 2-(oxazol-2-y D0 A-3046 H H H H 0 0GH 2 CH 3 H 2-CH= N0H 0 A-3047 H H H H 0 0H 2 CH 3 H 2-CH= NOM e 0 A-3048 H H H H 0 0GH 2 CH 3 H 2-(4,b-dihydro-3-oxazo D 0 A-3049 H H H H H 0 0H 2 CH 3 H 2-CN 0 A-3050 H H H H H UGH 2 0H 3 H 2-NO 2 0
A-3051 H H H H 0 0GH 2 CH 3 H 2-F,6-GI 0 A-3052 H H H H Ef 0DH2 GH 3 H 2-F,6-i e 0 A-3053 H H H H E 0 0 H 2 GH 3 H 3-F,6-i e 0 A-3054 H H H H 0 0H 2 CH 3 H 4-F,2-M e 0 A-3055 H H H H 0 0H 2 CH 3 H 2-F,6-M e 0 A-3056 H H H H H 0 0H 2 CH 3 H 3-F,6-M e 0 A-3057 H H H H 0 0H 2 CH 3 H 2,6-C 0 A-3058 H H H H D 0H 2 CH 3 H 2- 1,6-M e 0 A-3059 H H H H f0 0H 20H 3 H 3- 1,6-M e 0 A-3060 H H H H H 0H 20H 3 H 4-01,2-M e 0 A-3061 H H H H E D H2 GH 3 H Z-jlb-CH 3 0 A-3062 H H H H H GH 2 0 3 H Z-C16-CH 3 0 A-3063 H H H H D0 0GH 2 CH 3 H 2-C 1,6-0M e 0 A-3064 H H H H 0 0H 2 CH 3 H 3-C 1,6-0M e 0 A-3065 H H H H 0 0H 2 CH 3 H 4-C 1,2-0M e 0 A-3066 H H H H f0 UH 2 0 3 H 2,40 e2 F A-3067 A-06/H H HH H H H 0D 0HGHCH3 20H 3 HH 2,54 2,b-M e2 e2 |0 A-3068 H H H H F 0H 20H 3 H 2,6-M e 2 0
A-3069 H H H H f Di 0H 2 CH 3 H 2-M e,4-CF 3 0 A-3070 H H H H 0 0H 2 CH 3 H 2-M e,b-CF 3 0 A-3071 H H H H 0E 0 H 2 GH 3 H 2-M e,6-CF 3 0 A-3072 H H H H ifi0 UGH2H3 H 2 -Me,4-UMe 0 A-3073 ifiFiFi
[0H8 0CH 2 3 H 2-0 e]-OMe 0
[0180]
[Table 55]
com pound R' R2 R R A R R' (R)m p A-3074-i H H H H 0 UGH2CH3 H 2-Me,6-OMe 0 A-3075 H H H H H 0 UGH 2 CH 3 H 3 -Me,6-UMe 0 A-3076 H H H H 0 UH 2 CH 3 H 4-M e,2-0M e A-3077 H H H H if 0 0GH 2 GH 3 H 2,b-UMe 2 0 A-3078 H H H H 0 UGH 2 CH 3 H 2,6-0M e 2 0 A-3079 H H H H 0 UGH 2 CH 3 H 2-0Me,6-F 3 0 A-3080 H H H H 0 UGH 2 CH 3 H 2-CHF 2,b-F 0 A-3081 H H H H 0 0GH 2 CH 3 H 2-CHF 2,6-F 0 A-3082 H H H H 0 0GH 2 CH 3 H 2-CHF 2,b-Me 0 A-3083 H H H H Dif 0 UH20H3 H 2-CH2,6-M e 0 A-3084 H H H H i 0 0GH 20H 3 H 2-cycbpropy 1,b-F A-3085 H H H H D 0GH 20H 3 H 2-cycbpropy 1,6-F 0 A-3086 H H H H 0GH 20H 3 H 2-cyclopropylb-M e 0 A-3087 H H H H 0 0H 2 CH 3 H 2-cyclopropyl,6-M e 0 A-3088 H H H H 0 UGH 2 CH 3 H 2-ethenyl,6-F 0 A-3089 H H H H El a "0GH2 GH 3 H 2-ethenyl,6-M e 0 A-3090 H H H H f0 UGH 20H 3 H 2-0Etb-F 0 A-3091 H H H H 0 0GH 2 CH 3 H 2-0Et6-F 0 A-3092 H H H H 0UH 2 0H 3 H 2-0Etb-CI 1 A-3093 H H H H 0 0H 2 CH 3 H 2-0Et6-C I 0 A-3094 H H H H H 0H 2 CH 3 H 2-0Etb-M e 0 A-3095 H H H H 0 0H 2 CH 3 H 2-0Et6-M e 0 A-3096 H H H H 0 0H 2 CH 3 H 2-0CH F 2,b-F F A-3097 H H H H Hi0 0GH 2 CH 3 H 2-0CH F 2,6-F 0 A-3098 H H H H H 0H 20H 3 H 2-GH H2 b-M e 0 A-3099 H H H H H 0H 20H 3 H 2-GH h 2 6-M e 0 A-3100 H H H H H 0H 20H 3 H 2-(cycbpropyloxy),b-F 0 A-3101 H H H H i 0 0GH 2 CH 3 H 2-(cycbpropyloxy),6-F 0 A-3102 H H H H D UGH 2 CH 3 H 2-(cyclopropy loxy),b-M e 0 A-3103 H H H H 0 UGH 2 CH 3 H 2-(cyclopropy bxy),6-M e 0 A-3104 H H H H D UGH 2 CH 3 H 2-SM e,b-F 0 A-3105 H H H H 0 0H 2 CH 3 H 2-SM e,6-F 0 A-3106 H H H H H 0 0H 2 CH 3 H 2-SM e,b-M e 0 A-3107 H H H H 0 0H 20H 3 H 2-SMe,6-M e 0 A-3108 H H H H D 0H 2 CH 3 H 2-S(=0)Me,b-F 0 A-3109 H H H H D UGH 20C 3 H 2-S(=0)Me,6-F 0 A-3110 H H H H H 0H 20H 3 H 2-S = U)Meb- e 0 A-3111 H H H H D 0H 2 CH 3 H 2-S(=0)Me,6-M e 0 A-3112 H H H H D 0H 2 CH 3 H 2-S(= 0) 2 Me,b-F 0 A-3113 H H H H D 0H 2 CH 3 H 2-S(= 0) 2 Me,6-F 0 A-3114 H H H H D 0H 2 CH 3 H 2-S(= 0M eb-M e 0 A-3115 H H H H 0 UGH 2 H 3 H 2-S (=0 M e,6 -Me 0 A-3116 H H H H Hi 0GH 20H 3 H 2-SCF 3 ,b-H A-311/ H H H HF UH 2 0H 3 H 2-SC 3 ,6-1 0 A-3118 H H H H D UGH 20H 3 H 2-SCF 3 ,b-M e 0 A-3119 H H H H D UGH 20H 3 H 2-SCF 3 ,6-M e 0 A-3120 H H H H 0 0H 2 CH 3 H 2-S =U)C3,b-F 0 A-3121 H H H H 0 0H 2 CH 3 H 2-S =U)0F 3,6-F 0 A-3122 H H H H 0 0H 2 CH 3 H 2-S(= )CF 3 ,b-M e 0 A-3123 H H H H f0 0H 20H 3 H 2-S =U)CF 3 ,6-M e 0 A-3124 H H H H 0 0H 2 CH 3 H 2-S (=0) 2 G3,b-F 0 A-3125 H H H H Hi 0GH 20H 3 H 2-S (=0) 2 F 3 ,6-F A-3126 H H H H 0GH 20H 3 H 2-S =0) 2CF 3 ,b-M e A-3127 H H H H 0 0H 2 CH 3 H 2-S =0) 2 CF 3 ,6-M e 0 A-3128 H H H H H 0H 2 CH 3 H 2-(cycobpropylth b),b-F 0 A-3129 H H H H H UGH 20H 3 H 2-(cycobpropylth b),6-F 0 A-3130 H f HF f H UH 2 CH 3 H 2-(cycobpropy tio),b-M e 0
[0181]
[Table 56]
com pound R' R2 R R A R R' (R)m p A-3131 H H H H 0 UGH 2 CH 3 H 2-(cycbpropy thio),6-M e 0 A-3132 H H H H 0 UH 2 CH 3 H 2- 0(= )M e,b-F 0 A-3133 H H H H 0 UH 2 CH 3 H 2- 0(= )M e,6-F W A-3134 H H H H H UGH 20H 3 H 2-(= O)M e,b-M e 0 A-3135 H H H H 0 UGH 2 CH 3 H 2-(=O )M e,6-M e 0 A-3136 H H H H 0 UGH 2 CH 3 H 2-GH 2UH,b-F 0 A-3137 H H H H D UGH 2 CH 3 H 2-GH 2UH,6-F 0 A-3138 H H H H 0 UGH 2 CH 3 H 2-CH 2UH,b5-M e 0 A-3139 H H H H H 0 UGH 2 CH 3 H 2-CH 2UH,6 -Me 0 A-3140 H H H H Dif 0 UH20H 3 H 2-GH20H 34-F A-3141 H H H H i 0 0GH 20H 3 H 2-GH 20H 3 ,b-H 0
A-3142 H H H H D 0GH 20H 3 H 2-GH 20H 3,6-F 0 A-3143 H H H H H 0H 20H 3 H 2-CH 20CH 3 ,4-M e 0 A-3144 H H H H 0 0GH 2 CH 3 H 2-0H 20CH 3 ,b- e 0 A-3145 H H H H 0 0GH 2 CH 3 H 2-0H 20CH 3 ,6-Me 0 A-3146 H H H H E 00H 2 GH 3 H 2-0C(= 0)GH 3 ,b-H 0
A-3147 H H H H f0 0GH 20H 3 H 2-0C(= 0)GH 3,6-F A-3148 H H H H E D 0H 2 CH 3 H 2-0C(=0)CH 3 b-M e 0 A-3149 H H H H I UGH 20H 3 H 2-0CG(= 0)CH 3 6-M e A-3150 H H H H 0 0GH 2 CH 3 H 2-0S =0 ) 2 H 3 ,b- 0 A-3151 H H H H Hi0 0GH 2 CH 3 H 2-0S T=0 2 GH 3 ,6-F 0 A-3152 H H H H H 0H 2 CH 3 H 2-0S(= 0) 2 H 3,b-M e 0 A-3153 H H H H D 0H 2 CH 3 H 2-S(= 0) 2 CH 3,6-M e 0 A-3154 H H H H Hi0 0GH 2 CH 3 H 2-0H 2 S0H 3 ,b-4 0 A-31 55 H H H H Ei 0 CH 2 GH 3 H 2-CH 2SCH 3 6-F A-3156 H H H H 0GH 20H 3 H 2-CH 2SCH 3,b-M e 0 A-3157 H H H H 0GH 20H 3 H 2-CH 2SCH 3,6-Me 0 A-3158 H H H H i 0 0GH 2 CH 3 H 2-NM e 2 ,b-F 0 A-3159 H H H H D 0H 2 CH 3 H 2-NM e 2 ,6-F 0 A-3160 H H H H 0 0GH 2 CH 3 H 2NM e 2 ,b-M e 0 A-3161 H H H H D 0H 2 CH 3 H 2-NM e 2 ,6-M e 0 A-3162 H H H H 0 0GH 2 CH 3 H 2-ON,4-F 0 A-3163 H H H H f0 0H 2 CH 3 H 2-ONb-F 0 A-3164 H H H H f0 0H 20H 3 H 2-ON,6-F 0 A-3165 H H H H 0 0H 2 CH 3 H 2-ON,6-M e 0 A-3166 H H H H D UGH 20C 3 H 2-ON,b-0Me 0 A-3167 H H H H ifFf UGH203 H 2-ON,6-0M e 0 A-3168 H H H H D 0H 2 CH 3 H 3-ON,6-M e 0 A-3169 H H H H 0 0H 2 CH 3 H 3-ON,6-OMe 0 A-3170 H H H H H 0 0H 2 CH 3 H 4-ON,2-M e 0 A-3171 H H H H 0 0H 2 CH 3 H 4-N,2-OM e 0 A-3172 H H H H Ei0 0 H 2 CH 3 H 20 2,4-F 0 A-3173 H H H H Ei 00 H 2 H3 H 2-NO 2,b- 0 A-3174 H H H H E 0H 2 GH 3 H 2-N0 2 ,6-~ 0 A-3175 H H H H ifE D UGH2GH3 H 2-02,44 Ae 0 A-3176 H H H H D 0UGH 2 0H 3 H 2-N0 2,b-i e 0 A-3177 H H H H D0 0GH 2 CH 3 H 2-N0 2,6-MAe 0 A-3178 H H H H 0 0H 2 CH 3 H 2-M e,4,b- 2 0 A-3179 H H H H 0 0H 2 CH 3 H 2-M e,6-Et 0 A-3180 H H H H H 0H 20H 3 H 2-cyclopropyl,6-OM e 0 A-3181 H H H H E D 0H 2 CH 3 H 2-M e,b-Et F A-3182 H H H H i 0GH 20H 3 H 2,6-Et 2 0 A-3183 H H H H i 0GH 20H 3 H 2-Et,6-F 0 A-3184 H H H H 0 0H 2 CH 3 H 2-OH 20H 3 ,6- I 0 A-3185 H H H H Hi0 0H 2 CH 3 H 2-OH 20H 2CH 3 ,6-O 1 0 A-3186 H H H H H UGH 20H 3 H 2-CH 2 NM e 2 A-3187 H HFFH CH 20F 3 H H
[0182]
[Table 57]
com pound R' R2 R R A R R' (R)m p A-3188 H H H H 0 CH 20F 3 H 2-F 0 A-3189 H H H H f0 CH 20F 3 H 2-C I0 A-3190 H H H H 0 CH 20 3 H 2-Br A-3191 H H H H i 0 GH 20F 3 H 2-UH 0 A-3192 H H H H D 0H20F3 H 2-Me 0 A-3193 H H H H 0 CH 20F 3 H 2-Et 0 A-3194 H H H H D0H20F3 H 2-Pr 0 A-3195 H H H H 0 CH 20F 3 H 2-CF 3 0 A-3196 H H H H H 0 CH 20F 3 H 2-H F2 0 A-3197 H H H H D F GH20F3 H 2-GH2F A-3198 H H H H i 0 GH 20F 3 H 2-GE 201 0 A-3199 H H H H D GH 20F 3 H 2-cycbpropy 1 0 A-3200 H H H H GH 20F 3 H 2-cycobbutyl 0 A-3201 H H H H 0 CH 20F 3 H 2-cycbpentyl 0 A-3202 H H H H 0 CH 20F 3 H 2-ethenyl 0 A-3203 H H H HF GH 20F 3 H 2-aIlyl 0 A-3204 H H H H i 0 GH 20F 3 H 2-(prop-1-en-1-y D 0 A-3205 H H H H 0 CH 20F 3 H 2-(trifforoetheny D 0 A-3206 H H H H GH 2 0F 3 H 2-M e 0 A-3207 H H H H 0 CH 20F 3 H 2-OEt 0 A-3208 H H H H f0 CH 20F 3 H 2-UPr 0 A-3209 H H H H f0 CH 20F 3 H 2-0 (/-Pr) 0 A-3210 H H H H 0 CH 20F 3 H 2-03 F A-3211 H H H H Hi0 CH 20F 3 H 2-0CH F 2 0 A-3212 H H H H iF GH 20F 3 H 2-(cycbpropy bxy) 0 A-3213 H H H H GH 20F 3 H 2-(cycobbuty bxy) 0 A-3214 H H H H GH 20F 3 H 2-(cycbpenty bxy) 0 A-3215 H H H H i 0 CH 20F 3 H 2-((2,2-d ch brocycbpropyIoxy) 0 A-3216 H H H H D0H20F 3 H 2-(oxiran-2-y D0 A-3217 H H H H 0 3 CH 20F H 2-SMe 0 A-3218 H H H H D0H20F3 H 3-SMe 0 A-3219 H H H H 0 CH 20F 3 H 2-S (=0)M e 0 A-3220 H H H H f0 CH 20F 3 H 3-S (=0 )M e 0 A-3221 H H H H f0 GH 20F 3 H 2-S (=) 2M e A-3222 H H H H D0H20F3 H 3-S(=0) 2Me 0 A-3223 H H H H 0Di CH 2 F3 H 2-SGE3 A-3224 H H H H i GH 20F 3 H 3-SCF3 A-3225 H H H H 0 CH 20F 3 H 3-S (= 0)3 0 A-3226 H H H H 0 CH 20F 3 H 3-SCF (H3 2 0
A-3227 H H H H H 0 CH 20F 3 H 2-(cycbpropy thb) 0 A-3228 H H H H 0 CH 20F 3 H 2-(cycbpropylsu finy D 0 A-3229 H H H H D0H20F 3 H 2-(cycbpropy ufony D 0 A-3230 H H H H f0 GH 20F 3 H 2-C (= 0)M e 0 A-3231 H H H H H GH 20F 3 H Z-GH 2 G(=U)GH 3 W A-3232 H H H H D GH 20F 3 H Z-GH 2G =U)GF 3 A-3233 H H H H H 0 GH 20U 3 H 2-GH 2 H 0 A-3234 H H H H D0H20F3 H 2-C2H0H3 0
A-3235 H H H H 0 CH 20F 3 H 2-CH 20H 2CH 3 0
A-3236 H H H H 0 CH 20F 3 H 2-CH 2SCH 3 0 A-3237 H H H H H 0 GH 20F 3 H 2-GH 2S = )GH 3 0
A-3238 H H H H 0 CH 20F 3 H 2-CH 2S(= 0) 2 CH3 A-3239 H H H H f0 GH 2 0F 3 H 2-(benzy bxy) 0 A-3240 H H H H GH 20F 3 H 2-NH 2 A-3241 H H H H 0 CH 20F 3 H 2-NH Me A-3242 H H H H f0 CH 20F 3 H 2-N (e) 2 0 A-3243 H H H H GH 20F 3 H 2-0,3-d bxo n-2-yD 0 A-3244 H H HHii f GH20F 3 H 2-0,3-d bxan-2-y D 0
[0183]
[Table 58]
com pound R' R2 R R A R R' (R)m p A-3245i H H H H 0 CH20F3 H 2-(1H-~ idazoE2-yD 0 A-3246 H H H H 0 CH 20F H 2-(thiazo -2-y1)0 A-3247 H H H H 0 CH 20F H 2-(oxazol1-2-y D A-3248 H H H H H GH 2G H 2-OH= NUH0 A-3249 H H H H 0 CH 20F3 H 2-CH= NOM e 0 A-3250 H H H H 0 CH 20F3 H 2-(4,b-dihydro-3-oxazo y D 0 A-3251 H H H H D0H20F3 H 2-N 0 A-3252 H H H H 0 CH 20F3 H 2-NO 2 0 A-3253 H H H H H 0 CH 20F3 H 2-F,6-I 0 A-3254 H H H H D if GH2GF3 H 2-F,6-Me 0 A-3255 H H H H 0 Ei C H 2G 3 H 3-F,6-M e 0 A-3256 H H H H D Ei H 2GF 3 H 4-F,2-M e 0 A-3257 H H H H GH 2GF 3 H 2-F,6-M e 0 A-3258 H H H H 0 CH 20F 3 H 3-F,6-M e 0 A-3259 H H H H 0 CH 20F 3 H 2,6-Oh 0 A-3260 H H H H GH 2CF 3 H 2- 1,6-M e 0 A-3261 H H H H H GH 2G 3 H 3- 1,6-M e 0 A-3262 H H H HD 0H2F3 H 4-1,2-Me 0 A-3263 H H H H GH 2G 3 H 2-C b-GI 3 0 A-3264 H H H H 0 CH 20F 3 H 2-0 ,6-F 3 0 A-3265 H H H H 0 CH 2 F 3 H 2-O 1,6-0M e 0 A-3266 H H H H H 0H 2 F3 H 3-O 1,6-0M e 0 A-3267 H H H H 0 CH 2 F3 H 4-GI,2-0Me 0 A-3268 H H H H H 0H 2 F3 H 2,4-M e 2 0 A-3269 H H H H f0 GH 2 G H 2,b- e2 0 A-3270 H H H H f0 GH 2 G H 2,6-M e 2 0
A-3271 H H H H H GH 2G 3 H 2-M e,4-CF 3 0 A-3272 H H H H i 0 CH 20F 3 H 2-M e,b-0F3 0 A-3273 H H H H D0H2F3 H 2-Me,6-OF3 0 A-3274 H H H H 0 CH 20F 3 H 2 -Me,4-0Me 0 A-3275 H H H H 0 CH 2 F3 H 2-M e,b-OM e A-3276 H H H H 0 CH 20F 3 H 2-M e,6-0M e 0 A-32 77 H H H H H 0 CH 20F 3 H 3-M e,6-0M e 0 A-3278 H H H H 0 E GH 2G 3 H 4-M e,2-UMe 0 A-3279 H H H HD 0HF23 H 2,5-0Me2 0 A-3280 H H H H GH 2GF 3 H 2,6-0M e 2 0 A-3281 H H H H GH 2Gl 3 H 2-OMe,6-G 3 0 A-3282 H H H H 0 CH 20F 3 H 2-OH,b-F 0 A-3283 H H H H 0 CH 20F 3 H 2-OHF 2 ,6-F 0 A-3284 H H H H H 0 CH 20F 3 H 2-H F 2,b-Me 0 A-328b H H H H 0 CH 20F 3 H 2-OHF 2,6-Me 0 A-3286 H H H H D0H2F3 H 2-cycbpropy 1,b-F 0 A-3287 H H H H GH 2GF 3 H 2-cycbpropy1,6-F 0 A-3288 H H H H GH 2GF 3 H 2-cyclopropyLb-M e 0 A-3289 H H H H D GH 2G 3 H 2-cyclopropyL,6-M e 0 A-3290 H H H H GH 2GF 3 H 2-etheny1,6-F 0 A-3291 H H H H 0 CH 20F 3 H 2-ethenyl,6- e 0 A-3292 H H H H 0 CH 20F 3 H 2-0Etb-F A-3293 H H H H 0 CH 20F 3 H 2-OEt6-F 0 A-3294 H H H H i0 GH 2G 3 H 2-U Etb-UI 1 A-329b H H H H 0 CH 20F 3 H 2-0 Et6-C 1 0 A-3296 H H H H f0 GH 2G 3 H 2-0Etb-M e 0 A-3297 H H H H f0 GH 2G 3 H 2-OEt6-M e 0 A-3298 H H H H 0 CH 20F 3 H 2-CH F2 ,b-F 0 A-3299 HIHjIH H 0 CH 2 F 3 H 2-CH F2 ,6-F 0 A-3300 H H H H GH 2GF 3 H 2-OCHF 2 ,b-M e 0 A-3301 H H H H 0 H 2G 3 H 2-0CHF 2 ,6-Me 0
[0184]
[Table 59]
com pound R' R2 R R A R R' (R)m p A-3302 H H H H 0 CH 20F3 H 2-(cycbpropyloxy),b-F 0 A-3303 H H H H 0 CH 20F H 2-(cycbpropyloxy),6-F A-3304 H H H H 0 CH 20F3 H 2-(cyclopropy bxy),b-Me A-3305 H H H H f GH 2G H 2-(cyclopropy bxy),6-M e 0 A-3306 H H H H 0 CH 20F3 H 2-SM e,b-F 0 A-3307 H H H H 0 CH 20F3 H 2-SMe,6-F 0 A-3308 H H H H D 0H20F3 H 2-SMe,b-M e 0 A-3309 H H H H 0 CH 20F3 H 2-SM e,6-iMe 0 A-3310 H H H H H 0 CH 20F3 H 2-S(=0)Me,b-F 0 A-3311 H H H H GH 2GF 3 H 2-S(=0)Me,6-F 0 A-3312 H H H H GH 2Gl 3 H 2-S = )Me,b-M e 0 A-3313 H H H H D GH 2GF 3 H 2-S (=0)Me,6Mie 0 A-3314 H H H H GH 2GF 3 H 2-S (= ) 2 Me,b-F A-3315 H H H H 0 CH 20F 3 H 2-S(= 0) 2 Me,6-F 0 A-3316 H H H H 0 CH 20F 3 H 2-S(= 0) 2 Me,b-M e 0 A-3317 H H H HF GH 2 F 3 H 2-S (= )M e,6 -M e 0 A-3318 H H H H f0 GH 2G 3 H 2-SC,b-H 0 A-3319 H H H H 0 CH 20F 3 H 2-SGF 3 ,6-F 0 A-3320 H H H H GH 2G 3 H 2-SCF 3 ,b-M e 0 A-3321 H H H H 0 CH 20F 3 H 2-SCF 3 ,6-M e 0 A-3322 H H H H Hi0 CH 20F 3 H 2-S =0 )C,b-F 0 A-3323 H H H H Hi0 CH 20F 3 H 2-S = )0F3 ,6-F 0 A-3324 H H H H D0H2F3 H 2-S(= 0)CF3,b-Me F A-3325 H H H H 0 CH 2 F 3 H 2-S(= 0)CF 3 ,6-M e 0 A-3326 H H H H GH 2GF 3 H 2-S (= ) 2 ,b-F A-3327 H H H H GH 2GF 3 H 2-S (= ) 2 F3 ,6-F A-3328 H H H H GH 2GF 3 H 2-S (= ) 2CF 3 ,b-M e 0 A-3329 H H H H i 0 CH 20F 3 H 2-S =0 2 CF 3 ,6-M e 0 A-3330 H H H H D0H 2F3 H 2-(cycbpropylth b),b-F 0 A-3331 H H H H 0 CH 20F 3 H 2-(cycbpropylth b),6-F 0 A-3332 H H H H D0H 2F3 H 2-(cycbpropy thio),b-M e 0 A-3333 H H H H 0 CH 20F 3 H 2-(cycbpropy thio),6-M e 0 A-3334 H H H H i 0 CH 20F 3 H 2-C )M e,b-F 0 A-3335 H H H H f0 GH 2G 3 H 2-C (=0 )M e,6-F 0 A-3336 H H H H D0H2F3 H 2-C(= 0)M e,b-M e 0 A-3337 H H H H D GH 2GF3 H 2-C(= 0)M e,6-M e 0 A-3338 H H H H i GH 2GF 3 H 2-CH 2 H,b--F F A-3339 H H H H 0 CH 20F 3 H 2-0H 20H,6-F 0 A-3340 H H H H 0 CH 20F 3 H 2-0H 20H,b-iMe 0 A-3341 H H H H H 0 CH 20F 3 H 2-0H 20H,6 -Me 0 A-3342 H H H H 0 CH 20F 3 H 2-0H 20H 3,4-F 0 A-3343 H H H H 0 CH 20F 3 H 2-0H 20H 3 ,b-F 0 A-3344 H H H H Hi0 GH 2GF 3 H 2-GH 20H 3 ,6-1 0 A-3345 H H H H 0 GH 2G 3 H Z-GH 2 UH 3 ,4-M e 0 A-3346 H H H H D GH 2GF 3 H -H 2 H 3,b- e A-3347 H H H H f0 GH 2GF 3 H 2-CH 2UCH 3 ,6-M e 0 A-3348 H H H H 0 CH 20F 3 H 2-0 C= 0)H 3 ,b-F 0 A-3349 H H H H 0 CH 20F 3 H 2-0 C= 0)H 3,6-F 0 A-3350 H H H H 0 CH 20F 3 H 2-0 C= )CH 3 ,b-M e 0 A-3351 H H H H f0 GH 2GF 3 H 2- C(= U)GH 3 ,6il0e 0 A-3352 H H H H 0 CH 20F 3 H 2-OS =0 ) 2 H 3 ,b-F 0 A-3353 H H H H f0 GH 2GF 3 H 2-OS( = ) 2 H3 ,6 A-3354 H H H H GH 2GF 3 H 2-OS (= ) 2CH 3,b-M e 0 A-3355 H H H H 0 CH 20F 3 H 2-S(= 0) 2 CH 3,6-M e 0 A-3356 H H H H Hi0 CH 20F 3 H 2-CH 2 SCH 3 ,b-F 0 A-3357 H H H H H2if GH 2 G 3 H 2-CH 2SCH 3 ,6-1 0 A-3358 H H H H iif GH2G03 H 2-CH 2SCH3,b-M e 0
[0185]
[Table 60]
com pound RI R2 R R R A R R' (R)m P A-3359 i H H H H H 0 CH2CF3 H 2-CH2SCH3,6-M e 0 A-3360 H H H H H 0 CH 2CF3 H 2-NM e 2 ,5-F 0 A-3361 H H H H H 0 CH 2CF3 H 2-NM e 2 ,6-F 0 A-3362 H H H H H 0 CH 20F 3 H 2-NMe 2 ,b-M e 0 A-3363 H H H H H 0 CH 2CF3 H 2-NMe 2 ,6-Me 0 A-3364 H H H H H 0 CH 2CF3 H 2-CN,4-F 0 A-3365 H H H H H 0 CH 2CF 3 H 2-CN,5-F 0 A-3366 H H H H H 0 CH 2CF3 H 2-CN,6-F 0 A-3367 H H H H H 0 CH 2CF3 H 2-CN,6-M e 0 A-3368 H H H H H 0 CH 20F 3 H 2-CN,5-0Me 0 A-3369 H H H H H 0 CH 20F 3 H 2-CN,6-0Me 0 A-3370 H H H H H 0 CH 20F 3 H 3-CN,6-M e 0 A-3371 H H H H H CH 20F 3 H 3-CN,6-0Me 0 A-3372 H H H H H 0 CH 2CF3 H 4-CN,2-M e 0 A-3373 H H H H H 0 CH 2CF3 H 4-CN,2-0Me 0 A-3374 H H H HF 0 0H 2 0F 3 H 2-N0 2 ,4-F 0 A-3375 H H H H H 0 CH 20F 3 H 2-N0 2,b- 0 A-3376 H H H H H 0 CH 2CF3 H 2-N0 2,6-F 0 A-3377 H H H H HH 2 0F 3 H 2A0N 2.4-MAe 0 A-3378 H H H H H 0 CH 2CF3 H 2-N0 2,5-Me 0 A-3379 H H H H H 0 CH 2CF3 H 2-N0 2,6-Me 0 A-3380 H H H H H 0 CH 2CF3 H 2-Me,4,5-F 2 0 A-3381 H H H H H 0 CH 2CF3 H 2-Me,6-Et 0 A-3382 H H H H H 0 CH 2CF3 H 2-cyclopropyl,6-OMe 0 A-3383 H H H H H CH 20F 3 H 2-Me,5-Et 0 A-3384 H H H H H 0 H 20F 3 H 2,6-Et2 0 A-3385 H H H H H 0 H 20F 3 H 2-Et,6-F 0 A-3386 H H H H H 0 CH 2CF3 H 2-CH 20CH 3 ,6-CI 0 A-3387 H H H H H 0 CH 2CF3 H 2-CH 20CH 2CH 3 ,6-CI 0 A-3388 H H H H H 0 CH 2CF3 H 2-CH 2 NMe 2 0 A-3389 H H H H H 0 tetrahydrofuran-3-yI H H 0 A-3390 H H H H H 0 tetrahydrofuran-3-yI H 2-F 0 A-3391 H H H H H 0 tetrahydrotfuran-3-yI H 2-CI 0 A-3392 H H H H H 0 tetrahydrofuran-3-yI H 2-Br 0 A-3393 H H H H H 0 tetrahydrofuran-3-yI H 2-OH 0 A-3394 H H H H H 0 tetrahydrofuran-3-yI H 2-Me 0 A-3395 H H H H H 0 tetrahydrofuran-3-yI H 2-Et 0 A-3396 H H H H H 0 tetrahydrofuran-3-yI H 2-Pr 0 A-3397 H H H H H 0 tetrahydrofuran-3-yI H 2-CF 3 0 A-3398 H H H H H 0 tetrahydrofuran-3-yI H 2-CHF 2 0 A-3399 H H H H H 0 tetrahydrofuran-3-yI H 2-CH 2F 0 A-3400 H H H H H 0 tetrahydrofuran-3-yI H 2-CF 2CI 0 A-3401 H H H H H 0 tetrahydrofuran-3-yI H 2-cycbpropyl 0 A-3402 H H H H H 0 tetrahydrofuran-3-yI H 2-cycobbutyl 0 A-3403 H H H H H 0 tetrahydrofuran-3-yI H 2-cycbpentyl 0 A-3404 H H H H H 0 tetrahydrofuran-3-yI H 2-ethenyl 0 A-3405 H H H H H 0 tetrahydrofuran-3-yI H 2-aIlyl 0 A-3406 H H H H H 0 tetrahydrofuran-3-yI H 2-(prop-1-en-1-y) 0 A-3407 H H H H H 0 tetrahydrofuran-3-yI H 2-(triflioroethenyD 0 A-3408 H H H H H 0 tetrahydrofuran-3-yI H 2-0Me 0 A-3409 H H H H H 0 tetrahydrofuran-3-yI H 2-0Et 0 A-3410 H H H H H 0 tetrahydrofuran-3-yI H 2-0Pr 0 A-3411 H H H H H 0 tetrahydrofuran-3-yI H 2-0 (/-Pr) 0 A-3412 H H H H H 0 tetrahydrofuran-3-yI H 2-0CF 3 0 A-3413 H H H H H 0 tetrahydrofuran-3-yI H 2-0CHF 2 0 A-3414 H H H H H 0 tetrahydrofuran-3-yI H 2-(cycbpropybxy) 0 A-3415 H H H iH I H tetrahydrofuran-3-ylI H 2-(cycbbutybxy) 0
[0186]
[Table 61]
com pound RI R2 R R R A R R' (R)m P A-3416 H H H H H 0 tetrahydrofuran-3-yl H 2-(cycbpentybxy) 0 A-3417 H H H H H 0 tetrahydrofuran-3-yl H 2-((2,2-dichbrocycobpropyl)oxy) 0 A-3418 H H H H H 0 tetrahydrofuran-3-yl H 2-(oxiran-2-y) A-3419 H H H H H 0 tetrahydrofuran-3-yI H 2-SMe 0 A-3420 H H H H H 0 tetrahydrofuran-3-yI H 3-SMe 0 A-3421 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0)Me 0 A-3422 H H H H H 0 tetrahydrofuran-3-yI H 3-S(=0)Me 0 A-3423 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0)2 Me 0 A-3424 H H H H H 0 tetrahydrofuran-3-yI H 3-S(=0)2 Me 0 A-3425 H H H H H 0 tetrahydrofuran-3-yI H 2-SCF3 0 A-3426 H H H H H 0 tetrahydrofuran-3-yI H 3-SCF3 0 A-3427 H H H H H 0 tetrahydrofuran-3-yI H 3-S(=0)0%3 0 A-3428 H H H H H 0 tetrahydrofuran-3-yI H 3-SCF(CF 3 ) 2 0 A-3429 H H H H H 0 tetrahydrofuran-3-yI H 2-(cycbpropylthio) 0 A-3430 H H H H H 0 tetrahydrofuran-3-yI H 2-(cycbpropylsulfinyD 0 A-3431 H H H H H 0 tetrahydrofuran-3-yI H 2-(cycbpropylsulfonyl 0 A-3432 H H H H H 0 tetrahydrofuran-3-yI H 2-C(=0)Me 0 A-3433 H H H H H 0 tetrahydrofuran-3-yI H 2-CH 2C(=0)CH 3 0 A-3434 H H H H H 0 tetrahydrofuran-3-yI H 2-OH20 (0)G 0 A-3435 H H H H H 0 tetrahydrofuran-3-yI H 2-CH 2 0H 0 A-3436 H H H H H 0 tetrahydrofuran-3-yI H 2-CH 2 0CH 3 0 A-3437 H H H H H 0 tetrahydrofuran-3-yI H 2-CH 2 0CH 2CH 3 0 A-3438 H H H H H 0 tetrahydrofuran-3-yI H 2-CH 2SCH 3 0 A-3439 H H H H H 0 tetrahydrofuran-3-yI H 2-CH 2S(=0)CH 3 0 A-3440 H H H H H 0 tetrahydrofuran-3-yI H 2-CH 2S(=0%20H 3 0 A-3441 H H H H 0H tetrahydrofuran-3-yI H 2-(benzybxy) 0 A-3442 H H H H 0H tetrahydrofuran-3-yI H 2-NH2 0 A-3443 H H H H 0H tetrahydrofuran-3-yI H 2-NHMe 0 A-3444 H H H H 0H tetrahydrofuran-3-yI H 2-N e) 2 0 A-3445 H H H H 0H tetrahydrofuran-3-yI H 2-(1,3-dioxolan-2-yD 0 A-3446 H H H H 0H tetrahydrofuran-3-yI H 2-(1,3-dioxan-2-y) 0 A-3447 H H H H 0H tetrahydrofuran-3-yI H 2-(1H--m idazol-2-yD 0 A-3448 H H H H 0H tetrahydrofuran-3-yl H 2-(thiazol-2-yl) 0 A-3449 H H H H 0H tetrahydrofuran-3-yl H 2-(oxazol-2-yl 0 A-3450 H H H H 0H tetrahydrofuran-3-yI H 2-CH=N0H 0 A-3451 H H H H 0H tetrahydrofuran-3-yI H 2-CH=NOMe 0 A-3452 H H H H 0H tetrahydrofuran-3-yI H 2-(4,5-dihydro-3-isoxazolyl 0 A-3453 H H H H 0H tetrahydrofuran-3-yI H 2-CN 0 A-3454 H H H H 0H tetrahydrofuran-3-yI H 2-N0 2 0 A-3455 H H H H 0H tetrahydrofuran-3-yI H 2-F,6-CI 0 A-3456 H H H H 0H tetrahydrofuran-3-yI H 2-F,6-Me 0 A-3457 H H H H 0H tetrahydrofuran-3-yI H 3-F,6-Me 0 A-3458 H H H H 0H tetrahydrofuran-3-yI H 4-F,2-Me 0 A-3459 H H H H 0H tetrahydrofuran-3-yI H 2-F,6-OMe 0 A-3460 H H H H 0H tetrahydrofuran-3-yl H 3-F,6-OM e 0 A-3461 H H H H 0H tetrahydrofuran-3-yl H 2,6-01 0 A-3462 H H H H 0H tetrahydrofuran-3-yl H 2-CI,6-M e 0 A-3463 H H H H 0H tetrahydrofuran-3-yI H 3-CI,6-M e 0 A-3464 H H H H 0H tetrahydrofuran-3-yI H 4-CI,2-Me 0 A-3465 H H H H 0H tetrahydrofuran-3-yI H 2-CIb-CF 3 0 A-3466 H H H H 0H tetrahydrofuran-3-yI H 2-CI,6-CF 3 0 A-3467 H H H H 0H tetrahydrofuran-3-yI H 2-C1,6-0Me 0 A-3468 H H H H 0H tetrahydrofuran-3-yI H 3-C1,6-0Me 0 A-3469 H H H H 0H tetrahydrofuran-3-yI H 4-CI,2-0Me 0 A-3470 ifH H H 0 tetrahydrofuran-3-yI H 2,4-M e 2 0 A-3471 H H H H H 0 tetrahydrofuran-3-yI H 2,b-M e 2 0 A-3472 H H H H H 0 tetrahydrofuran-3-yI H 2,6-M e 2 0
[0187]
[Table 62]
com pound RI R2 R R R A R R' (R)m P A-3473 H H H H H 0 tetrahydrofuran-3-yI H 2-M e,4-CF 3 0 A-3474 H H H H H 0 tetrahydrofuran-3-yI H 2-Me,5-CF3 0 A-3475 H H H H H 0 tetrahydrofuran-3-yI H 2-MAe,6-CF 3 0 A-3476 H H H H H 0 tetrahydrofuran-3-yI H 2-MAe,4-0Me 0 A-3477 H H H H H 0 tetrahydrofuran-3-yI H 2-e,5-0Me 0 A-3478 H H H H H 0 tetrahydrofuran-3-yI H 2-MAe,6-0Me 0 A-3479 H H H H H 0 tetrahydrofuran-3-yI H 3-MAe,6-0Me 0 A-3480 H H H H H 0 tetrahydrofuran-3-yI H 4-Me,2-0Me 0 A-3481 H H H H H 0 tetrahydrofuran-3-yI H 2,5-0Me 2 0 A-3482 H H H H H 0 tetrahydroifuran-3-yI H 2,6-0Me 2 0 A-3483 H H H H H 0 tetrahydrofuran-3-yI H 2-0Me,6-G 3 0 A-3484 H H H H H 0 tetrahydrofuran-3-yI H 2-CHF2b-F 0 A-3485 H H H H H 0 tetrahydrofuran-3-yI H 2-CHF 2,6-F 0 A-3486 H H H H H 0 tetrahydrofuran-3-yI H 2-CHF 2,5-Me 0 A-3487 H H H H H 0 tetrahydrofuran-3-yI H 2-CHF 2,6-Me 0 A-3488 H H H H H 0 tetrahydrofuran-3-yI H 2-cycbpropyl,5-F 0 A-3489 H H H H H 0 tetrahydrofuran-3-yI H 2-cycbpropyl,6-F 0 A-3490 H H H H H 0 tetrahydrofuran-3-yI H 2-cyclopropyl,5-Me 0 A-3491 H H H H H 0 tetrahydrofuran-3-yl H 2-cyclopropyl,6-Me 0 A-3492 H H H H H 0 tetrahydrofuran-3-yl H 2-ethenyl,6-F 0 A-3493 H H H H H 0 tetrahydrofuran-3-yl H 2-ethenyl,6-M e 0 A-3494 H H H H H 0 tetrahydrofuran-3-yl H 2-0Et,5-F 0 A-3495 H H H H H 0 tetrahydrofuran-3-yI H 2-0Et,6-F 0 A-3496 H H H H H 0 tetrahydrofuran-3-yI H 2-0Et,5-CI 0 A-3497 H H H H H 0 tetrahydrofuran-3-yI H 2-0Et,6-CI 0 A-3498 H H H H H 0 tetrahydrofuran-3-yI H 2-0Et,5-M e 0 A-3499 H H H H H 0 tetrahydrofuran-3-yI H 2-0Et,6-Me 0 A-3500 H H H H H 0 tetrahydrofuran-3-yI H 2-0CHF2,5-F 0 A-3501 H H H H H 0 tetrahydrofuran-3-yI H 2-0CHF 2,6-F 0 A-3502 H H H H H 0 tetrahydrofuran-3-yI H 2-0CHF 2 ,5-MAe 0 A-3503 H H H H H 0 tetrahydrofuran-3-yI H 2-0CHF 2 ,6-MAe 0 A-3504 H H H H H 0 tetrahydrofuran-3-yI H 2-(cycbpropyloxy),5-F 0 A-3505 H H H H H 0 tetrahydrofuran-3-yI H 2-(cycbpropyloxy),6-F 0 A-3506 H H H H H 0 tetrahydrofuran-3-yI H 2-(cyclopropyloxy),5-M e 0 A-3507 H H H H H 0 tetrahydrofuran-3-yI H 2-(cyclopropybxy),6-M e 0 A-3508 H H H H H 0 tetrahydrofuran-3-yl H 2-SMe,5-F 0 A-3509 H H H H H 0 tetrahydrofuran-3-yI H 2-SMe,6-F 0 A-3510 H H H H H 0 tetrahydrofuran-3-yI H 2-SMe,5-M e 0 A-3511 H H H H H 0 tetrahydrofuran-3-yI H 2-SMe,6-M e 0 A-3512 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0)Me,5-F 0 A-3513 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0)Me,6-F 0 A-3514 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0)Me,5-M e 0 A-3515 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0)Me,6-M e 0 A-3516 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0) 2Me,b-F 0 A-3517 H H H H H 0 tetrahydrofuran-3-yI H 2-S (=0) 2M e,6-F 0 A-3518 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0) 2 Me,b-M e 0 A-3519 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0) 2 Me,6-MAe 0 A-3520 H H H H H 0 tetrahydrofuran-3-yI H 2-SCF,5-F 0 A-3521 H H H H H 0 tetrahydrofuran-3-yI H 2-SCF 3 ,6-F 0 A-3522 H H H H H 0 tetrahydrofuran-3-yI H 2-SCF 3 ,b-Me 0 A-3523 H H H H H 0 tetrahydrotfuran-3-yI H 2-SCF 3 ,6-Me 0 A-3524 H H H H H 0 tetrahydrofuran-3-yI H 2-S O)CFb-F 0 A-3525 H H H H H 0 tetrahydrofuran-3-yI H 2-S O)0F 3,6-F 0 A-3526 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0)CF 3 ,5-Me 0 A-3527 H H H H H 0 tetrahydrofuran-3-yI H 2-S(=0)CF 3 ,6-M e 0 A-3528 H H H H H 0 tetrahydrofuran-3-yI H 2-S(0) 2CF3 ,b-F 0 A-3529 f H H H H 0 tetrahydrofuran-3-y I H 2-S(=0) 2CF3 ,6-F 0
[0188]
[Table 63]
com pound R' R2 R R A R R' (R)m p A-3530 H H H H 0 tetrahydrofuran-3-yl H 2-S(=0) 20F 3 ,b-M e 0 A-3531 H H H H tetrahydrouran-3-yl H 2-S(=0) 20F 3 ,6-Me A-3532 H H H H 0 tetrahydroturan-3-y H 2-(cycobpropylthb),b- A-3533 H H H H i 0 tetrahydroturan-3-yi H 2-(cycobpropylthlo),6-F 0 A-3534 H H H H 0 tetrahydroturan-3-y H 2-(cycbpropylthio),b-Me 0 A-3535 H H H H 0 tetrahydroturan-3-y H 2-(cycbpropylthio),6-Me 0 A-3536 H H H H D fitetrahydrouran-3-yl H 2-0(=0)Me,b-F 0 A-3537 H H H H 0 tetrahydrofuran-3-yI H 2-0(0)Me,6-F 0 A-3538 H H H H H 0 tetrahydroturan-3-yI H 2-0(=0)Me,b-Me 0 A-3539 H H H H 0 tetrahydroturan-3-yI H 2-0(=0)Me,6-Me A-3540 H H H H i 0 tetrahydrofulran-3-yI H 2-CH 2UH,b-H A-3541 H H H H 0 tetrahydrofuran-3-yI H 2-CH 2UN,6-H 0 A-3542 H H H H 0 tetrahydrofuran-3-yI H 2-CH 2 H,b-M e 0 A-3543 H H H H 0 tetrahydrofulran-3-yI H 2-0H 20H,6-M e 0 A-3544 H H H H 0 tetrahydrofulran-3-yI H 2-0H 20H 3 ,4-F 0 A-3545 H H H H 0 tetrahydrofuran-3-yI H Z-GH 2UGH 3,b-H 0 A-3546 H H H H 0 tetrahydrofulran-3-yI H -GH 2 GH 3,6- 0 A-3547 H H H H 0 tetrahydrofuran-3-yI H 2-OH 20CH 3,4-Me 0 A-3548 H H H H tetrahydroturan-3-yI H -H 2UH 3 ,b-me 0 A-3549 H H H H 0 tetrahydroturan-3-yI H 2-OH 20H 3 ,6-Me 0 A-3550 H H H H tetrahydrouran-3-yI H 2-U0(=0)0H 3 ,b-F 0 A-3551 H H H H 0 tetrahydrofuran-3-yI H 2-UC(=U)0H 3 ,6-F 0 A-3552 H H H H 0 tetrahydroturan-3-yl H 2-U0(=0)CH 3 ,b-Me 0 A-3553 H H H H 0 tetrahydrofuran-3-yI H 2-00(=0)0H 3 ,6-Me 0 A-3554 H H H H tetrahydrouran-3-y H 2-US(0) 20H 3,b-H 0 A-3555 H H H H tetrahydrouran-3-y H -OS(=) 20H 3,6- 0 A-3556 H H H H tetrahydrouran-3-yI H 2-OS( =) 20H 3,b-M e 0 A-3 557 H H H H i 0 tetrahydrotfuran-3-yI H 2-OS(= 0) 2CH 3,6-Me 0 A-3558 H H H H 0 tetrahydroturan-3-yI H 2-OH 2 S0H 3 ,b-F 0 A-3559 H H H H 0 tetrahydroturan-3-yI H 2-OH 2 S0H 3 ,6-F 0 A-3560 H H H H 0 tetrahydroturan-3-yI H 2-OH 2SOH 3,b-Me 0 A-3561 H H H H 0 tetrahydrofuran-3-yI H 2-OH 2SOH 3 ,6-Me 0 A-3562 H H H H tetrahydroturan-3-yI H 2-NM e 2 ,b-F 0 A-3563 H H H H tetrahydroturan-3-yI H 2-NM e 2 ,6-F 0 A-3564 H H H H 0 tetrahydroturan-3-yI H 2-NM e 2 ,b-A e 0 A-3565 H H H H 0 tetrahydroturan-3-yI H 2-NMe 2 ,6- e A-3566 H H H H 0 tetrahydrotiuran-3-yI H 2-N,4-F 0 A-3567 H H H H 0 tetrahydroturan-3-yI H 2-ONb-F 0 A-3568 H H H H 0 tetrahydroturan-3-yI H 2-N,6-F 0 A-3569 H H H H H 0 tetrahydrofuran-3-yI H 2-ON,6-Me 0 A-3570 H H H H 0 tetrahydrofuran-3-yI H 2-GN,b-OMe 0 A-3571 H H H H 0 tetrahydrofuran-3-yI H 2-GN,6-OMe 0 A-3572 H H H H 0 tetrahydroturan-3-yI H 3-ON,6-Me 0 A-3573 H H H H 0 tetrahydroturan-3-yI H 3-GN,6-OMe F A-3574 H H H H 0 tetrahydrofuran-3-yI H 4-ON,2-Me 0 A-3575 H H H H 0 tetrahydroturan-3-yI H 4-GN,2-OMe 0 A-3576 H H H H 0 tetrahydrofuran-3-yI H 2-N0 2,4-F 0 A-3577 H H H H 0 tetrahydrofturan-3-yI H 2-N0 2,b-F 0 A-3578 H H H H 0 tetrahydroturan-3-yI H 2-N0 2 ,64 0 A-3579 H H H H 0 tetrahydrofuran-3-yI H 2-N0 2,4-Mle 0 A-3580 H H H H 0 tetrahydrofuran-3-yI H 2-N0 2,b-M e F A-3581 H H H H 0 tetrahydrofturan-3-yI H 2-NU 2,6-MA e 0 A-3582 H H H H tetrahydrouran-3-yI H 2-M e,4,b-F 2 0 A-3583 H H H H 0 tetrahydrofuran-3-yI H 2-M e,6-Et 0 A-3584 H H H H 0 tetrahydrofuran-3-yI H 2-cyclopropyl,6-OM e 0 A-3585 H H H H 0 tetrahydroturan-3-yI H 2-M e,b-Et 0 A-3586 H f F IFH 0 tetrahydrofuran-3-yI H 2,6-Et 2 0
[0189]
[Table 64]
com pound RI R2 R R R A R R' (R)m P A-3587 iH H H H H 0 tetrahydrofuran-3-yl H 2-Et,6-F 0 A-3588 H H H H H 0 tetrahydrofuran-3-yl H 2-CH 20CH3 ,6-CI 0 A-3589 H H H H H 0 tetrahydrofuran-3-yl H 2-CH 20CH 2 CH 3 ,6-CI 0 A-3590 H H H H H 0 tetrahydrofuran-3-yI H 2-CH 2 NMe 2 0 A-3591 H H H H H 0 tetrahydropyran-4-yI H H 0 A-3592 H H H H H 0 tetrahydropyran-4-yI H 2-F 0 A-3593 H H H H H 0 tetrahydropyran-4-yI H 2-Cl 0 A-3594 H H H H H 0 tetrahydropyran-4-yI H 2-Br 0 A-3595 H H H H H 0 tetrahydropyran-4-yI H 2-OH 0 A-3596 H H H H H 0 tetrahydropyran-4-yI H 2-Me 0 A-3597 H H H H H 0 tetrahydropyran-4-yI H 2-Et 0 A-3598 H H H H H 0 tetrahydropyran-4-yI H 2-Pr 0 A-3599 H H H H H 0 tetrahydropyran-4-yI H 2-GOF 0 A-3600 H H H H H 0 tetrahydropyran-4-yI H 2-CHF 2 0 A-3601 H H H H H 0 tetrahydropyran-4-yI H 2-CH 2F 0 A-3602 H H H H H 0 tetrahydropyran-4-yI H 2-OCI 0 A-3603 H H H H H 0 tetrahydropyran-4-yI H 2-cycbpropyl 0 A-3604 H H H H H 0 tetrahydropyran-4-yI H 2-cycobbutyl 0 A-3605 H H H H H 0 tetrahydropyran-4-yI H 2-cycbpentyl 0 A-3606 H H H H H 0 tetrahydropyran-4-yI H 2-ethenyl 0 A-3607 H H H H H 0 tetrahydropyran-4-yI H 2-allyl 0 A-3608 H H H H H 0 tetrahydropyran-4-yl H 2-(prop-1-en-1-yD 0 A-3609 H H H H H 0 tetrahydropyran-4-yI H 2-(trifboroethenyD 0 A-3610 H H H H H 0 tetrahydropyran-4-yl H 2-0Me 0 A-3611 H H H H H 0 tetrahydropyran-4-yl H 2-0Et 0 A-3612 H H H H H 0 tetrahydropyran-4-yI H 2-0Pr 0 A-3613 H H H H H 0 tetrahydropyran-4-yl H 2-0 (/-Pr) 0 A-3614 H H H H H 0 tetrahydropyran-4-yl H 2-0CF, 0 A-3615 H H H H H 0 tetrahydropyran-4-yI H 2-0CHF 2 0 A-3616 H H H H H 0 tetrahydropyran-4-yl H 2-(cycbpropybxy) 0 A-3617 H H H H H 0 tetrahydropyran-4-yl H 2-(cycobbutyloxy) 0 A-3618 H H H H H 0 tetrahydropyran-4-yI H 2-(cycbpentybxy) 0 A-3619 H H H H H 0 tetrahydropyran-4-yl H 2-((2,2-dichbrocycbpropyl)oxy) 0 A-3620 H H H H H 0 tetrahydropyran-4-yl H 2-(oxiran-2-yD 0 A-3621 H H H H H 0 tetrahydropyran-4-yI H 2-SMe 0 A-3622 H H H H H 0 tetrahydropyran-4-yl H 3-SMe 0 A-3623 H H H H H 0 tetrahydropyran-4-yl H 2-S(=0)Me 0 A-3624 H H H H H 0 tetrahydropyran-4-yI H 3-S(=0)Me 0 A-3625 H H H H H 0 tetrahydropyran-4-yI H 2-S(=0) 2Me 0 A-3626 H H H H H 0 tetrahydropyran-4-yl H 3-S(=0) 2Me 0 A-3627 H H H H H 0 tetrahydropyran-4-yl H 2-SCF3 0 A-3628 H H H H H 0 tetrahydropyran-4-yI H 3-SCF3 0 A-3629 H H H H H 0 tetrahydropyran-4-yl H 3-S(=0)CF3 0 A-3630 H H H H H 0 tetrahydropyran-4-yI H 3-SCF(0F 3)2 0 A-3631 H H H H H 0 tetrahydropyran-4-yI H 2-(cycbpropylthio) 0 A-3632 H H H H H 0 tetrahydropyran-4-yl H 2-(cycbpropysulfinyD 0 A-3633 H H H H H 0 tetrahydropyran-4-yl H 2-(cycbpropylsulfonyD 0 A-3634 H H H H H 0 tetrahydropyran-4-yI H 2-C(=0)Me 0 A-3635 H H H H H 0 tetrahydropyran-4-yl H 2-CH 2C(=0)CH 3 0 A-3636 H H H H H 0 tetrahydropyran-4-yl H 2-CH 20(=0)G 3 0 A-3637 H H H H H 0 tetrahydropyran-4-yI H 2-CH20H 0 A-3638 H H H H H 0 tetrahydropyran-4-yl H 2-CH 2 00H 3 0 A-3639 H H H H H 0 tetrahydropyran-4-yl H 2-CH 2 00H 20H 0 A-3640 H H H H H 0 tetrahydropyran-4-yI H 2-CH 2SCH3 0 A-3641 H H H H H 0 tetrahydropyran-4-yl H 2-CH 2S(=0)CH 3 0 A-3642 H H H H H 0 tetrahydropyran-4-yl H 2-CH 2S(=0) 20H 3 0 A-3643 H H H H H 0 tetrahydropyran-4-yI H 2-(benzybxy) 0
[0190]
[Table 65]
com pound RI R2 R R R A R R' (R)m P A-3644 H H H H H 0 tetrahydropyran-4-yI H 2-NH 2 0 A-3645 H H H H H 0 tetrahydropyran-4-yI H 2-NHMe 0 A-3646 H H H H H 0 tetrahydropyran-4-yI H 2-N(e)2 0 A-3647 H H H H H 0 tetrahydropyran-4-yI H 2-(1,3-dbxolan-2-yD 0 A-3648 H H H H H 0 tetrahydropyran-4-yI H 2-(1,3-dbxan-2-yD 0 A-3649 H H H H H 0 tetrahydropyran-4-yI H 2-(1H--m idazol-2-yl) 0 A-3650 H H H H H 0 tetrahydropyran-4-yI H 2-(thiazol-2-yl) 0 A-3651 H H H H H 0 tetrahydropyran-4-yI H 2-(oxazol-2-y) 0 A-3652 H H H H H 0 tetrahydropyran-4-yI H 2-CH=N0H 0 A-3653 H H H H H 0 tetrahydropyran-4-yI H 2-CH=NOMe 0 A-3654 H H H H H 0 tetrahydropyran-4-yI H 2-(4,5-dihydro-3-soxazolyD 0 A-3655 H H H H H 0 tetrahydropyran-4-yI H 2-CN 0 A-3656 H H H H H 0 tetrahydropyran-4-yI H 2-N0 2 0 A-3657 H H H H H 0 tetrahydropyran-4-yI H 2-F,6-CI 0 A-3658 H H H H H 0 tetrahydropyran-4-yI H 2-F,6-Me 0 A-3659 H H H H H 0 tetrahydropyran-4-yI H 3-F,6-Me 0 A-3660 H H H H H 0 tetrahydropyran-4-yI H 4-F,2-M e 0 A-3661 H H H H H 0 tetrahydropyran-4-yI H 2-F,6-0Me 0 A-3662 H H H H H 0 tetrahydropyran-4-yI H 3-F,6-0Me 0 A-3663 H H H H H 0 tetrahydropyran-4-yI H 2,6-Cl 0 A-3664 H H H H H 0 tetrahydropyran-4-yI H 2-CI,6-Me 0 A-3665 H H H H H 0 tetrahydropyran-4-yI H 3-CI,6-M e 0 A-3666 H H H H H 0 tetrahydropyran-4-yI H 4-CI,2-M e 0 A-3667 H H H H H 0 tetrahydropyran-4-yI H 2-CL,5-CF, 0 A-3668 H H H H H 0 tetrahydropyran-4-yI H 2-CI,6-F 3 0 A-3669 H H H H H 0 tetrahydropyran-4-yI H 2-C1,6-0Me 0 A-3670 H H H H H 0 tetrahydropyran-4-yI H 3-C1,6-0Me 0 A-3671 H H H H H 0 tetrahydropyran-4-yI H 4-CI,2-0Me 0 A-3672 H H H H H 0 tetrahydropyran-4-yI H 2,4-M e 2 0 A-3673 H H H H H 0 tetrahydropyran-4-yI H 2,5-M e 2 0 A-3674 H H H H H 0 tetrahydropyran-4-yI H 2,6-M e 2 0 A-3675 H H H H H 0 tetrahydropyran-4-yI H 2-Me,4-CF3 0 A-3676 H H H H H 0 tetrahydropyran-4-yI H 2-Me,5-CF3 0 A-3677 H H H H H 0 tetrahydropyran-4-yI H 2-M e,6-F 3 0 A-3678 H H H H H 0 tetrahydropyran-4-yI H 2-Me,4-0Me 0 A-3679 H H H H H 0 tetrahydropyran-4-yI H 2-Me,5-0Me 0 A-3680 H H H H H 0 tetrahydropyran-4-yI H 2-Me,6-0Me 0 A-3681 H H H H H 0 tetrahydropyran-4-yI H 3-Me,6-0Me 0 A-3682 H H H H H 0 tetrahydropyran-4-yI H 4-Me,2-0Me 0 A-3683 H H H H H 0 tetrahydropyran-4-yI H 2,5-0Me 2 0 A-3684 H H H H H 0 tetrahydropyran-4-yI H 2,6-0Me 2 0 A-3685 H H H H H 0 tetrahydropyran-4-yI H 2-0Me,6-CF3 0 A-3686 H H H H H 0 tetrahydropyran-4-yI H 2-CHF2,b-F 0 A-3687 H H H H H 0 tetrahydropyran-4-yI H 2-CHF 2,6-F 0 A-3688 H H H H H 0 tetrahydropyran-4-yI H 2-CH F2,b-M e 0 A-3689 H H H H H 0 tetrahydropyran-4-yI H 2-CHF 2,6-MAe 0 A-3690 H H H H H 0 tetrahydropyran-4-yI H 2-cycbpropyL,5-F 0 A-3691 H H H H H 0 tetrahydropyran-4-yI H 2-cycbpropyL,6-F 0 A-3692 H H H H H 0 tetrahydropyran-4-yI H 2-cyclopropyL,5-Me 0 A-3693 H H H H H 0 tetrahydropyran-4-yI H 2-cyclopropyL,6-Me 0 A-3694 H H H H H 0 tetrahydropyran-4-yI H 2-ethenyl,6-F 0 A-3695 H H H H H 0 tetrahydropyran-4-yI H 2-ethenyl,6-M e 0 A-3696 H H H H H 0 tetrahydropyran-4-yI H 2-0Et,5-F 0 A-3697 H H H H H 0 tetrahydropyran-4-yI H 2-0Et,6-F 0 A-3698 H H H H H 0 tetrahydropyran-4-yI H 2-0Et,5-CI 0 A-3699 H H H H H 0 tetrahydropyran-4-yI H 2-0Et,6-CI 0 A-3700 HI HI HI 0 tetrahydropyran-4-y l H 2-0Et,5-Me 0
[0191]
[Table 66]
com pound R' R2 R R A R R' (R)m p A-3701 H H H H 0 tetrahydropyran-4-yI H 2-OEt,6-M e 0 A-3702 H H H H 0 tetrahydropyran-4-yI H 2-0HH2,b-F F A-3703 H H H H 0 tetrahydropyran-4-yI H 2-0HF 2,6-F 0 A-3704 H H H H i 0 tetrahydropyran-4-yI H 2-CHF 2 ,b-MAe 0 A-3705 H H H H 0 tetrahydropyran-4-yI H 2-CHF 2 ,6-Me A A-3706 H H H H 0 tetrahydropyran-4-yI H 2-(cycbpropyloxy),b-F 0 A-3/07 H H H H 0 tetrahydropyran-4-yI H 2-(cycbpropyloxy),6-F 0 A-3708 H H H H 0 tetrahydropyran-4-yI H 2-(cyclopropybxy),b-M e 0 A-3709 H H H H 0 tetrahydropyran-4-yI H 2-(cyclopropybxy),6-M e 0 A-3710 H H H H 0 tetrahydropyran-4-yI H 2-SMe,b-F F A-3/ll H H H H i 0 tetrahydropyran-4-yI H 2-SMe,6-F 0 A-3712 H H H H 0 tetrahydropyran-4-yI H 2-SMe,b-Me 0 A-3713 H H H H 0 tetrahydropyran-4-yI H 2-SMe,6-Me 0 A-3714 H H H H 0 tetrahydropyran-4-yI H 2-S(=0)Me,b-F 0 A-3/lb H H H H 0 tetrahydropyran-4-yI H 2-S(=0)Me,6-F 0 A-3716 H H H H 0 tetrahydropyran-4-yI H 2-S(=0)Me b-Me 0 A-31 H H H H 0 tetrahydropyran-4-yI H 2-S(=0)Me,6-MA e 0 A-318 H H H H 0 tetrahydropyran-4-yI H 2-S(0) 2Me,b-F 0 A-3719 H H H H 0 tetrahydropyran-4-yI H 2-S(=U) 2Me,6-H 0 A-3720 H H H H 0 tetrahydropyran-4-yI H 2-S(=0) 2Me,b-Me 0 A-3721 H H H H 0 tetrahydropyran-4-yI H 2-S(0) 2Me,6-MAe 0 A-3722 H H H H 0 tetrahydropyran-4-yI H 2-SGC,b-F 0 A-3723 H H H H 0 tetrahydropyran-4-yI H 2-SCF 3 ,6-F 0 A-3724 H H H H 0 tetrahydropyran-4-yI H 2-SOF 3 ,b-Me 0 A-3725 H H H H 0 tetrahydropyran-4-yI H 2-SCF 3 ,6-M e 0 A-3726 H H H H 0 tetrahydropyran-4-yI H 2-S (=O)Cb-H 0 A-3727 H H H H 0 tetrahydropyran-4-yI H 2-S=O)CF 3 ,6- 0 A-3728 H H H H i 0 tetrahydropyran-4-yI H 2-S(=)F 3 ,b-Me 0 A-3729 H H H H 0 tetrahydropyran-4-yI H 2-S(=0)F 3 ,6-M e 0 A-3730 H H H H 0 tetrahydropyran-4-yI H 2-S(=0) 2 F 3 ,b-F 0 A-3731 H H H H 0 tetrahydropyran-4-yI H 2-S(=0) OF2 3 ,6-F 0 A-3732 H H H H 0 tetrahydropyran-4-yI H 2-S(=0) 2 F 3 ,b-Me 0 A-3733 H H H H 0 tetrahydropyran-4-yI H 2-S(=0) 2 F 3 ,6-M e 0 A-3734 H H H H 0 tetrahydropyran-4-yI H 2-(cyclopropylthlo),b-F 0 A-3735 H H H H 0 tetrahydropyran-4-yI H 2-(cyclopropylthio),6-F 0 A-3736 H H H H 0 tetrahydropyran-4-yI H 2-(cyclopropylthio),b-M e 0 A-3737 H H H H 0 tetrahydropyran-4-yI H 2-(cyclopropyltho),6-M e 0 A-3738 H H H H 0 tetrahydropyran-4-yI H 2-C(=0)Me,b-F 0 A-3739 H H H H 0 tetrahydropyran-4-yI H 2-C(=0)Me,6-F 0 A-3740 H H H H H 0 tetrahydropyran-4-yI H 2-C(=0)Me,b-M e 0 A-3741 H H H H 0 tetrahydropyran-4-yI H 2-C(=0)Me,6-M e 0 A-3742 H H H H 0 tetrahydropyran-4-yI H 2-CH 2OH,b-F 0 A-3743 H H H H 0 tetrahydropyran-4-yI H 2-CH 2 ,6-H 0 A-3744 H H H H 0 tetrahydropyran-4-yI H 2-CH 2 H,b-M e 0 A-3745 H H H H 0 tetrahydropyran-4-yI H 2-CH 2U,6-M e 0 A-3746 H H H H 0 tetrahydropyran-4-yI H 2-CH 20H 3,4-F 0 A-3747 H H H H 0 tetrahydropyran-4-yI H 2-CH 20H 3 ,b-F 0 A-3748 H H H H 0 tetrahydropyran-4-yI H 2-CH 20H 3,6-F 0 A-3749 H H H H 0 tetrahydropyran-4-yI H 2-CH 20H 3 ,4-Me 0 A-3750 H H H H 0 tetrahydropyran-4-yI H Z-GH 2UGH 3 ,b-M e 0 A-375l H H H H 0 tetrahydropyran-4-yI H 2-CH 20H 3 ,6-Me 0 A-3752 H H H H 0 tetrahydropyran-4-yI H 2-UC0=)CH 3,b-H 0 A-3753 H H H H 0 tetrahydropyran-4-yI H 2-UC0=)CH 3,6-F 0 A-3754 H H H H 0 tetrahydropyran-4-yI H 2-0(=0)CH 3 ,5-M e 0 A-3755 H H H H 0 tetrahydropyran-4-yI H 2-0(=0)CH 3 ,6-M e 0 A-3756 H H H H 0 tetrahydropyran-4-yI H 2-USt0=) 2CH 3 ,b-F 0 A-3/b/ H H H H 0 tetrahydropyran-4-y 1 H 2-US(=0) 2 CH 3 ,6-F 0
[0192]
[Table 67]
com pound RI R2 R R R A R R' (R)m p A-3758 H H H H H 0 tetrahydropyran-4-yI H 2-OS(=0) 2CH3 ,5-Me 0 A-3759 H H 0 H H H tetrahydropyran-4-yI H 2-OS(=0) 2CH3 ,6-Me 0 A-3760 H H H H H 0 tetrahydropyran-4-yI H 2-CH 2 SCH 3 ,5-F 0 A-3761 H H H H H 0 tetrahydropyran-4-yI H 2-CH 2 SCH 3 ,6-F 0 A-3762 H H H H H 0 tetrahydropyran-4-yI H 2-CH 2SCH 3,5-Me 0 A-3763 H H H H H 0 tetrahydropyran-4-yI H 2-CH 2SCH 3,6-Me 0 A-3764 H H H H H 0 tetrahydropyran-4-yI H 2-NMe 2 ,5-F 0 A-3765 H H 0 H H H tetrahydropyran-4-yI H 2-NMe 2 ,6-F 0 A-3766 H H H H H 0 tetrahydropyran-4-yI H 2-NMe 2 ,5-Me 0 A-3767 H H 0 H H H tetrahydropyran-4-yI H 2-NMe 2 ,6-M e F A-3768 H H 0 H H H tetrahydropyran-4-yI H 2-CN,4-F 0 A-3769 H H 0 H H H tetrahydropyran-4-yI H 2-CN,5-F 0 A-3770 H H 0 H H H tetrahydropyran-4-yI H 2-CN,6-F 0 A-3771 H H 0 H H H tetrahydropyran-4-yI H 2-CN,6-M e 0 A-3772 H H 0 H H H tetrahydropyran-4-yI H 2-CN,5-OMe 0 A-3773 H H 0 H H H tetrahydropyran-4-yI H 2-CN,6-OMe 0 A-3774 H H 0 H H H tetrahydropyran-4-yI H 3-CN,6-Me 0 A-3775 H H 0 H H H tetrahydropyran-4-yI H 3-CN,6-OMe 0 A-3776 H H 0 H H H tetrahydropyran-4-yI H 4-CN,2-Me 0 A-3777 H H 0 H H H tetrahydropyran-4-yI H 4-CN,2-OMe 0 A-3778 H H 0 H H H tetrahydropyran-4-yI H 2-N0 2 ,4-F 0 A-3779 H H 0 H H H tetrahydropyran-4-yI H 2-N0 2 ,5-F 0 A-3780 H H 0 H H H tetrahydropyran-4-yI H 2-N0 2 ,6-F 0 A-3781 H H 0 H H H tetrahydropyran-4-yI H 2-N0 2,4--M e 0 A-3782 H H 0 H H H tetrahydropyran-4-yI H 2-N0 2,5-M e 0 A-3783 H H 0 H H H tetrahydropyran-4-yI H 2-N0 2,6-M e 0 A-3784 H H 0 H H H tetrahydropyran-4-yI H 2-M e,4,b- 2 0 A-3785 H H H H H 0 tetrahydropyran-4-yI H 2-Me,6-Et 0 A-3786 H H 0 H H H tetrahydropyran-4-yI H 2-cyclopropyl,6-OMe 0 A-3787 H H 0 H H H tetrahydropyran-4-yI H 2-Me,5-Et 0 A-3788 H H 0 H H H tetrahydropyran-4-yI H 2,6-Et2 0 A-3789 H H 0 H H H tetrahydropyran-4-yI H 2-Et,6-F 0 A-3790 H H H H H 0 tetrahydropyran-4-yI H 2-CH20CH3,6-C1 0 A-3791 H H 0 H H H tetrahydropyran-4-yI H 2-CH 200H 2CH 3 ,6-CI 0 A-3792 H H 0 H H H tetrahydropyran-4-yI H 2-CH 2 NMe 2 0 A-3793 H H H H H 0 CH 2CN H H 0 A-3794 H H 0 H H H CH 2CN H 2-F 0 A-3795 H H 0 H H H CH 2 CN H 2-C1 0 A-3796 H H 0 H H H CH 2 CN H 2-Br 0 A-3797 H H H H H 0 CH 2 CN H 2-OH 0 A-3798 H H 0 H H H CH 2 CN H 2-M e 0 A-3799 H H 0 H H H CH 2 CN H 2-Et 0 A-3800 H H 0 H H H CH 2CN H 2-Pr 0 A-3801 H H H H H 0 CH 2CN | H 2-GF 3 0 A-3802 H H H H H 0 CH 2CN H 2-CHF 2 0 A-3803 H H H H H 0 CH 2CN H 2-CH2f 0 A-3804 H H H H H 0 CH 2 CN H 2-CF 2C1 0 A-3805 H H H H H 0 CH 2 CN H 2-cycbpropyl 0 A-3806 H H H H H 0 CH 2 CN H 2-cyclobutyl 0 A-3807 H H H H H 0 CH 2CN H 2-cyclopentyl 0 A-3808 H H H H H 0 CH 2 CN H 2-ethenyl 0 A-3809 H H H H H CH 2CN H 2-allyl 0 A-3810 H H H H H CH 2CN H 2-(prop-1-en-1-yD 0 A-3811 H H H H H 0 CH 2 CN H 2-(trfflioroethenyD 0 A-3812 H H H H H 0 CH 2 CN H 2-0Me 0 A-3813 H H H H H 0 H 2CN H 2-0Et 0 A-3814 H H H H H 0 CH 2CN H 2-OPr 0
[0193]
[Table 68]
com pound R' R2 R R A R R' (R)m p A-3815 H H H H 0 CH 2CN H 2-0(/-Pr) 0 A-3816 H H H H f0 CH 2CN H 2-4)G 0 A-3817 H H H H E 0 CH 2CN H 2-CHF 2 0 A-3818 H H H H H CH 2CN H 2-(cycbpropy bxy) 0 A-3819 H H H H 0 CH 2CN H 2-(cycobbuty bxy) 0 A-3820 H H H H 0 CH 2CN H 2-(cycbpenty bxy) 0 A-3821 H H H H f Di CH 2CN H 2-((2,2-dbh brocycbpropy Doxy) 0 A-3822 H H H H 0 CH 2CN H 2-(oxiran-2-y D0 A-3823 H H H H H 0 CH 2CN H 2-SMe 0 A-3824 H H H H D 0 CH2CN H 3-SMe 0 A-3825 H H H H i 0 CH 2CN H 2-S =0 )M e 0 A-3826 H H H H D CH 2CN H 3-S (=0)M e 0 A-3827 H H H H CH 2CN H 2-S =0) 2M e A-3828 H H H H 0 CH 2CN H 3-S(= 0) 2M e 0 A-3829 H H H H 0 CH 2CN H 2-SG0 0 A-3830 H H H H f0 GH 2CN H 3-SG 0 A-3831 H H H H f0 GH 2 GN H 3-S (= U)G A-3832 H H H H 0 CH 2CN H 3-SCF (F)2 0
A-3833 H H H H f0 GH 2 GN H 2-(cycbpropytho) 0 A-3834 H H H H 0 CH 2CN H 2-(cycbpropy Isu finy D 0 A-3835 H H H H f0 CH 2CN H 2-(cycbpropy u fony 0 A-3836 H H H H f0 CH 2CN H 2-C (= 0)M e 0 A-3837 H H H H Ei0 CH 2CN H 2-GH 2C(= 0)H 3 0
A-3838 H H H H Hi0 CH 2CN H 2-GH 2C 0=U)F 3 0 A-3839 H H H H 0 GH 2CN H 2-CH 2 H 0 A-3840 H H H H Hi0 GH 2 GN H 2-GH 2 UH 3 A-3841 H H H H Hi0 CH 2CN H 2-GH 20H 2CH 3 0
A-3842 H H H H i 0 CH 2CN H 2-CH 2SCH 3 0 A-3843 H H H H 0 CH 2CN H 2-CH 2S =0 )H 3 0
A-3844 H H H H 0 CH 2CN H 2-CH 2S(= 0) 2 CH 3 A-3845 H H H H 0 CH 2CN H 2-(benzy bxy) 0 A-3846 H H H H 0 CH 2CN H 2-NH 2 A-3847 H H H H H 0 CH 2CN H 2-NHMe 0 A-3848 H H H H f0 CH 2CN H 2 NM e) 2 0 A-3849 H H H H 0 CH 2CN H 2-0,3-d bxoan-2-yD 0 A-3850 H H H H f Df CH 2CN H 2-0,3-d bxan-2-y D A-3851 H H H H f0 CH 2CN H 2-(l#-i idazoH2-yD 0 A-3852 H H H H 0 CH 2CN H 2-(thiazo -2-y) 0 A-3853 H H H H 0 CH 2CN H 2-(oxazol-2-y D 0 A-3854 H H H H H 0 CH 2CN H 2-CH= N0H 0 A-3855 H H H H 0 CH 2CN H 2-CH= NOM e 0 A-3856 H H H H 0 CH 2CN H 2-(4,b-dihydro-3-oxazo D 0 A-3857 H H H H Hf CH 2CN H 2-N 0 A-3858 H H H H H CH 2CN H 2-NO 2 0
A-3859 H H H H 0Di CH 2CN H 2-F,6-C1 0 A-3860 H H H H iif CH2CN H 2-F,6-Me 0 A-3861 H H H H 0Di CH 2CN H 3-F,6-M e 0 A-3862 H H H H 0 CH 2CN H 4-F,2-M e 0 A-3863 H H H H 0 CH 2CN H 2-F,6-M e 0 A-3864 H H H H f0 CH 2CN H 3-F,6-M e 0 A-3865 H H H H 0 CH 2CN H 2,6-C F A-3866 H H H H f0 CH 2CN H 2- 1,6-M e 0 A-3867 H H H H F CH 2CN H 3- 1,6-M e 0 A-3868 H H H H 0 CH 2CN H 4-01,2-M e 0 A-3869 H H H H H 0 CH 2CN H 2-C b,-CF 3 0 A-3870 H H H H 0 E CH 2 GN H 2-C1,6-0F 3 0 A-3871 H H H H f0 CH 2 GN H 2-C 1,6-0M e 0
[0194]
[Table 69]
com pound R' R2 R R A R R' (R)m p A-3872 H H H H 0 CH 2CN H 3-0 I,6-0M e 0 A-3873 H H H H 0 CH 2CN H 4-0 1,2-0Me A-3874 H H H H 0 CH 2CN H 2,4-M e 2 A-3875 H H H H if 0 CH 2CN H 2,b-M e 2 0 A-3876 H H H H D CH 2CN H 2,6-M e 2 0 A-3877 H H H H 0 CH 2CN H 2-M e,4-0F 3 0 A-3878 H H H H 0Di CH 2CN H 2-M e,b-F 3 0 A-3879 H H H H 0 CH 2CN H 2-M e,6-0F 3 0 A-3880 H H H H H 0 CH 2CN H 2 -Me,4-0Me 0 A-3881 H H H H if 0 CH 2CN H 2 -Me,b-0Me 0 A-388 Hf2 H H H i 0 CH 2CN H 2-M e,6-UM e 0 A-3883 H H H H D CH 2CN H 3-M e,6-0M e 0 A-3884 H H H H CH 2CN H 4-M e,2-M e 0 A-3885 H H H H 0 CH 2CN H 2,b-M e 2 0 A-3886 H H H H 0 CH 2CN H 2,6-0M e 2 0 A-3887 H H H H 0 GH 2CN H 2-1Me,6-GH 3 0 A-3888 H H H H f0 GH 2 GN H 2-GH2b-H 0 A-3889 H H H H 0 CH 2CN H 2-CH' 2,6-F 0 A-3890 H H H H H GH 2 GN H 2-GHF 2,b-M e 0 A-3891 H H H H 0 CH 2CN H 2-CHF 2,6-Me 0 A-3892 H H H H H CH 2CN H 2-cycbpropy 1,b-F 0 A-3893 H H H H H CH 2CN H 2-cycbpropy1,6-F 0 A-3894 H H H H D CH 2CN H 2-cyclopropylb-M e 0 A-3895 H H H H i 0 CH 2CN H 2-cyclopropyl,6-M e 0 A-3896 H H H H I GH 2CN H 2-etheny1,6-F 0 A-3897 H H H H 0 GH 2CN H 2-ethenyl,6- e 0 A-3898 H H H H f0 CH 2CN H 2-0Etb-F 0 A-3899 H H H H i 0 CH 2CN H 2-0Et6-F 0 A-3900 H H H H 0 CH 2CN H 2-0Etb-CI 0 A-3901 H H H H 0 CH 2CN H 2-OEt6-C I 0 A-3902 H H H H 0 CH 2CN H 2-0Etb-e 0 A-3903 H H H H 0 CH 2CN H 2-0Et6- e 0 A-3904 H H H H H 0 CH 2CN H 2-0CH F 2,b-F 0 A-3905 H H H H f0 GH 2 GN H 2-0CH H2,6-H 0 A-3906 H H H H 0 CH 2CN H 2-OCH F 2 ,b-Me 0 A-3907 H H H H EiF CH 2CN H 2-CH F2 ,6 A e 0 A-3908 H H H H H CH 2CN H 2-(cycobpropyloxy),b-F 0 A-3909 H H H H 0 CH 2CN H 2-(cycobpropyloxy),6-F 0 A-3910 H H H H 0 CH 2CN H 2-(cyclopropybxy),b-Me 0 A-3911 H H H H H 0 CH 2CN H 2-(cyclopropyoxy),6-Me 0 A-3912 H H H H 0 CH 2CN H 2-SM e,b-F 0 A-3913 H H H H 0 CH 2CN H 2-SM e,6-F 0 A-3914 H H H H CH 2CN H 2-SM e,b-M e 0 A-3915 H H H H CH 2CN H 2-SMe,6-M e 0 A-3916 H H H H f Di CH 2CN H 2-S(=0)Me,b-F 0 A-3917 H H H H CH 2CN H 2-S(= 0)Me,6-F 0 A-3918 H H H H 0 CH 2CN H 2-S(=0)Me,b-M e 0 A-3919 H H H H 0 CH 2CN H 2-S (=0)Me,6-M e 0 A-3920 H H H H 0 CH 2CN H 2-S(= 0Me,b-F 0 A-3921 H H H H E 0 CH 2CN H 2-S =U) 2Me,6-H 0 A-3922 H H H H D CH 2CN H 2-S(= 0) 2 Me,b-M e A-3923 H H H H H CH 2CN H 2-S = ) 2 Me,6--M e 0 A-3924 H H H H H7i CH 2CN H 2-SC3,b-F A-3925 H H H H 0 CH 2CN H 2-SCF 3 ,6-F 0 A-3926 H H H H H CH 2CN H 2-SCF 3 ,b-M e 0 A-3927 H H H H 0 CH 2 N H 2-SCF 3 ,6-M e 0 A-3928 H H H H f0 CH 2 GN H 2-S(=U)C3,b-F 0
[0195]
[Table 70]
com pound R' R2 R R A R R' (R)m p A-3929 H H H H 0 CH 2CN H 2-S (=O)0F 3 ,6-F 0 A-3930 H H H H 0 CH 2CN H 2-S(=O)CF 3 ,b-Me A-3931 H H H H E0 CH 2CN H 2-S(=O)CF 3 ,6-ie A-3932 H H H H i 0 CH 2CN H 2-S (= 0) 20F 3 ,b A-3933 H H H H 0 CH 2CN H 2-S (=U) 2CF 3 ,6-F W A-3934 H H H H 0 CH 2CN H 2-S (=U) 2CF 3 ,b-M e 0 A-3935 H H H H f Di CH 2CN H 2-S (=U) 2CF 3 ,6-M e 0 A-3936 H H H H 0 CH 2CN H 2-(cycobpropylth b),b-F 0 A-3937 H H H H H 0 CH 2CN H 2-(cycobpropylth b),6-F 0 A-3938 H H H H D 0 CH2CN H 2-(cycbpropy thio),b-M e 0 A-3939 H H H H i 0 CH 2CN H 2-(cycbpropy thio),6-M e 0 A-3940 H H H H D CH 2CN H 2- (=0)M e,b-F 0 A-3941 H H H H CH 2CN H 2- 0(= )M e,6-F 0 A-3942 H H H H 0 CH 2CN H 2-(= 0)M e,b-M e 0 A-3943 H H H H 0 CH 2CN H 2-(= 0)M e,6-M e 0 A-3944 H H H H 0 GH 2CN H 2-H 2UH,b-H 0 A-3945 H H H H f0 GH 2 GN H 2-H 2UN,6-F 0 A-3946 H H H H D CH 2CN H 2-CH 2UH, b-M e 0 A-3947 H H H H f0 GH 2 GN H 2-CH 20H,6-M e 0 A-3948 H H H H 0 CH 2CN H 2-0H 20H 3 ,4-F 0 A-3949 H H H H f0 CH 2CN H 2-GH 20H 3 ,b- 0 A-3950 H H H H f0 CH 2CN H 2-0H 20H 3 ,6-F 0 A-3951 H H H H 0 CH 2CN H 2-GH 20CH 3 ,4-i e 0 A-3952 H H H H f0 CH 2CN H 2-OH 20CH 3 ,b-i e 0 A-3953 H H H H CH 2CN H 2-GH 20CH 3 6-M e A-3954 H H H H CH 2CN H 2-0C(= 0)GH 3,b-F A-3955 H H H H i CH 2CN H 2-00(= 0)GH 3 ,6-F 0 A-3956 H H H H i 0 CH 2CN H 2-0(=0)CH 3 ,b-M e 0 A-3957 H H H H 0 CH 2CN H 2-0(=0)CH 3 ,6-M e 0 A-3958 H H H H 0 CH 2CN H 2-OS =0 ) 2 H 3 ,b-F 0 A-3959 H H H H 0 CH 2CN H 2-OS =0 ) 2 H 3 ,6-F 0 A-3960 H H H H 0 CH 2CN H 2-S(= 0) 2 CH 3,b- e 0 A-3961 H H H H f0 CH 2CN H 2-S(= 0) 2 CH 3,6-M e 0 A-3962 H H H H GH 2CN H 2-OH 2 S0H 3 ,b-H 0
A-3963 H H H H 0 CH 2CN H 2-OH 2 S0H 3 ,6-F 0 A-3964 H H H H f Di CH 2CN H 2-GH 2SCH 3,5-M e 0 A-3965 H H H H f0 CH 2CN H 2-GH 2SCH 3 ,6-M e 0 A-3966 H H H H 0 CH 2CN H 2NM e 2 ,b-F 0 A-3967 H H H H 0 CH 2CN H 2NM e 2,6-F 0 A-3968 H H H H H 0 CH 2CN H 2AM e 2 ,b-MA e 0 A-3969 H H H H 0 CH 2CN H 2AM e2,6-M Ae 0 A-3970 H H H H 0 CH 2CN H 2-ON,4-F 0 A-3971 H H H H Hi0 CH 2CN H 2-GN,b-F 0 A-3972 H H H H H CH 2CN H 2-GN,6-F 0 A-3973 H H H H D GH 2CN H 2-GN,6-M e 0 A-3974 H H H H 0 GH 2CN H 2-CN5-OMe 0 A-3975 H H H H 0Di CH 2CN H 2-GN,6-OM e 0 A-3976 H H H H 0 CH 2CN H 3-GN,6-M e 0 A-3977 H H H H 0 CH 2CN H 3-GN,6-OM e 0 A-3978 H H H H H GH 2CN H 4-ON,2-Me 0 A-3979 H H H H 0 CH 2CN H 4-GN,2-OM e 0 A-3980 H H H H i CH 2CN H 20 2 4-F 0 A-3981 H H H H Ei CH 2CN H 2-N0 2 b-F 0 A-3982 H H H H 0 CH 2CN H 2-N0 2 ,6-F 0 A-3983 H H H H H CH 2CN H 2-0 2,4-MAe 0 A-3984 H H H H H CH 2 GN H 2-N0 2,b-M e 0 A-3985 H HFFH CH 2CN H 2-N0 2,6-MAe 0
[0196]
[Table 71]
com pound RI R2 R R R A R R' (R)m P A-3986 H H H H H 0 CH 2 CN H 2-M e,4,5-F2 0 A-3987 H H H H H 0 CH 2 CN H 2-M e,6-Et 0 A-3988 H H H H H 0 CH 2 CN H 2-cyclopropyl,6-OM e 0 A-3989 H H H H H 0 CH 2 CN H 2-M e,5-Et 0 A-3990 H H H H H 0 CH 2 CN H 2,6-Et2 0 A-3991 H H H H H 0 CH 2 CN H 2-Et,6-F 0 A-3992 H H H H H 0 CH 2 CN H 2-CH 20CH3 ,6-C I 0 A-3993 H H H H H 0 CH 2 CN H 2-CH 20CH 2 CH 3 ,6-CI 0 A-3994 H H H H H 0 CH 2 CN H 2-CH 2NM e 2 0 A-3995 H H H H H 0 1-CN-cyclopropyl H H 0 A-3996 H H H H H 0 1-CN-cyclopropyl H 2-F 0 A-3997 H H H H H 0 1-CN-cyclopropyl H 2-Cl 0 A-3998 H H H H H 0 1-CN-cyclopropyl H 2-Br 0 A-3999 H H H H H 0 1-CN-cyclopropyl H 2-OH 0 A-4000 H H H H H 0 1-CN-cyclopropyl H 2-M e 0 A-4001 H H H H H 0 1-CN-cyclopropyl H 2-Et 0 A-4002 H H H H H 0 1-CN-cyclopropyl H 2-Pr 0 A-4003 H H H H H 0 1-CN-cyclopropyl H 2-CF 3 0 A-4004 H H H H H 0 1-CN-cyclopropy| H 2-UHF 2 0 A-4005 H H H H H 0 1-CN-cyclopropyl H 2-CH 2F 0 A-4006 H H H H H 0 1-CN-cyclopropy| H 2-CF 2C1 0 A-4007 H H H H H 0 1-CN-cyclopropyl H 2-cycbpropy 1 0 A-4008 H H H H H 0 1-CN-cyclopropyl H 2-cycobbutyl 0 A-4009 H H H H H 0 1-CN-cyclopropyl H 2-cycbpenty 1 0 A-4010 H H H H H 0 1-CN-cyclopropyl H 2-etheny 1 0 A-4011 H H H H H 0 1-CN-cyclopropyl H 2-a Ilyl 0 A-4012 H H H H H 0 1-CN-cyclopropyl H 2-(prop-1-en-1-y D 0 A-4013 H H H H H 0 1-CN-cyclopropy| H 2-(trifboroetheny D 0 A-4014 H H H H H 0 1-CN-cyclopropyl H 2-0M e 0 A-4015 H H H H H 0 1-CN-cyclopropyl H 2-0Et 0 A-4016 H H H H H 0 1-CN-cyclopropyl H 2-0Pr 0 A-4017 H H H H H 0 1-CN-cyclopropyl H 2-0 (/-Pr) 0 A-4018 H H H H H 0 1-CN-cyclopropyl H 2-0CF 0 A-4019 H H H H H 0 1-CN-cyclopropy| H 2-0CH F2 0 A-4020 H H H H H 0 1-CN-cyclopropyl H 2-(cycbpropy bxy) 0 A-4021 H H H H H 0 1-CN-cyclopropyl H 2-(cycbbuty bxy) 0 A-4022 H H H H H 0 1-CN-cyclopropyl H 2-(cycbpenty bxy) 0 A-4023 H H H H H 0 1-CN-cyclopropy H 2-((2,2-d ih brocycbpropy Doxy) 0 A-4024 H H H H H 0 1-CN-cyclopropy H 2-(oxiran-2-y D 0 A-4025 H H H H H 0 1-CN-cyclopropy H 2-SMe 0 A-4026 H H H H H 0 1-CN-cyclopropy H 3-SMe 0 A-4027 H H H H H 0 1-CN-cyclopropy H 2-S (=0)M e 0 A-4028 H H H H H 0 1-CN-cyclopropy H 3-S (=0)M e 0 A-4029 H H H H H 0 1-CN-cyclopropy H 2-S (=O)Me 0 A-4030 H H H H H 0 1-CN-cyclopropy H 3-S (=O06Me 0 A-4031 H H H H H 0 1-CN-cyclopropy H 2-SC3a 0 A-4032 H H H H H 0 1-CN-cyclopropy H 3-SCF 0 A-4033 H H H H H 0 1-CN-cyclopropy H 3-S (=0)CF 0 A-4034 H H H H H 0 1-CN-cyclopropyI H 3-SCF(CF3) 2 0 A-4035 H H H H H 0 1-CN-cyclopropyl H 2-(cycobpropy th b) 0 A-4036 H H H H H 0 1-CN-cyclopropyl H 2-(cycobpropylsu finy D 0 A-4037 H H H H H 0 1-CN-cyclopropyl H 2-(cycbpropylsulfonyD 0 A-4038 H H H H H 0 1-CN-cyclopropyl H 2-C (=0)M e 0 A-4039 H H H H H 0 1-CN-cyclopropyl H 2-CH 2C(=0)CH 3 0 A-4040 H H H H H 0 1-CN-cyclopropyl H 2-CH 2C(=0)CF3 0 A-4041 f H H H H 0 1-CN-cyclopropyl H 2-CH 2 0H 0 A-4042 H H IH H H 0 1-CN-cyclopropyl H 2-CH 2 0CH 3 0
[0197]
[Table 72]
com pound RI R2 R R R A R R' (R)m P A-4043 H H H H H 0 1-CN-cyclopropyl H 2-CH 2 0CH 2 CH3 0 A-4044 H H H H H 0 1-CN-cyclopropyl H 2-CH 2SCH3 0 A-4045 H H H H H 0 1-CN-cyclopropyl H 2-CH 2S (= )CH, 0 A-4046 H H H H H 0 1-CN-cyclopropyl H 2-CH 2S(= O) 2 CH 0 A-4047 H H H H H 0 1-CN-cyclopropyl H 2-(benzy bxy) 0 A-4048 H H H H H 0 1-CN-cyclopropyl H 2-NH 2 0 A-4049 H H H H H 0 1-CN-cyclopropyl H 2-NH M e 0 A-4050 H H H H H 0 1-CN-cyclopropyl H 2-N e)2 0 A-4051 H H H H H 0 1-CN-cyclopropyl H 2-(1,3-d bxo an-2-y D 0 A-4052 H H H H H 0 1-CN-cyclopropyl H 2-(1,3-d bxan-2-y D0 A-4053 H H H H H 0 1-CN-cyclopropyl H 2-(1H-m dazoE2-yD 0 A-4054 H H H H H 0 1-CN-cyclopropyl H 2-(thiazo -2-y ) 0 A-4055 H H H H H 0 1-CN-cyclopropyl H 2-(oxazol-2-y D 0 A-4056 H H H H H 0 1-CN-cyclopropyl H 2-CH= NOH 0 A-4057 H H H H H 0 1-CN-cyclopropyl H 2-CH= NOM e 0 A-4058 H H H H H 0 1-CN-cyclopropyI H 2-(4,5-d ihydro-3-oxazo D 0 A-4059 H H H H H 0 1-CN-cyclopropyl H 2-CN 0 A-4060 H H H H H 0 1-CN-cyclopropyl H 2-N0 2 0 A-4061 H H H H H 0 1-CN-cyclopropyl H 2-F,6-O 1 0 A-4062 H H H H H 0 1-CN-cyclopropyl H 2-F,6-M e 0 A-4063 H H H H H 0 1-CN-cyclopropyl H 3-F,6-M e 0 A-4064 H H H H H 0 1-CN-cyclopropyl H 4-F,2-M e 0 A-4065 H H H H H 0 1-CN-cyclopropyl H 2-F,6-OM e 0 A-4066 H H H H H 0 1-CN-cyclopropyl H 3-F,6-OM e 0 A-4067 H H H H H 0 1-CN-cyclopropyl H 2,6-0 0 A-4068 H H H H H 0 1-CN-cyclopropyl H 2-C 1,6-M e 0 A-4069 H H H H H 0 1-CN-cyclopropyl H 3-C ,6-M e 0 A-4070 H H H H H 0 1-CN-cyclopropyl H 4-C 1,2-M e 0 A-4071 H H H H H 0 1-CN-cyclopropyl H 2-C ,5-CF, 0 A-4072 H H H H H 0 1-CN-cyclopropyl H 2-C ,6- 3 0 A-4073 H H H H H 0 1-CN-cyclopropyl H 2-C 1,6-0M e 0 A-4074 H H H H H 0 1-CN-cyclopropyl H 3-C ,6-0M e 0 A-4075 H H H H H 0 1-CN-cyclopropyl H 4-C 1,2-0M e 0 A-4076 H H H H H 0 1-CN-cyclopropyl H 2,4-i e 2 0 A-4077 H H H H H 0 1-CN-cyclopropyl H 2,5- e 2 0 A-4078 H H H H H 0 1-CN-cyclopropyl H 2,6-M e 2 0 A-4079 H H H H H 0 1-CN-cyclopropyl H 2-M e,4-F 3 0 A-4080 H H H H H 0 1-CN-cyclopropyl H 2-M e,5-CF3 0 A-4081 H H H H H 0 1-CN-cyclopropyl H 2-M e,6-CF 3 0 A-4082 H H H H H 0 1-CN-cyclopropyl H 2-M e,4-0M e 0 A-4083 H H H H H 0 1-CN-cyclopropyl H 2-M e,5-0M e 0 A-4084 H H H H H 0 1-CN-cyclopropyl H 2-M e,6-0M e 0 A-4085 H H H H H 0 1-CN-cyclopropyl H 3-M e,6-0M e 0 A-4086 H H H H H 0 1-CN-cyclopropyl H 4-M e,2-0M e 0 A-4087 H H H H H 0 1-CN-cyclopropyl H 2,5-0M e 2 0 A-4088 H H H H H 0 1-CN-cyclopropyl H 2,6-0M e 2 0 A-4089 H H H H H 0 1-CN-cyclopropyl H 2-OM e,6-CF3 0 A-4090 H H H H H 0 1-CN-cyclopropyl H 2-OHF2,5-F 0 A-4091 H H H H H 0 1-CN-cyclopropyl H 2-OHF 2,6-F 0 A-4092 H H H H H 0 1-CN-cyclopropy| H 2-CH F 2,bie 0 A-4093 H H H H H 0 1-CN-cyclopropyl H 2-OHF 2,6-M e 0 A-4094 H H H H H 0 1-CN-cyclopropyl H 2-cycbpropy 1,5-F 0 A-4095 H H H H H 0 1-CN-cyclopropyl H 2-cycbpropy 1,6-F 0 A-4096 H H H H H 0 1-CN-cyclopropyl H 2-cyclopropyl,5-M e 0 A-4097 H H H H H 0 1-CN-cyclopropyl H 2-cyclopropyl,6-M e 0 A-4098 H H H H H 0 1-CN-cyclopropyl H 2-ethenyl,6-F 0 A-4099 H f F H H 0 1-CN-cyclopropyl H 2-etheny 1,6-M e 0
[0198]
[Table 73]
com pound RI R2 R R R A R R' (R)m P A-4100 H H H H H 0 1-CN-cyclopropyl H 2-0Et,5-F 0 A-4101 H H H H H 0 1-CN-cyclopropyl H 2-0Et,6-F 0 A-4102 H H H H H 0 1-CN-cyclopropyl H 2-0Et,5-CI A-4103 H H H H H 0 1-CN-cyclopropyl H 2-0Et,6-CI 0 A-4104 H H H H H 0 1-CN-cyclopropyl H 2-0Et,5-Me 0 A-4105 H H H H H 0 1-CN-cyclopropyl H 2-0Et,6-Me 0 A-4106 H H H H H 0 1-CN-cyclopropyl H 2-0CHF 2,5-F 0 A-4107 H H H H H 0 1-CN-cyclopropyl H 2-0CHF 2,6-F 0 A-4108 H H H H H 0 1-CN-cyclopropyl H 2-0CHF 2 ,5-Me 0 A-4109 H H H H H 0 1-CN-cyclopropyl H 2-0CHF 2 ,6-MAe 0 A-4110 H H H H H 0 1-CN-cyclopropyl H 2-(cycobpropyloxy),5-F 0 A-4111 H H H H H 0 1-CN-cyclopropyl H 2-(cycobpropyloxy),6-F 0 A-4112 H H H H H 0 1-CN-cyclopropyl H 2-(cyclopropybxy),5-M e 0 A-4113 H H H H H 0 1-CN-cyclopropyl H 2-(cyclopropybxy),6-M e 0 A-4114 H H H H H 0 1-CN-cyclopropyl H 2-SMe,5-F 0 A-4115 H H H H H 0 1-CN-cyclopropyl H 2-SMe,6-F 0 A-4116 H H H H H 0 1-CN-cyclopropyl H 2-SMe,5-Me 0 A-4117 H H H H H 0 1-CN-cyclopropyl H 2-SMe,6-Me 0 A-4118 H H H H H 0 1-CN-cyclopropyl H 2-S(0)Me,5-F 0 A-4119 H H H H H 0 1-CN-cyclopropyl H 2-S(=0)Me,6-F 0 A-4120 H H H H H 0 1-CN-cyclopropyl H 2-S(=0)Me,5-Me 0 A-4121 H H H H H 0 1-CN-cyclopropyl H 2-S (=0)M e,6-MA e 0 A-4122 H H H H H 0 1-CN-cyclopropyl H 2-S(=0) 2 Me,5-F 0 A-4123 H H H H H 0 1-CN-cyclopropyl H 2-S(=0) 2 Me,6-F 0 A-4124 H H H H H 0 1-CN-cyclopropyl H 2-S(=O) 2Me,b-M e 0 A-4125 H H H H H 0 1-CN-cyclopropyl H 2-S(=O) 2Me,6-Me 0 A-4126 H H H H H 0 1-CN-cyclopropyI H 2-SCF 3 ,b-F 0 A-4127 H H H H H 0 1-CN-cyclopropyI H 2-SCF 3 ,6-F 0 A-4128 H H H H H 0 1-CN-cyclopropyl H 2-SCF 3 ,5-Me 0 A-4129 H H H H H 0 1-CN-cyclopropyl H 2-SCF 3 ,6-Me 0 A-4130 H H H H H 0 1-CN-cyclopropyl H 2-S (=0)CF3,5-F 0 A-4131 H H H H H 0 1-CN-cyclopropyl H 2-S (=0)CF 3 ,6-F 0 A-4132 H H H H H 0 1-CN-cyclopropyl H 2-S(=0)CF 3 ,5-Me 0 A-4133 H H H H H 0 1-CN-cyclopropyl H 2-S(=O)CF3 ,6-Me 0 A-4134 H H H H H 0 1-CN-cyclopropyI H 2-S(=0) 2CF3 ,5-F 0 A-4135 H H H H H 0 1-CN-cyclopropyl H 2-S(=O) 20F 3 ,6-F 0 A-4136 H H H H H 0 1-CN-cyclopropyl H 2-S(=0) 2CF 3 ,b-Me 0 A-4137 H H H H H 0 1-CN-cyclopropyl H 2-S(=0) 2 CF3 ,6-Me 0 A-4138 H H H H H 0 1-CN-cyclopropyl H 2-(cycobpropylthb),5-F 0 A-4139 H H H H H 0 1-CN-cyclopropyl H 2-(cycobpropylthb),6-F 0 A-4140 H H H H H 0 1-CN-cyclopropyl H 2-(cycobpropylthio),5-M e 0 A-4141 H H H H H 0 1-CN-cyclopropyl H 2-(cycobpropylthio),6-M e 0 A-4142 H H H H H 0 1-CN-cyclopropyl H 2-C(=0)Me,5-F 0 A-4143 H H H H H 0 1-CN-cyclopropyl H 2-C(=0)Me,6-F 0 A-4144 H H H H H 0 1-CN-cyclopropyl H 2-C (=0)M e,5-M e 0 A-4145 H H H H H 0 1-CN-cyclopropyl H 2-C(=0)Me,6-Me 0 A-4146 H H H H H 0 1-CN-cyclopropyl H 2-CH 20H,5-F 0 A-4147 H H H H H 0 1-CN-cyclopropyl H 2-CH 20H,6-F 0 A-4148 H H H H H 0 1-CN-cyclopropyl H 2-CH20H, 5-M e 0 A-4149 H H H H H 0 1-CN-cyclopropyl H 2-CH 2 OH,6-Me 0 A-4150 H H H H H 0 1-CN-cyclopropyl H 2-CH 20CH 3 ,4-F 0 A-4151 H H H H H 0 1-CN-cyclopropyl H 2-CH 200H 3,b-F 0 A-4152 H H H H H 0 1-CN-cyclopropyl H 2-3H 2 00H3 ,6-F 0 A-4153 H H H H H 0 1-CN-cyclopropyl H 2-CH 20CH 3 ,4-M e 0 A-4154 IH H H H H 0 1-CN-cyclopropyl H 2-CH 20CH 3 ,5-M e 0 A-4155 H H H H H 0 1-CN-cyclopropyl H 2-CH 20CH 3 ,6-M e 0 A-4156 H Hf H H 1-CN-cyclopropyl H 2-0C(=0)CH 3 ,5-F 0
[0199]
[Table 74]
com pound RIR2 R R R A R R' (R)m P A-4157 H H H H H 0 1-CN-cyclopropyl H 2-0C (=O)CH,,6-F 0 A-4158 H H H H H 0 1-CN-cyclopropyl H 2-0C (=0)CH 3 ,5-Me 0 A-4159 H H H H H 0 1-CN-cyclopropyl H 2-0C (=0)CH 3 ,6-M0e A-4160 H H H H H 0 1-CN-cyclopropyl H 2-OS (= ) 2CH,b-F 0 A-4161 H H H H H 0 1-CN-cyclopropyl H 2-OS (= ) 2CH 3 ,6-F 0 A-4162 H H H H H 0 1-CN-cyclopropyl H 2-OS (= ) 2CH 3,b- e 0 A-4163 H H H H H 0 1-CN-cyclopropyl H 2-OS(= 0) 2CH 3 ,6-M e 0 A-4164 H H H 0 H H 1-CN-cyclopropyl H 2-CH 2 SCH 3 ,b-F 0 A-4165 H H H 0 H H 1-CN-cyclopropyl H 2-CH 2 SCH 3 ,6-F 0 A-4166 H H H 0 H H 1-CN-cyclopropyl H 2-CH 2SCH 3 ,b--M e 0 A-4167 H H H H H 0 1-CN-cyclopropyl H 2-CH 2SCH 3,6-M e 0 A-4168 H H H H H 0 1-CN-cyclopropyl H 2-NM e 2 ,5-F 0 A-4169 H H H H H 0 1-CN-cyclopropyl H 2-NM e 2 ,6-F 0 A-4170 H H H H H 0 1-CN-cyclopropyl H 2-NM e 2 ,5-b e 0 A-4171 H H H H H 0 1-CN-cyclopropyl H 2-NM e 2 ,6-M e 0 A-4172 H H H H H 0 1-CN-cyclopropyl H 2-CN,4-F 0 A-4173 H H H H H 0 1-CN-cyclopropyl H 2-CN,5-F 0 A-4174 H H H H H 0 1-CN-cyclopropyl H 2-CN,6-F 0 A-4175 H H H H H 0 1-CN-cyclopropyl H 2-CN,6-M e 0 A-4176 H H H H H 0 1-CN-cyclopropyl H 2-CN,5-OM e 0 A-4177 H H H H H 0 1-CN-cyclopropyl H 2-CN,6-OM e 0 A-4178 H H H H H 0 1-CN-cyclopropyl H 3-CN,6-M e 0 A-4179 H H H H H 0 1-CN-cyclopropyl H 3-CN,6-OM e 0 A-4180 H H H H H 0 1-CN-cyclopropyl H 4-CN,2-M e 0 A-4181 H H H H H 0 1-CN-cyclopropyl H 4-CN,2-OM e 0 A-4182 H H H H H 0 1-CN-cyclopropyl H 2-N0 2,4-F 0 A-4183 H H H H H 0 1-CN-cyclopropyl H 2-N0 2 ,b-F 0 A-4184 H H H H H 0 1-CN-cyclopropyl H 2-N0 2 ,6-F 0 A-4185 H H H H H 0 1-CN-cyclopropyl H 2-N0 2,4-Ae 0 A-4186 H H H H H 0 1-CN-cyclopropyl H 2-N0 2,b- e 0 A-4187 H H H H H 0 1-CN-cyclopropyl H 2-NO 2,6-M e 0 A-4188 H H H H H 0 1-CN-cyclopropyl H 2-M e,4,5-F2 0 A-4189 H H H H H 0 1-CN-cyclopropyl H 2-M e,6-Et 0 A-4190 H H H H H 0 1-CN-cyclopropyl H 2-cyclopropyl,6-OM e 0 A-4191 H H H H H 0 1-CN-cyclopropyl H 2-M e,5-Et 0 A-4192 H H H H H 0 1-CN-cyclopropyl H 2,6-Et2 0 A-4193 H H H H H 0 1-CN-cyclopropyl H 2-Et,6-F 0 A-4194 H H H H H 0 1-CN-cyclopropyl H 2-CH 20CH 3 ,6-CI 0 A-4195 H H H H H 0 1-CN-cyclopropyl H 2-CH 20CH 2CH ,6-C| 0 A-4196 H H H H H 0 1-CN-cyclopropyl H 2-CH 2 NM e 2 0 A-4197 H H H H H 0 CH 20H H H 0 A-4198 H H H H H 0 CH 20H H 2-F 0 A-4199 H H H H H 0 22H 0H H 2-C1 0 A-4200 H H H H H 0 CH 20H H 2-Br 0 A-4201 H H H H H 0 CH 2OH H 2-OH 0 A-4202 H H H H H 0 CH 20H H 2-M e 0 A-4203 H H H H H 0 CH 20H H 2-Et 0 A-4204 H H H H H 0 CH 20H H 2-Pr 0 A-4205 H H H H H 0 CH 20H H 2-CF 3 0 A-4206 H H H H H 0 CH 20H H 2-CHF 2 0 A-4207 H H H H H 0 CH 20H H 2-CH 2F 0 A-4208 H H H H H 0 CH 20H H 2-0F 20 1 0 A-4209 H H H H H 0 22H OH H 2-cycbpropy 1 0 A-4210 H H H H H 0 CH 20H H 2-cycbbutyl 0 A-4211 H H H H H 0 CH 20H H 2-cycbpenty 1 0 A-4212 f H H H H 0 CH 2UH H 2-etheny 1 0 A-4213 iH H HIH H 0 CH 20H H 2-a Ilyl 0
[0200]
[Table 75]
com pound R' R2 R R A R R' (R)m p A-4214 H H H H 0 CH 20H H 2-(prop-l-en-1-yD 0 A-4215 H H H H i 0 CH 20H H 2-(trfboroetheny D A-4216 H H H H 0 CH 20H H 2-0M e A-4217 H H H H i 0 CH 2UH H 2-UEt A-4218 H H H H 0 CH 20H H 2-OPr 0 A-4219 H H H H 0 CH 20H H 2-0 (/-Pr) 0 A-4220 H H H H f Di CH 20H H 2G-0H 3 A-4221 H H H H 0 CH 20H H 2-0CH F2 A-4222 H H H H H 0 CH 20H H 2-(cycbpropy bxy) 0 A-4223 H H H H D0 CH2UH H 2-(cycobbuty bxy) 0 A-4224 H H H H if 0 CH 2UH H 2-(cycbpentybxy) 0 A-4225 H H H H D CH 2UH H 2-((2,2-d bh brocycbpropy Doxy) 0 A-4226 H H H H CH 2UH H 2-(oxiran-2-y D 0 A-4227 H H H H 0 CH 20H H 2-SMe 0 A-4228 H H H H 0 CH 20H H 3-SMe 0 A-4229 H H H H 0 GH 2UH H 2-S = )M e 0 A-4230 H H H H 0 GH 2UH H 3-S =0 )M e 0 A-4231 H H H H E 0 CH 20H H 2-S(= 0) 2Me 0 A-4232 H H H H 0 GH 2UH H 3-S =U) 2M e A-4233 H H H H 0 CH 20H H 2-SG,3 A-4234 H H H H 0 CH 20H H 3-SGH3 0 A-4235 H H H H f0 CH 20H H 3-S (=0)CF3 0 A-4236 H H H H 0 CH 20H H 3-SCF(F3 2 0 A-4237 H H H H 0 CH 20H H 2-(cycbpropy th) 0 A-4238 H H H H 0 GH 2UH H 2-(cycbpropy Isu finy D 0 A-4239 H H H H 0 GH 2UH H 2-(cycbpropy u fony D 0 A-4240 H H H H H CH 2UH H 2-C (=0)M e 0 A-4241 H H H H i 0 CH 20H H 2-GH 2 0(= )CH3 0 A-4242 H H H H 0 CH 20H H 2-GH 2C 0= )CF 3 A-4243 H H H H 0 CH 20H H 2-CH 2 UH 0 A-4244 H H H H 0 CH 20H H 2-0H 20H 3 A-4245 H H H H 0 CH 20H H 2-0H 2 0H 2CH 3 0
A-4246 H H H H H 0 CH 20H H 2-CH 2SCH 3 0 A-4247 H H H H H0 0 GH2U H 2-CH2S(= )H 3 0
A-4248 H H H H 0 CH 20H H 2-CH 2S(= 0) 2 CH 3 A-4249 H H H H D CH 2UH H 2-(benzy bxy) A-4250 H H H H f0 CH 2UH H 2-NH 2 A-4251 H H H H D CH 20H H 2-NHMe 0 A-4252 H H H H 0 CH 20H H 2 N e)2 0 A-4253 H H H H H 0 CH 20H H 2-0,3-d bxolan-2-yD 0 A-4254 H H H H 0 CH 20H H 2-0,3-d bxan-2-y D 0 A-4255 H H H H 0 CH 20H H 2-(1H-m idazokF2-yD 0 A-4256 H H H H f CH 2UH H 2-(thiazo -2-y) 0 A-4257 H H H H F CH 2UH H 2-(oxazo -2-yD 0 A-4258 H H H H D 0 CH2UH H 2-CH=N0H 0 A-4259 H H H H H CH 2UH H 2-CH= NOM e 0 A-4260 H H H H 0 CH 20H H 2-(4,b-dihydro-3-oxazo D 0 A-4261 H H H H 0 CH 20H H 2-ON 0 A-4262 H H H H 0 CH 20H H 2-NO 2 0
A-4263 H H H H Hi0 CH 2UH H 2-F,6-C1 0 A-4264 H H H H Ei0 CH 20H H 2-F,6-M e F A-4265 H H H H f0 CH 2UH H 3-F,6-M e 0 A-4266 H H H H EF CH 2UH H 4-F,2-M e 0 A-4267 H H H H 0 CH 20H H 2-F,6-OM e 0 A-4268 H H H H f0 CH 20H H 3-F,6-OM e 0 A-4269 H H H H Hi0 CH 2UH H 2,6-Cl 0 A-4270 H H H H f0 CH 2UH H 2- 1,6-M e 0
[0201]
[Table 76]
com pound R' R2 R R A R R' (R)m p A-4271 H H H H 0 CH 20H H 3-C I,6- e 0 A-4272 H H H H 0 CH 20H H 4-C1,2-Me A-4273 H H H H 0 CH 20H H 2-C 1,b- 3 A-4274 H H H H i 0 CH 2UH H 2-C ,6-F 3 A-427b H H H H 0 CH 20H H 2-C ,6-0M e 0 A-4276 H H H H 0 CH 20H H 3-C ,6-0M e 0 A-4277 H H H H f Di CH 20H H 4-C I,2-0M e 0 A-4278 H H H H 0 CH 20H H 2,4-M e 2 0 A-4279 H H H H H 0 CH 20H H 2,b-M e 2 0 A-4280 H H H H if 0 CH 2UH H 2,6-M e 2 0
A-4281 H H H H i 0 CH 2UH H 2-M e,4-FH 3 0 A-4282 H H H H D CH 2UH H 2-M e,b-F 3 0 A-4283 H H H H CH 2UH H 2-M e,6-F 3 0 A-4284 H H H H 0 CH 20H H 2 -Me,4-0Me 0 A-428b H H H H 0 CH 20H H 2 -Me,b-0Me 0 A-4286 H H H H f0 H 2UH H 2-M e,6-UM e 0 A-4287 H H H H Ei0 H 2UH H 3 -Me,6-UMe 0 A-4288 H H H H Ei0 CH 20H H 4-M e,2-0Me A-4289 H H H H 0 GH 2UH H 2,b-M e2 0
A-4290 H H H H 0 CH 20H H 2,6-0M e 2 0 A-4291 H H H H H CH 20H H 2-0Me,6-F 3 0 A-4292 H H H H Hi0 CH 20H H 2-CHF 2,b-F 0 A-4293 H H H H 0 CH 20H H 2-CHF 2,6-F 0 A-4294 H H H H H CH 20H H 2-CHF 2,b-Me 0 A-4295 H H H H f0 GH 2 H H 2-CHF 2,6-M e 0 A-4296 H H H H 0 GH 2UH H 2-cycbpropy 1,b-F 0 A-4297 H H H H 0 CH 2UH H 2-cycbpropy1,6-F 0 A-4298 H H H H i 0 CH 20H H 2-cyclopropyLb-M e 0 A-4299 H H H H D CH 20H H 2-cyclopropyL,6-M e 0 A-4300 H H H H 0 CH 20H H 2-ethenyl,6-F 0 A-4301 H H H H D CH 20H H 2-ethenyl,6- e 0 A-4302 H H H H 0 CH 20H H 2-0Etb-F 0 A-4303 H H H H H 0 CH 20H H 2-0Et6-F 0 A-4304 H H H H H GH 2UN H 2-0Etb-CI 0 A-430b H H H H 0 CH 20H H 2-OEt6-C I 0 A-4306 H H H H f Di CH 2UH H 2-0Etb-M e 0 A-4307 H H H H 0 CH 2UH H 2-0Et6-M e 0 A-4308 H H H H 0 CH 20H H 2-0CH F 2,b-F 0 A-4309 H H H H 0 CH 20H H 2-0CH F 2,6-F 0 A-4310 H H H H H 0 CH 20H H 2-OCH F 2 ,b-M e 0 A-4311 H H H H 0 CH 20H H 2-CH F 2,6-Me 0 A-4312 H H H H 0 CH 20H H 2-(cycobpropyloxy),b-F 0 A-4313 H H H H CH 2UH H 2-(cycobpropyloxy),6-F 0 A-4314 H H H H CH 2UH H 2-(cyclopropy oxy),b-M e 0 A-431b H H H H f Di CH 2UH H 2-(cyclopropy bxy),6-M e 0 A-4316 H H H H H CH 2UH H 2-SMe,b-F 0 A-4317 H H H H 0Di CH 20H H 2-SMe,6-F 0 A-4318 H H H H 0 CH 20H H 2-SM e,b- e 0 A-4319 H H H H 0 CH 20H H 2-SM e,6-M e 0 A-4320 H H H H H CH 2UH H 2-S(= 0)Me,b-F 0 A-4321 H H H H E 0 CH 20H H 2-S(=0)Me,6-F F A-4322 H H H H H CH 2UH H 2-S = )Me,b5- e 0 A-4323 H H H H H CH 2UH H 2-S (=0 )Me,6-Me 0 A-4324 H H H H 0 CH 20H H 2-S(= 0) 2 Me,b-F 0 A-432b H H H H 0 CH 20H H 2-S(= 0) 2M e,6-F 0 A-4326 H H H H H CH 2UH H 2-S = ) 2 Me,b5- e 0 A-4327 H H H H 0 CH 2UH H 2-S (=0 )M e,6 -e 0
[0202]
[Table 77]
com pound R' R2 R R A R R' (R)m p A-4328 H H H H 0 CH 20H H 2-SCH3,b-F 0 A-4329 H H H H H 0 CH 20H H 2-SCF 3,6-F 0 A-4330 H H H H 0 CH 20H H 2-SCF 3 ,b-M e 0 A-4331 H H H H i 0 CH 2UH H 2-SCF 3 ,6-M e 0 A-4332 H H H H 0 CH 20H H 2-S =U)0F 3 ,b-F 0 A-4333 H H H H 0 CH 20H H 2-S =U)0F 3 ,6-F 0 A-4334 H H H H 0 CH 20H H 2-S(= )CF 3 ,b-M e 0 A-4335 H H H H 0 CH 20H H 2-S(= )CF 3 ,6-M e 0 A-4336 H H H H 0 CH 20H H 2-S (=0) 2 F 3 ,b-F 0 A-4337 H H H H D i0 CH2UH H 2-S (=U) 2F3,6-F 0 A-4338 H H H H i 0 CH 2UH H 2-S =U) 2CF 3 ,b-M e A-4339 H H H H D CH 2UH H 2-S=U) 2CF 3 ,6-M e 0 A-4340 H H H H CH 2UH H 2-(cycobpropylth ),b-F 0 A-4341 H H H H 0 CH 20H H 2-(cycobpropylth b),6-F 0 A-4342 H H H H 0 CH 20H H 2-(cycbpropy thio),b-M e 0 A-4343 H H H H 0 GH 2UH H 2-(cycbpropy thio),6-M e 0 A-4344 H H H H E0 GH 2UH H 2-(= 0)Me,b-F 0 A-4345 H H H H E 0 H 20H H 2-0(=0)Me,6-F 0 A-4346 H H H H 0 GH 2UH H 2-(= U)M e,b-M e 0 A-4347 H H H H 0 CH 20H H 2-(= 0)M e,6-M e 0 A-4348 H H H H 0 CH 20H H 2-GH 20H,b-F 0 A-4349 H H H H f0 CH 20H H 2-GH 20H,6-F 0 A-4350 H H H H D0H20H H 2-0H 20H,b5-M e 0 A-4351 H H H H f0 CH 20H H 2-0H 20H,6 -Me 0 A-4352 H H H H HF CH 2UH H 2-GH 20H 3,4-F 0 A-4353 H H H H H F CH 2UH H 2-GH 20H 3,b-F A-4354 H H H H HiF CH 2UH H 2-GH 20H 3 ,6-F 0 A-4355 H H H H i 0 CH 20H H 2-GH 20CH 3 ,4-i e 0 A-4356 H H H H D 0H 20H H 2-OH20CH3,b-Me A-4357 H H H H 0 H20H H 2-GH 20CH 3 ,6-M e 0 A-4358 H H H H 0 CH 20H H 2-0 C= 0)CH 3 ,b- 0 A-4359 H H H H 0 CH 20H H 2-0 C= 0)CH 3,6-F 0 A-4360 H H H H f0 CH 20H H 2-00(=0)CH 3 ,b-M e 0 A-4361 H H H H F GH 2UH H 2-C0(=U)CH 3 ,6-M e 0 A-4362 H H H H 0 CH 20H H 2-OS =0 ) 2 H 3 ,b- F A-4363 H H H H f Di CH 2UH H 2-0S =OUH)2 3 ,6-F 0 A-4364 H H H H H CH 2UN H 2-OS =O ) 2 CH 3,b-M e 0 A-4365 H H H H 0 CH 20H H 2-S(= 0) 2 CH 3,6-M e 0 A-4366 H H H H 0 CH 20H H 2-OH 2 SCH 3 ,b-4 0 A-4367 H H H H H 0 CH 20H H 2-OH 2 SCH 3 ,6-F 0 A-4368 H H H H 0 CH 20H H 2-OH 2SCH 3 ,b-M e 0 A-4369 IfH H H H D H20H H 2-GH 2SCH 3,6-M e 0 A-4370 H H H H E 0 CH 2UN H 2-AMe 2 ,b-H A-4371 H H H H E 0 CH 2UN H 2-NMe 2 ,6-F 0 A-4372 H H H H D GH 2UH H 2AM e2 ,- -e 0 A-4373 H H H H f0 GH 2UH H 2AM e2 ,6-A e 0 A-4374 H H H H D 0 H0H2 H 2-ON,4-F 0 A-4375 H H H H 0 CH 20H H 2-GN,b-F 0 A-4376 H H H H 0 CH 20H H 2-ON,6-F 0 A-4377 H H H H Ei0 H 2UN H 2-N,6 -Me 0 A-4378 H H H H Ei0 H 20H H 2-CN,b-OMe 0 A-4379 H H H H 0 GH 2UH H 2-ON,6-0M e 0 A-4380 H H H H H GH 2UN H 3-CN,6-M e 0 A-4381 H H H H D 0H20H H 3-N,6-OMe 0 A-4382 H H H H H 0 H 20H H 4-ON,2-Me 0 A-4383 H H H H 0 GH 2UH H 4-GN,2-0M e 0 A-4384 H H 7iH H i0 H 20H H 2-0 2 ,4-F
[0203]
[Table 78]
com pound R' R2 R R A R R' (R)m p A-4385 H H H H 0 CH 20H H 2-N0 2 ,b-F 0 A-4386 H H H H f0 CH 20H H 2-N0 2 ,64 0 A-4387 H H H H 0 CH 20H H 2-NU 2,4-MAe 0 A-4388 H H H H i 0 CH 2UH H 2-NU 2,b-M e 0 A-4389 H H H H D CH 20H H 2-NU 2,6-Me 0 A-4390 H H H H 0 CH 20H H 2-Me,4,b-F 2 0 A-4391 H H H H D CH 20H H 2-M e,6-Et 0 A-4392 H H H H 0 CH 20H H 2-cyclopropyl,6-OMe 0 A-4393 H H H H H 0 CH 20H H 2-M e,b-Et 0 A-4394 H H H H D 0 CH2UH H 2,6-Et2 0 A-4395 H H H H i 0 CH 2UH H 2-Et,6-F 0 A-4396 H H H H D CH 2UH H 2-GH 20H 3,6-CI 1 A-4397 H H H H i CH 2UH H 2-GH 20H 2 CH 3 ,6-C 1F A-4398 H H H H 0 CH 20H H 2-CH 2 NMe 2 0 A-4399 H H H H 0Di NH 2 H H 0 A-4400 H H H H H 0 NH 2 H 2-F 0 A-4401 H H H H H NH 2 H 2-Cl 0 A-4402 H H H H f Di NH 2 H 2-Br 0 A-4403 H H H H H NH 2 H 2-OH 0 A-4404 H H H H 0Di NH 2 H 2-Me 0 A-4405 H H H H Hi0 NH 2 H 2-Et 0 A-4406 H H H H f0 NH 2 H 2-Pr 0 A-4407 H H H H 0 NH 2 H 2-CF 3 0
A-4408 H H H H Hi0 NH 2 H 2-UHF 2 0 A-4409 H H H H i NH 2 H 2-CH 2F 0 A-4410 H H H H i NH 2 H 2-H 2 G1 A-4411 H H H H f0 NH 2 H 2-cycbpropyl 0 A-4412 H H H H i 0 NH 2 H 2-cycobbutyl 0 A-4413 H H H H 0 NH 2 H 2-cycobpentyl 0 A-4414 H H H H 0 NH 2 H 2-ethenyl 0 A-4415 H H H H 0 NH 2 H 2-allyl A-4416 H H H H 0 NH 2 H 2-(prop-1-en-1-y) 0 A-4417 H H H H 0 NH 2 H 2-(triftLoroethenyD 0 A-4418 H H H H NH 2 H 2-UMe 0 A-4419 H H H H 0 NH 2 H 2-OEt A-4420 H H H H f Df NH 2 H 2-OPr 0 A-4421 H H H H f0 NH 2 H 2-0(/-Pr) 0 A-4422 H H H H 0 NH 2 H 2-0 G3 A-4423 H H H H 0 NH 2 H 2-CHF 2 0
A-4424 H H H H H 0 NH 2 H 2-(cycbpropybxy) 0 A-4425 H H H H 0 NH 2 H 2-(cycobbutyloxy) 0 A-4426 H H H H 0 NH 2 H 2-(cycobpentybxy) 0 A-4427 H H H H NH 2 H 2-((2,2-dichbrocycobpropyl)oxy) 0 A-4428 H H H H NH 2 H 2-(oxiran-2-yD A-4429 H H H H 0 NH 2 H 2-SMe 0 A-4430 H H H H f0 NH 2 H 3-SMe 0 A-4431 H H H H D NH 2 H 2-S(=0)Me 0 A-4432 H H H H 0 NH 2 H 3-S(=0)Me 0 A-4433 H H H H 0 NH 2 H 2-S(=0)2 Me 0 A-4434 H H H H f0 NH 2 H 3-S(=0) 2Me 0 A-4435 H H H H 0 NH 2 H 2-SCFH3 0
A-4436 H H H H f0 NH 2 H 3-SGH3 A-4437 H H H H F NH 2 H 3-S (=0)GH3 A-4438 H H H H 0 NH 2 H 3-SCF(CF3)2 A-4439 H H H H f0 NH 2 H 2-(cycobpropyltho) 0 A-4440 H H H H f0 NH 2 H 2-(cycbpropysufinyD 0 A-4441 H H H H f0 NH 2 H 2-(cycbpropylsulfonyD 0
[0204]
[Table 79]
com pound R' R2 R R A R R' (R)m p A-4442 H H H H 0 NH 2 H 2-C(=0)Me 0 A-4443 H H H H 0 NH 2 H 2-GH 20(=O)0H 3 0 A-4444 H H H H 0 NH 2 H 2-GH 20(=O)0F3 A-4445 H H H H i 0 NH 2 H 2-CH 2 UN A-4446 H H H H 0 NH 2 H 2-0H 20H 3 0 A-4447 H H H H 0 NH 2 H 2-0H 2 0H2 CH 3 0 A-4448 H H H H 0Di NH 2 H 2-CH 2SCH 3 0 A-4449 H H H H 0 NH 2 H 2-CH 2S(=U)CH 3 A-4450 H H H H i 0 NH 2 H 2-CH 2S(=U) 2 CH3 A-4451 H H H H i 0 NH 2 H 2-(benzybxy) 0 A-4452 H H H H i 0 NH 2 H 2-NH 2 A-4453 H H H H i 0 NH 2 H 2-NHMe 0 A-4454 H H H H f0 NH 2 H 2-N (Me)2 0 A-4455 H H H H 0 NH 2 H 2-(1,3-dbxolan-2-yD 0 A-4456 H H H H 0 NH 2 H 2-(1,3-dbxan-2-yD 0 A-4457 H H H H ii f NH2 H 2-(lH-i idazol-2-yD 0 A-4458 H H H H 0 NH 2 H 2-(thiazol-2-yl) 0 A-4459 H H H H 0 NH 2 H 2-(oxazol1-2-y) 0 A-4460 H H H H H0f NH 2 H 2-CH=NUH 0 A-4461 H H H H 0 NH 2 H 2-CH=NOM e 0 A-4462 H H H H 0 NH 2 H 2-(4,b-dihydro-3-IsoxazolyD A-4463 H H H H H 0 NH 2 H 2-N 0 A-4464 H H H H 0 NH 2 H 2-NO 2 0
A-4465 H H H H H 0 NH 2 H 2-F,6-C1 0 A-4466 H H H H HF NH 2 H 2-F,6-Me 0 A-4467 H H H H H D NH 2 H 3-F,6-Me 0 A-4468 H H H H HD NH 2 H 4-F,2-Me 0 A-4469 H H H H i 0 NH 2 H 2-F,6-UMe 0 A-4470 H H H H 0 NH 2 H 3-F,6-0Me 0 A-4471 H H H H 0 NH 2 H 2,6-C 12 A-4472 H H H H 0 NH 2 H 2-GI,6-M e 0 A-4473 H H H H 0 NH 2 H 3-GI,6-M e 0 A-4474 H H H H H 0 NH 2 H 4-GI,2-M e 0 A-4475 H H H H 0 H NH 2 H 2-CIb-C 3 A-4476 H H H H 0 H NH 2 H 2-CI,6-CF 3 A-4477 H H H H 0 NH 2 H 2-C,6-0Me 0 A-4478 H H H f H NH 2 H 3-C,6-UMe 0 A-4479 H H H H 0 NH 2 H 4-C,2-0Me 0 A-4480 H H H H 0 NH 2 H 2,4-M e2 0
A-4481 H H H H H 0 NH 2 H 2,b-M e 2 0 A-4482 H H H H 0 NH 2 H 2,6-M e2 0
A-4483 H H H H 0 NH 2 H 2-M e,4-CF 3 0 A-4484 H H H H 0 NH 2 H 2-M e,b-GH 3 0 A-4485 H H H H 0 NH 2 H 2-M e,6-GH 3 0 A-4486 H H H H f NH 2 H 2-M e,4-0Me A-4487 H H H H iff NH2 H 2-M e,b-UMe 0 A-4488 H H H H 0Di NH 2 H 2-M e,6-OMe 0 A-4489 H H H H 0 NH 2 H 3-M e,6-OMe 0 A-4490 H H H H 0 NH 2 H 4-M e,2-OMe 0 A-4491 H H H H f NH 2 H 2,b-UMe 2 0 A-4492 H H H H 0 NH 2 H 2,6-UMe 2 0 A-4493 H H H H f NH 2 H 2-OMe,6-GH 3 0 A-4494 H H H H Hf NH 2 H Z-GHH 2,b-H 0 A-4495 H H H H H0 NH 2 H 2-CHF 2,6-F 0 A-4496 IH H H H 0 NH 2 H 2-CHF 2,b-M e 0 A-4497 H H H H 0 NH 2 H 2-CHF 2,6-M e 0 A-4498 H H H H 0 NH 2 H 2-cycbpropyLb- 0
[0205]
[Table 80]
com pound R' R2 R R A R R' (R)m p A-4499 H H H H 0Di NH 2 H 2-cycbpropyl,6-F 0 A-4500 H H H H i 0 NH 2 H 2-cyclopropylb-Me A-4501 H H H H 0 NH 2 H 2-cyclopropyl,6-M e A-4502 H H H Hi NH 2 H 2-ethenyl,6-F 0 A-4503 H H H H 0 NH 2 H 2-ethenyl,6-Me 0 A-4504 H H H H 0 NH 2 H 2-OEt,b-F 0 A-4505 H H H H 0 NH 2 H 2-OEt,6-F 0 A-4506 H H H H 0 NH 2 H 2-OEt,b-CI 0 A-4507 H H H H H 0 NH 2 H 2-OEt,6-CI 0 A-4508 H H H H i 0 NH 2 H 2-OEt,b-M e 0 A-4509 H H H H 0 NH 2 H 2-UEt,6-M e 0 A-4510 H H H H 0 NH 2 H 2-CHH 2,b- 0 A-4511 H H H H f0 NH 2 H 2-CHH 2,6- 0 A-4512 H H H H 0 NH 2 H 2-CHF 2 ,b--M e 0 A-4513 H H H H 0 NH 2 H 2-CHF 2 ,6-M e 0 A-4514 H H H H 0 NH 2 H 2-(cyclopropyloxy),b-F 0 A-4515 H H H H 0 NH 2 H 2-(cyclopropyloxy),6-F 0 A-4516 H H H H 0 NH 2 H 2-(cyclopropybxy),b-M e 0 A-451 7 H H H H 0 NH 2 H 2-(cyclopropyloxy),6-M e 0 A-4518 H H H H 0 NH 2 H 2-SMe,b-F 0 A-4519 H H H H 0 NH 2 H 2-SMe,6-F 0 A-4520 H H H H 0 NH 2 H 2-SMe,b-Me 0 A-4521 H H H H 0 NH 2 H 2-SMe,6-M e 0 A-4522 H H H H 0 NH 2 H 2-S(=0)Me,b-F 0 A-4523 H H H H 0 NH 2 H 2-S(=0)Me,6-F 0 A-4524 H H H H H 0 NH 2 H 2-S(=0)Me,b-M e 0 A-4525 H H H H 0 NH 2 H 2-S(=0)Me,6-M e 0 A-4526 H H H H i 0 NH 2 H 2-S(=0) 2Me,b-F 0 A-4527 H H H H 0 NH 2 H 2-S(=0) 2Me,6-F 0 A-4528 H H H H 0 NH 2 H 2-S(=0) 2 Me,b-M e 0 A-4529 H H H H 0 NH 2 H 2-S(=0) 2 Me,6--M e 0 A-4530 H H H H 0 NH 2 H 2-SCF 3 ,b-F 0 A-4531 H H H H H 0 NH 2 H 2-SCF 3 ,6-F 0 A-4532 H H H H NH 2 H 2-SCF 3 ,b-M e 0 A-4533 H H H H 0 NH 2 H 2-SCF 3 ,6-Me 0 A-4534 H H H H H D NH 2 H 2-S (=O)F 3 ,-F 0 A-4535 H H H H 0 NH 2 H 2-S (=O)F 3 ,6-F A-4536 H H H H 0 NH 2 H 2-S(=U)CF 3 ,b-Me 0 A-4537 H H H H 0 NH 2 H 2-S(=U)CF 3,6-Me 0 A-4538 H H H H 0 NH 2 H 2-S(=0) 20F 3 ,b-F 0 A-4539 H H H H 0 NH 2 H 2-S(=0) 20F 3 ,6-F 0 A-4540 H H H H 0 NH 2 H 2-S(=0) 2CF 3 ,b-Me 0 A-4541 H H H H NH 2 H 2-S(=U) 2CF 3 ,6-M e 0 A-4542 H H H H NH 2 H 2-(cyclopropylthlo),b-F 0 A-4543 H H H H 0 NH 2 H 2-(cycobpropylthio),6-F 0 A-4544 H H H H 0 NH 2 H 2-(cyclopropylthio),b-M e 0 A-4545 H H H H 0 NH 2 H 2-(cycbpropylthio),6-M e 0 A-4546 H H H H 0 NH 2 H 2-C(=0)Me,b-F 0 A-4547 H H H H 0 NH 2 H 2-C(=0)Me,6-F 0 A-4548 H H H H 0 NH 2 H 2-C(=U)Me,b-M e 0 A-4549 H H H H 0 NH 2 H 2-C(=0)Me,6-Me A-4550 H H H H H 0 NH 2 H 2-CH 2UNb-H 0 A-4551 H H H H HF NH 2 H 2-CH 2UN,6-F A-4552 H H H H 0 NH 2 H 2-CH 2UH,b-M e 0 A-4553 H H H H 0 NH 2 H 2-CH 2UH,6-M e 0 A-4554 H H H H H 0 NH 2 H 2-GH 20H 3 ,4-F 0 A-4555 H H H H H 0 NH 2 H 2-CH 20H 3 ,b-F 0
[0206]
[Table 81]
com pound R' R2 R R A R R' (R)m p A-4556 H H H H 0 NH 2 H 2-OH 20H 3 ,6-F 0 A-4557 H H H H H 0 NH 2 H 2-OH 20CH 3 ,4-Me 0 A-4558 H H H H 0 NH 2 H 2-OH 20CH 3 ,b-Me 0 A-4559 H H H H i 0 NH 2 H 2-CH 2UCH 3 ,6-M e A-4560 H H H H 0 NH 2 H 2-OC(=U)0H 3 ,b-F A-4561 H H H H 0 NH 2 H 2-OG(=U)GH 3 ,6-F 0 A-4562 H H H H 0 NH 2 H 2-UC(=0)CH 3 ,b-M e 0 A-4563 H H H H 0 NH 2 H 2-0(=0)GH 3 ,6-Me 0 A-4564 H H H H i 0 NH 2 H 2-OS(=0) 2CH 3 ,b 0 A-4565 H H H H Hf D NH 2 H 2-USt=U) 20H 3,6-F A-4566 H H H H i 0 NH 2 H 2-UOS=U) 2CH 3,b-M e 0 A-4567 H H H H 0 NH 2 H 2-OSt=U) 2CH 3,6-Me 0 A-4568 H H H H f0 NH 2 H 2-CH 2SCH 3 ,b-H 0
A-4569 H H H H 0 NH 2 H 2-OH 2 SCH 3 ,6-F 0 A-4570 H H H H 0 NH 2 H 2-OH 2SCH 3,b-Me 0 A-4571 H H HH ii f NH2 H Z-GH2SCH3,6-e A-4572 H H H H NH 2 H -NMe 2 ,b-H A-4573 H H H H 0 NH 2 H 2-NMe 2 ,6-F 0 A-4574 H H H H iff NH2 H 2-NMe2,b-M e 0 A-4575 H H H H 0 NH 2 H 2-NMe 2 ,6-M e 0 A-4576 H H H H H 0 NH 2 H 2-N,4-F 0 A-4577 H H H H H 0 NH 2 H 2-ONb-F 0 A-4578 H H H H 0 NH 2 H 2-N,6-F 0 A-4579 H H H H 0 NH 2 H 2-ON,6-Me 0 A-4580 H H H H 0 NH 2 H 2-ON,b-OMe 0 A-4581 H H H H NH 2 H 2-ON,6-OMe 0 A-4582 H H H H NH 2 H 3-ON,6-M e 0 A-4583 H H H H i 0 NH 2 H 3-ON,6-OMe 0 A-4584 H H H H 0 NH 2 H 4-ON,2-M e 0 A-4585 H H H H 0 NH 2 H 4-ON,2-OMe 0 A-4586 H H H H 0 NH 2 H 2-N0 2 ,4-F 0 A-4587 H H H H 0 NH 2 H 2-N0 2,b-F 0 A-4588 H H H H H 0 NH 2 H 2-N0 2 ,64 0 A-4589 H H H H 0 NH 2 H 2-NU 2,4-MAe 0 A-4590 H H H H 0 NH 2 H 2-N0 2,b-M e 0 A-4591 H H H H 0 NH 2 H Z-NU 2,6-e A-4592 H H H H F NH 2 H 2-M e,4,b-F 2 0 A-4593 H H H H 0 NH 2 H 2-M e,6-Et F A-4594 H H H H 0 NH 2 H 2-cyclopropyl,6-OMe 0 A-4595 H H H H H 0 NH 2 H 2-M e,b-Et 0 A-4596 H H H H 0 NH 2 H 2,6-Et2 0 A-4597 H H H H 0 NH 2 H 2-Et,6-F 0 A-4598 H H H H 0 NH 2 H 2-GH 20H 3 ,6-CI F A-4599 H H H H 0 NH 2 H 2-GH 20H 20H 3 ,6-CI 1 A-4600 H H HH ii D NH2 H 2-C2HNMe2 0 A-4601 H H H H H0f G(=U)GH 3 H H 0 A-460 2 H H H H 0 C(=0)H 3 H 2 A-4603 H H H H f DII C(=U)H 3 H 2-G1 0 A-4604 H H H H ifDf C(=0)H3 H 2-Br 0 A-4605 H H H H Hf )C(=U)GH 3 H 2-OH 0 A-4606 H H H H C D-(=0)C3H H 2-Me 0 A-4607 H H H H Ff0 G(=O)H 3 H 2-Et 0 A-4608 H H H H I F G0=)GH 3 H 2-Pr 0 A-4609 H H H H T f DC(=U)H 3 H 2-OF 3 0
A-4610 H H H H H0f )C(=U)H 3 H 2-GHF 2 0 A-4611 H H H H H 0 C(=U)GH 3 H 2-CH 2F 0
A-4612 H H H H H U G(=U)GH 3 H 2-GF 201 0
[0207]
[Table 82]
com pound R' R2 R R A R R' (R)m p A-4613 H H H H 0 C(=0)CH 3 H 2-cycbpropyl 0 A-4614 H H H H F 0 (=U)H 3 H 2-cycobbutyl 0 A-4615 H H H H if0 D (=U)CH3 H 2-cycbpentyl 0 A-4616 H H H H f G(=0)GH 3 H 2-ethenyl1 A-4617 H H H H D 0 C(=U)CH3 H 2-allyl 1 A-4618 H H H H f C(=U)0H 3 H 2-(prop-1-en-1-yD 0 A-4619 H C(H=U)CH 3H HH 2-(triDfC fboroethenyD 0 A-4620 H H H H Df C(=U)0H 3 H 2-0Me 0 A-4621 H H H H i 0 C0(=U)H 3 H 2-OEt A-4622 H H H H iF 0 G(=U)GH 3 H 2-OPr 0 A-4623 H H H H i 0 C(=0)GH 3 H 2-0(/-Pr) 0 A-4624 H H H H HCf D (=U)GH 3 H 2-0G3 A-4625 H H H H Hf G(=U)GH 3 H 2-CHF 2 A-4626 H H H H Df C(=U)0H 3 H 2-(cycbpropybxy) 0 A-4627 H H H H Hf DC(=U)0H 3 H 2-(cycobbutyloxy) 0 A-4628 H H H H 0 G(=U)H 3 H 2-(cycbpentybxy) 0 A-4629 H H H H H 0 G(=0)GH 3 H 2-((2,2-dichbrocycbpropy)oxy) 0 A-4630 H H H H H D c(=U)0H 3 H 2-(oxiran-2-yID 0 A-4631 H H H H f0 G(=U)H 3 H 2-SMe 0 A-4632 H H H H DIf H(=U)30H H 3-SMe 0 A-4633 H H H H H 0 C(=U)CH 3 H 2-S(=U)Me 0 A-4634 H H H H H 0 C(=U)CH 3 H 3-S (=)Me 0 A-4635 H H H H f D C(=U)0H 3 H 2-S(=U) 2Me 0 A-4636 H H H H H 0 C(=U)0H 3 H 3-S(=U) 2Me 0 A-4637 H H H H Hf G(=U)GH 3 H 2-SG3 0 A-4638 H H H H (=U)GH 3 H 3-SG 3 A-4639 H H H H f0 G(=U)H 3 H 3-S(=0)G H3 A-4640 H H H H i 0 C0(=U)CH 3 H 3-SCF(GH3 2 0 A-4641 H H H H D C(=U)CH 3 H 2-(cycbpropylthio) 0 A-4642 H H H H D0f C(=U)0H 3 H 2-(cycbpropylsufinyD 0 A-4643 H H H H D C(=U)CH 3 H 2-(cycbpropylsufonyD 0 A-4644 H H H H D0f C(=U)0H 3 H 2-C(=0)Me 0 A-4645 H H H H Hf )C(=U)0H3 H 2-GH 2 0(=U)CH 3 0 A-4646 H H H H Hf )C(=U)GH3 H 2-GH 2 0(=U)GF 3 0 A-4647 H H H H Hf DC(=U)0H 3 H 2-CH 2 UH 0 A-4648 H H H H H C (=UGH3 H 2-GH 20H 3 0
A-4649 H H H H H0f G(=0)GH 3 H 2-GH 20H 2CH 3 0
A-4650 H H H H D0f C(=O)0H 3 H 2-CH 2SCH 3 0 A-4651 H H H H 0 C(=O)0H 3 H 2-CH 2S(=U)CH 3 0
A-4652 H H H H D C(=U)0H 3 H 2-CH 2S(=U) 2 CH 3 0
A-4653 H H H H 0 C(=O)0H 3 H 2-(benzybxy) 0 A-4654 H H H H 0 C (=O)0H 3 H 2-NH 2 A-4655 H H H H f C (=U)G3H H 2-NHMe 0 A-4656 H H H H -- 7(=0)GH 3 H 2-N (Me) 2 0 A-4657 H H H H f D (=0)GH 3 H 2-(1,3-dioxolan-2-yD 0 A-4658 H H H H f0 G(=U)H 3 H 2-(1,3-dloxan-2-yD 0 A-4659 H H H H iff C(=U)0H 3 H 2-(1#-m idazol-2-yD 0 A-4660 H H H H D if 0 O(=U)H3 H 2-(thiazol-2-y) 0 A-4661 H H H H 0 C(=O)0H 3 H 2-(oxazo-2-yD 0 A-4662 H H H H Hi0 C(=U)GH 3 H 2-CH=NUH 0 A-4663 H H H HfF D (=U)0H 3 H 2-CH=NOMe 0 A-4664 H H H H C (=U)GH 3 H 2-(4,b-dihydro-3-soxazoyD 0 A-4665 H H H H i C(=U)G3HH 2-N 0 A-4666 H H H HF i C(=O)0H 3 H 2-NO 2 0
A-4667 H H H H Hi0 C(=O)0H 3 H 2-F,6-CI 0 A-4668 H H H H H 0 G(=0)GH 3 H 2-F,6-M e 0 A-4669 H H H H H U G(=U)GH 3 H 3-F,6-M e 0
[0208]
[Table 83]
com pound ' R2 RR R A R R' (R)m P A-4670 H H H H D 0 (0)CH3 H 4-F,2-Me 0 A-4671 H H H H 0 )(=U)0H 3 H 2-F,6-UMe 0 A-4672 H H H H C (0)CH 3 H 3-F,6-0Me 0 A-4673 H H H H i 0 C(=U)H 3 H 2,6-C A-4674 H H H H D C(=U)CH 3 H 2-GI,6-M e 0 A-4675 H H H H f C(=U)CH 3 H 3-GI,6-M e 0 A-4676 H H H H ifC 0(=U)CH 3 H 4-GI,2-M e 0 A-4677 H H H H Df C(=U)CH 3 H 2-CIb-CF 3 A-467 8 H H H H 0 C0(=U)CH 3 H 2-C,6-CF 3 A-4679 H H H H iF 0 G(=U)GH 3 H 2-C,6-0Me 0 A-4680 H H H H i 0 C(=U)GH 3 H 3-C,6-UMe 0 A-4681 H H H H f 0 G(=U)GH 3 H 4-C,2-0Me 0 A-4682 H H H H G(=U)GH 3 H 2,4-M e 2 0 A-4683 H H H H f C(=U)CH 3 H 2,b-M e 2 0 A-4684 H H H H f C C(=U)CH 3 H 2,6-M e 2 0 A-468b H H H H (=U)GH3 H 2-M e,4-GH 3 0 A-4686 H H H H H 0 G(=U)GH3 H 2-M e,b-GH 3 0 A-4687 H H H H f C(=U)CH 3 H 2-Me,6-CF 3 0 A-4688 H H H H f0 G(=U)H 3 H 2-M e,4-UMe 0 A-4689 H H H H iff C(=O)CH3 H 2-M e,b-0Me 0 A-4690 H H H H H 0 C(=U)CH 3 H 2-M e,6-UMe 0 A-4691 H H H H f H(=U)3CH H 3-M e,6-UMe 0 A-4692 H H H H f C(=U)CH 3 H 4-M e,2-0Me A-4693 H H H H f H(=U)3CH H 2,b-UMe 2 0 A-4694 H H H H f G(=U)GH 3 H 2,6-UMe 2 0
A-469b H H H H f )(=U)GH3 H 2-UMe,6-GH3 0 A-4696 H H H H f 0(=U)GH3 H -GHH 2 ,b-H A-4697 H H H H i 0 C0(=U)CH 3 H 2-CHF 2,6-F 0 A-4698 H H H H C0(=U)CH3 H 2-CHF2,b-Me 0 A-4699 H H H H iff C(=U)CH3 H 2-CHF2,6-Me 0 A-4700 H H H H D- (=U)CH 3 H 2-cycbpropyLb-F 0 A-4701 H H H H iff C(=U)CH 3 H 2-cycbpropyL,6- 0 A-4702 H H H H iF 0 C(=U)CH 3 H 2-cyclopropyLb-Me 0 A-4703 H H H H 0 0G(=U)GH3 H 2-cyclopropyL,6-Me 0 A-4704 H H H H C D C(=U)CH3 H 2-ethenyL,6-F 0 A-470b H H H H C 0 (=U)GH3 H 2-ethenyl,6-M e 0 A-4706 H H H H H 0 G(=U)GH 3 H 2-UEt,b-F A-4707 H H H H D0f C(=O)CH 3 H 2-OEt,6-F 0 A-4708 H H H H D0f C(=U)CH 3 H 2-OEt,b-CI 0 A-4709 H H H H C0(=0CH3 H 2-OEt,6-CI 0 A-4710 H H H H iff C(=U)CH3 H 2-OEt,b-Me 0 A-4/11 H H H H f D C(=U)CH 3 H 2-OEt,6-M e 0 A-4712 H H H H Hf 0 G(=U)G3 H 2-UGH2,b-F A-4713 H H H H Hf 0(=U)GH3 H 2-UGHF 2,6-F 0 A-4714 H H H H C (=U)GH3 H 2-0GH2,-Ae 0 A-471b H H H H G(=U)GH 3 H 2-0GH 2,6-MAe A-4716 H H H H Df C(=U)CH 3 H 2-(cycbpropyloxy),b-F 0 A-4/1/ H H H H f C(=U)CH 3 H 2-(cycbpropyloxy),6-F 0 A-4/18 H H H H Df C(=O)CH 3 H 2-(cyclopropyoxy),b-Me 0 A-4719 H H H H iff 0(=0)GH3 H 2-(cyclopropyloxy),6-M e 0 A-4720 H H H H C D C(=U)CH3 H 2-SMe,b-F 0 A-4721 H H H H 0 G(=U)GH 3 H 2-SMe,6-F 0 A-4722 H H HHiff )(=U)GH 3 H 2-SMe,b-Me 0 A-4723 H H H H C D- (=U)CH3 H 2-SMe,6-Me 0 A-4724 H H H H CD(=U)CH3 H 2-S(=U)Me,b-F 0 A-4/25 H H H H f )C(=U)GH 3 H 2-S(=U)Me,6-F 0 A-4/26 H H H H f C (=U)CH 3 H 2-S(=U)Me,b-Me 0
[0209]
[Table 84]
com pound R' R2 R R A R R' (R)m p A-4727 H H H H 0 0U)CH 3 H 2-S (= )Me,6- e 0 A-4728 H H H H F )(=U)H 3 H 2-S(= ) 2 Me,b-F 0 A-4729 H H HHif0 )(=U)H 3 H 2-S(= )2Me,6-F W A-4730 H H H H if 0 C =0 )H H 2-S = ) 2 Me,b-M e A-4731 H H H H 0 C (= )CH 3 H 2-S (= )M e,6 -Me 0 A-4732 H H H H D0f )C(=U)H 3 H 2-SC3,b-F 0 A-4733 H H H H D C 0 (=U)CH3 H 2-SCF3,6-F 0 A-4734 H H HHiff 0 C(=U)H3 H 2-SCF 3,b-M e 0 A-4735 H H H H f 0 0(=U)CH 3 H 2-SCF 3 ,6-i e 0 A-4736 H H H H D GF f 0)GH3 H 2-S =0 )Cb-F 0 A-4737 H H H H i 0 C= 0)GH3 H 2-S =0 )F 3 ,6-F 0 A-4738 H H H H D C =0 )GH3 H 2-S =0 )CF 3,b- e 0 A-4739 H H H H C =0 )GH3 H 2-S =0 )CF 3 ,6- e 0 A-4740 H H H H f D C0I (=U)H 3 H 2-S (= ) 2 F 3 ,b-F 0 A-4741 H H H H D0f 0 C(=U)H 3 H 2-S (= ) 2 F 3 ,6-F 0 A-4742 H H H H 0 )G3 H 2-S =0 2 C 3,b-M e 0
A-4743 H H H H 0G= U)GH3 H 2-S =0 2F3,6-M e 0 A-4744 H H H H D E c(=U)0H 3 H 2-(cycbpropy thb),b-F 0 A-4745 H H H H f0 G=0)H 3 H 2-(cycbpropylth b),6-F 0 A-4746 H H H H 0 C =O)0H 3 H 2-(cycbpropy thio),b-M e 0 A-4/4/ H H H H f )(=U)H 3 H 2-(cycbpropy thio),6-M e 0 A-4748 H H H H 0 G (=C )CH 3 H 2- 0(= )M e,b-F 0 A-4749 H H H H iff 0(= )H3 H 2- 0(= )M e,6-F 0 A-4750 H H H H ifU CO)CH3 H 2-(= O)Me,b-M e 0 A-4751 H H H H i 0 0= )GH 3 H 2-(= U)M e,6-M e 0 A-4752 H H H H I G7= 0)GH 3 H 2-CH 2UH,b-H 0 A-4753 H H H H f0 G(=U)GH 3 H 2-CH 20H,6-F A-4754 H H H H i 0 C= U)0H 3 H 2-CH 2UH,b5-M e 0 A-4755 H H H H 0 C = U)0H 3 H 2-CH 2UH,6 -Me 0 A-4756 H H H H D0f )C(=U)H 3 H 2-GH 20H 3 ,4-F 0 A-4757 H H H H 0 C = )CH 3 H 2-GH 20H 3 ,b- 0 A-4758 H H H H D0f )C(=U)H 3 H 2-GH 20H 3,6-F 0 A-4759 H H H H 0 G(=U)CH3 H 2-0H 2OCH3,4-i e 0 A-4760 H H H H 0G(=0)CH3 H 2-CH20H3,b5-Me 0 A-4761 H H H H D G(=U)CH3 H E0 2 -H2CH3,6-MAe 0 A-4762 H H H H DiC 0=U)GH3 H 2)-0G = U)0H 3 ,b- 0
A-4763 H H H H 0fGf= U=)GH 3 H 2)-0G = U)0H 3 ,6-F 0 A-4764 H H H H ifDf )(=U)H 3 H 2-C(=U)CH 3,b-M e F A-4765 H H H H f D0I 0(=U)H 3 H 2-0(=U)CH 3,6-M e 0 A-4766 H H H H DIf )C(=U)H 3 H 2-US (= )2 H 3 ,b- 0 A-4767 H H H H D0f )C(=U)H 3 H 2-US (= )2 H 3 ,6-F 0 A-4768 H H H H f 0)(=O)0H 3 H 2-OS(= ) 2 GH 3,b-M e 0 A-4769 H H H H 0GC= 0)GH3 H 2-US =0 )2H3,6-M e 0 A-4770 H H H H H C= 0)GH 3 G H 2-GH 2S0H 3 ,b-H 0
A-4771 H H H H D GC= U)GH 3 H 2-GH 2S0H 3,6-F 0 A-4772 H H H H = )GH 3 H 2-CH 2S0H 3,b-M e 0 A-4773 H H H H 0 0= O)0H 3 H 2-0H 2S0H 3,6-M e 0 A-4774 H H (=U)0H3H HH 2-NMeDIC 2,b-F 0 A-4775 H H H H 0 0 (= )H3 H 2-NMe2,6-F 0 A-4776 H H H H 0G(=U)0H3 H 2AMe2,biAe 0 A-4777 H H H H iff 0 C(=U)0H3 H 2-NMe2,6-i e 0 A-4778 H H H H HDi =0 )GH 3 H 2-GN,4-F 0 A-4779 H H H H f0 =0 )GH 3 H 2-GN,b-F 0 A-4780 H H H H D0f 0(= )0H 3 H 2-ON,6-F 0 A-4781 H H H H H 0 (=U)CH 3 H 2-CN,6-Me 0 A-4782 H H H H 0 G t=0U)GH3 H 2-GNS5-OM e 0 A-4/83 H H H FH 0 G (= U)GH 3 H 2-GN,6-OMe 0
[0210]
[Table 85]
com pound ' R2 RR R A R R' (R)m P A-4784 H H H H i0 C0(=U)H 3 H 3-CN,6-M e 0 A-4785 H H H H F 0 (=U)H3 H 3-CN,6-UMe 0 A-4786 H H H H iff D (=0)CH 3 H 4-CN,2-M e 0 A-4787 H H H H iff G(=0)GH H 4-CN,2-UMe 0 A-4788 H H H H DfC 0(=U)CH 3 H 2-N0 2,4-F A-4789 H H H H Df C(=U)CH 3 H 2-N0 2 ,b-F 0 A-4790 H H H H DfC 0(=U)CH 3 H 2-N0 2 ,64 0 A-4791 H H H H 0 (=U)CH3 H 2-N02,4-MAe 0 A-4792 H H H H 0 C0(=U)CH 3 H 2-N0 2,b-Me 0 A-4793 H H H H iF 0 G(=U)GH3 H 2-N0 2,6-MAe 0 A-4794 H H H H H i 0 (=0)GH3 H 2-M e,4,b- 2 0
A-4795 H H H H i 0 G(=U)H3 H 2-M e,6-Et 0 A-4796 H H H H 0 G(=0)GH3 H 2-cyclopropyl,6-OMe 0 A-4797 H H H H H (=U)CH3 H 2-M e,b-Et 0 A-4798 H H H H Hf C C(=U)CH 3 H 2,6-Et2 0 A-4799 H H H H f0 O(=U)GH 3 H 2-Et,6-F 0 A-4800 H H H H Hf G(=U)GH 3 H 2-GH 20H 3,6-CI 0 A-4801 H H H H Hf D C(=0)CH 3 H 2-CH 20H 2CH 3,6-CI 0 A-4802 H H H H f 0(=U)GH3 H 2-CH 2 NMe 2 0
A-4803 H H H H D0f C(=0)CH 20H 3 H H 0 A-4804 H H H H H 0 C(=0)CH 20H 3 H 2-F 0 A-4805 H H H H Hf C(=U)CH 20H 3 H 2-Cl 0 A-4806 H H H H H C 0(=U)CH 20H 3 H 2-Br 0 A-4807 H H H H H Cf C(=U)CH 20H 3 H 2-OH 0 A-4808 H H H H if 0 G(=U)0H 2 0H 3 H 2-M e 0 A-4809 H H H H F0 G(=U)GH 20H 3 H 2-Et 0 A-4810 H H H H f0 G(=U)H 20H 3 H 2-Pr 0 A-4811 H H H H 0 C(=0)CH 200H 3 H 2-CF 3 0 A-4812 H H H H D0f C(=U)CH 200H 3 H 2-UHF 2 0
A-4813 H H H H C0(=0)CH200H3 H 2-CH2F 0
A-4814 H H H H D0f C(=U)CH 20H 3 H 2-CF 2CI 0 A-4815 H H H H iff C(=0)CH 200H3 H 2-cycbpropyl 0 A-4816 H H H H iF 0C(=U)CH 20H 3 H 2-cycobbutyl 0 A-4817 H H H H iif G(=U)GH 20H 3 H 2-cycobpentyl 0 A-4818 H H H H CD -(=0)CH20H 3 H 2-ethenyl A-4819 H H H H H D G(=0)GH 20H 3 H 2-allyl A-4820 H H H H OD G(=U)GH20H3 H 2-(prop-1-en-1-yD A-4821 H H H H D C(=0)CH 20H 3 H 2-(trifboroethenyD 0 A-4822 H H H H iff C(=0)CH200H 3 H 2-0Me A-4823 H H H H D 0C0(=U)CH20CH 3 H 2-OEt 0 A-4824 H H HHiff C(=0)CH200H3 H 2-OPr 0 A-4825 H H H H f DH(=U)CH 20H 3 H 2-0 (/-Pr) 0 A-4826 H H H H i0 G(=U)GH 20H 3 H 2-0G3 A-4827 H H H H f 0(=U)GH 2UGH 3 H 2-0HH 2 0
A-4828 H H H H H D (=0)GH 20H 3 H 2-(cycbpropybxy) 0 A-4829 H H H H G(=U)GH 2 UGH 3 H 2-(cycobbutyloxy) 0 A-4830 H H H H D C(=U)CH 200H 3 H 2-(cycbpentybxy) 0 A-4831 H H H H D C(=U)CH 200H3 H 2-((2,2-dichbrocycobpropy)oxy) 0 A-4832 H H H H D C(=U)CH 200H 3 H 2-(oxiran-2-y) 0 A-4833 H H H H f0 0G(=U)H20H3 H 2-SMe 0 A-4834 H H H H H D C(=U)CH 200H 3 H 3-SMe 0 A-4835 H H H H 0 G=)GH 20H 3 H 2-S(=0)Me 0 A-4836 H H H H 0 G=)GH 2UGH 3 H 3-S (=0)Me 0 A-4837 H H H H 0 C(0)CH 20H 3 H 2-S(=0) 2Me 0 A-4838 H H H H f C (=0)CH 20H 3 H 3-S(=0) 2Me 0 A-4839 H H H H H0f 0(=U)GH 2UGH 3 H 2-SGF 3 0 A-4840 H H H H7- i C(=U)GH2UGH3 H 3-SCF3 0
[0211]
[Table 86]
com pound R' R2 R R A R R' (R)m p A-4841 i H H H H 0 C(= C)H20H 3 H 3-S (= 0)C 3 A-4842 H H H H HFf )0H H(= 20H 3 H 3-SCF (CF3) 2 0 A-4843 H H H H D C(= U)0H 20H 3 H 2-(cycobpropy thb) 0 A-4844 H H H H CO U)0H 20H 3 H 2-(cycbpropylsu finy D A-4845 H H H H D if 0 ( )H 20H3 H 2-(cycobpropy u fony D 0 A-4846 H H H H iff H(= )0H 20H 3 H 2-C (= 0)M e 0 A-4847 H H H H Df C = U)0H 20H 3 H 2-GH 2 C 0 )H 3 A-4848 H H H H 0 C = U)0H 20H 3 H 2-0H 2C 0 ) 3 0 A-484 Hf9 H H H 0 C0(= U)0H 20H 3 H 2-0H 20H 0 A-4850 H H H H D G (=O) H 2 UH 3 H 2-GH 2 UGH 3 A-4851 H H H H i 0 C(=O)GH 20H 3 H 2-GH 20H 2CH 3 0
A-4852 H H H H D C (=O)GH 2 UGH 3 H Z-H2 SH 3 A-4853 H H H H H C (=O)GH 20H 3 H Z-GH 2 (= U)GH 3 A-4854 H H H H D C(= U)CH 20H 3 H 2-CH 2S(= 0) 2 CH3 A-4855 H H H H 0 C = )0H 20H 3 H 2-(benzy bxy) 0 A-4856 H H H H G(=U)H 20H 3 H 2-NH 2 A-4857 H H H H f0 G(=U)GH 2UGH 3 H 2-NH M e A-4858 H H H H D C(= U)0H 200H 3 H 2-N (M e)2 A-4859 H H H H f0 G(=U)GH 20H 3 H 2-(1,3-d bxo an-2-y D A-4860 H H H H f C(= U)0H 200H 3 H 2-(1,3-d bxan-2-y D 0 A-4861 H H H H 0 C(= 0)0H 20H 3 H 2-(/H- idazoE2-yD 0 A-4862 H H H H i i f =U)0H 20CH3 H 2-(thiazo -2-yl) 0 A-4863 H H H H D C(=U)0H 200H 3 H 2-(oxazol-2-y D A-4864 H H H H H C H (=U)0H 20H3 H 2-CH= N0H 0 A-4865 H H H H iff G(=U)GH20H 3 H 2-CH= NUMe 0 A-4866 H H H H H )GH 20H3 H 2-(4,b-dihydro-3-soxazoD 0 A-4867 H H H H H0 G(=U)CH 20H 3 H 2-N 0 A-4868 H H H H i 0 C= U)0H 200H 3 H 2-NO 2 0 A-4869 H H H H 0 C=U)0H 200H 3 H 2-F,6-CI 0 A-4870 H H HHiff H(= )0H20H3 H 2-F,6-M e 0 A-4871 H H H H 0 (= O)0H 200H 3 H 3-F,6-M e 0 A-4872 H H H H 0 (= O)CH 200H 3 H 4-F,2-i e 0 A-4873 H H H H Hif 0 (=C)H 20CH 3 H 2-F,6-M e 0 A-4874 H H H HF G(=U)CH 20H 3 H 3-F,6-UM e A-4875 H H H H DfF0 C(=U)H 20CH 3 H 2,6-C 0 A-4876 H H H H f C(= U)CH 20H 3 H 2-C 1,6- e 0 A-4877 H H H H 0 G(= U)CH 2 0H 3 H 3-C 1,6- e 0 A-4878 H H H H C0(= U)CH20H3H 4-C 1,2- e F A-4879 H H H H C0 (=U)CH 20H 3 H 2-C ,b-CF 3 A-4880 H H H H Df C(= O)CH 200H 3 H 2-C I,6-CF 3 0 A-4881 H H H H 0 C(= O)CH 200H 3 H 2-C 1,6-0M e 0 A-4882 H H H H D i CO)CH200H3 H 3-C ,6-0M e 0 A-4883 H H H H 0 CG(=O)CH 20H 3 H 4-C 1,2-UM e 0 A-4884 H H H H 0 C(= O)CH 20H 3 H 2,4-M e 2 0 A-4885 H H H H ifW CG(=U)GH2UGH3 H 2,b- e2 0
A-4886 H H H H (=U)CH 20H 3 H 2,6-M e 2 0
A-4887 H H H H 0 C(= U)CH 200H 3 H 2-M e,4-CF 3 0 A-4888 H H H H f C(= U)CH 20CH 3 H 2-M e,b-CF 3 0 A-4889 H H H H 0 C(= O)CH 200H 3 H 2-M e,6-CF 3 0 A-4890 H H H HF G(=U)CH 20H 3 H 2-M e,4-0M e A-4891 H H H H C 0 C= U)CH2UGH3 H 2-M e,b-OM e A-4892 H H H H H G(= U)GH 2 UCH 3 H 2-M e,6-OM e 0 A-4893 H H H H C (=i )GH 2 OCH 3 H 3-M e,6-OM e 0 A-4894 H H H H 0 C =U)CH 200H 3 H 4-M e,2-OM e A-4895 H H H H f0 C(=O)CH 200H 3 H 2,5-0M e 2 0 A-4896 H H H H G(= )H 2 UGH 3 H Z,6-)Me 2 F A-489/ H H H fH 0 (=U)GH 2UGH 3 H 2-OMe,6-CF 3 0
[0212]
[Table 87]
com pound ' R2 RR R A R R' (R)m P A-4898 H H H H 0 C(=U)0H 200H 3 H 2-CHF 2,b-F 0 A-4899 H H H H H Ci)f (=U)H 20H 3 H 2-CHF 2,6-F 0 A-4900 H H H H 0DH(=U)CH 20H 3 H 2-CHF 2,b-Me 0 A-4901 H H H H i 0 C(=U)CH 20H 3 H 2-CHF 2,6-M e 0 A-4902 H H H H D C(=0)CH 20H 3 H 2-cycbpropylb- 0 A-4903 H H H H iff C(=0)CH200H3 H 2-cycbpropyl,64 0 A-4904 H H H H C G(=0)CH 20H 3 H 2-cyclopropylb-Me 0 A-4905 H H H H f Di C(=U)CH 200H 3 H 2-cyclopropyl,6-Me 0 A-4906 H H H H i 0 C(=U)CH 200H 3 H 2-ethenyl,6-F 0 A-4907 H H H H i 0 G(=O)CH 2 UGH 3 H 2-ethenyl,6-Me 0 A-4908 H H H H i 0 C(=O)CH 20H 3 H 2-Ut-t,bF A-4909 H H H H i 0 G(=O)CH 2 UGH 3 H 2-OEt,6-F 0 A-4910 H H H H 0 C(=O)CH 20H 3 H 2-UEt,b-CI F A-4911 H H H H 0 C(=U)CH 200H 3 H 2-OEt,6-CI 0 A-4912 H H H H f C C(=U)CH 200H 3 H 2-OEt,b-Me 0 A-4913 H H H H 0 G(=U)CH 20H 3 H 2-UEt,6-M e 0 A-4914 H H H H H 0 C(=U)GH 2UGH 3 H 2-CH2b-H 0 A-4915 H H H H H0f C(=U)CH 200H 3 H 2-CH' 2,6-F 0 A-4916 H H H H 0 G(=U)CH 20H 3 H 2-CHH 2 ,b-M e 0 A-4917 H H H H if0 (=U)CH200H3 H 2-CHF2,6-Me 0 A-4918 H H H H f C H(=U)C2H0H 3 H 2-(cycbpropyloxy),b-F 0 A-4919 H H H H H 0 C(=0)CH 20H 3 H 2-(cycobpropyloxy),6-F 0 A-4920 H H H H CDC(=0)CH 20H3 H 2-(cyclopropybxy),b-Me 0 A-4921 H H H H iff C(=U)CH 200H3 H 2-(cyclopropybxy),6-M e 0 A-4922 H H H H f0 C G(=U)H 2UGH3 H 2-SMe,b-F 0 A-4923 H H H H 0 C G(=U)CH20H 3 H 2-SMe,6-F 0 A-4924 H H H H f0 G(=U)H 2UGH 3 H 2-SMe,b-Me 0 A-4925 H H H H 0 C(=U)CH 200H 3 H 2-SMe,6-Me 0 A-4926 H H H H 0 C(=U)CH 200H 3 H 2-S(=0)Me,b-F 0 A-4927 H H H H 0 C(=U)CH 200H 3 H 2-S(=0)Me,6-F 0 A-4928 H H H H D CG(=U)CH 200H 3 H 2-S(=0)Me,b-Me 0 A-4929 H H H H 0 C(=0)CH 200H 3 H 2-S(=0)Me,6-Me 0 A-4930 H H H H T C-(=U)CH 20H3 H 2-S(=0) 2Me,b-F 0 A-4931 H H H H H 0 C(=U)CH 20H 3 H 2-S(=U) 2 Me,6-F A-4932 H H H H CDC(=0)CH 20H 3 H 2-S(=0) 2Me,b-Me 0 A-4933 H H H H C DG(=U)CH 20H3 H 2-S(=U) 2Me,6-iMe F A-4934 H H H H C- G(=U)CH20H3 H 2-SC 3,b-H F A-4935 H H H H 0 Di C(=U)CH 20H 3 H 2-SCF 3 ,6-F 0 A-4936 H H H H 0 C(=0)CH 200H 3 H 2-SCF 3 ,b-Me 0 A-4937 H H H H ifI C(=U)CH 20H 3 H 2-SCF 3,6-Me 0 A-4938 H H H H 0 C(=U)CH 200H 3 H 2-S(=U)C3,b-F 0 A-4939 H H H H 0 C DC(=U)CH 200H3 H 2-S(=U)CF 3,6-F 0 A-4940 H H H H H 0 C(=U)GH 2UGH 3 H 2-S=O)CF 3 ,b-Me 0 A-4941 H H H H H 0 C(=U)GH 2UGH 3 H 2-S=O)CF 3 ,6-M e 0 A-4942 H H H H D G(=U)CH 20H 3 H 2-S (=U) 2CF3b-- 0 A-4943 H H H H 0 G(=U)CH 20H 3 H 2-S(=U) 2CF 3,6-- 0 A-4944 H H HHif- (=U)CH 20CH 3 H 2-S(=0) 2CF 3,b-Me 0 A-4945 H H H H 0 C(=U)CH 200H 3 H 2-S(=0) 2CF 3 ,6-M e 0 A-4946 H H H H D C(=U)CH 20H 3 H 2-(cycobpropylthb),b-F 0 A-4947 H H H H iff G(=U)GH 20H 3 H 2-(cycobpropylthlo),6-F 0 A-4948 H H H H C D (=0)CH 20H3 H 2-(cycobpropythio),b-Me 0 A-4949 H H H H H C (=O)CH 2 UGH 3 H 2-(cycobpropylthio),6-M e 0 A-4950 H H H H 0 C (=O)CH 2UCH 3 H 2-C(=0)Me,b-F 0 A-4951 H H H H H D C(=0)CH 20H 3 H 2-C(=0)Me,6-F 0 A-4952 H H H H f C (=0)CH 20H 3 H 2-CG(=)Me,b-Me 0 A-4953 H H H H f0 C =)GH 2UGH 3 H 2-CG(=)Me,6-Me 0 A-4954 H H H H 0 G(=0)GH 2UGH 3 H 2-CH 2 0H,b-F 0
[0213]
[Table 88]
com pound R' R2 R R A R R' (R)m p A-4955 H H H H 0 C(=U)0H 200H 3 H 2-OH 20H,6-F 0 A-4956 H H H H C (=U)0H 200H 3 H 2-CH 2UH,b-iMe 0 A-4957 H H H H D C (=U)0H 200H 3 H 2-0H 20H,6 -Me F A-4958 H H H H i 0 C(=O)GH 20H 3 H 2-GH 20H 3 ,4-F 0 A-4959 H H H H D f0 C(=U)0H 200H3 H 2-OH 20H 3,b-F 0 A-4960 H H H H 0 C(=U)0H 200H 3 H 2-OH 20H 3 ,6-F 0 A-4961 H H H H i Df C(=U)0H 200H 3 H 2-OH 20CH 3 ,4-i e 0 A-4962 H H H H D0 C(=0)CH 200H 3 H 2-OH 20CH 3 ,b5iMe 0 A-4963 H H H H 0 C(=U)CH 200H 3 H 2-OH 20CH 3 ,6-i e 0 A-4964 H H H H D G (=O)GH 2 UGH 3 H 2-OC(=O)GH 3 ,5-F 0 A-4965 H H H H i 0 C(=O)GH 20H 3 H 2-OC(=O)GH 3 ,6-F 0 A-4966 H H H H C(=O)GH 2 UGH 3 H 2- C(= U)CH 3 ,5- e 0 A-4967 H H H H D C(=O)0H 20H 3 H 2-US(=OUCH 3 ,6-Me 0 A-4968 H H H H 0Df C(=U)CH 200H 3 H 2-S (=0 ) 2 CH 3 ,5-4 0 A-4969 H H H H H0 C=0 )CH 20H 3 H 2-0S =0 ) 2 CH 3 ,6-F A-4970 H H H H 0 GO)CH 20H 3 H 2-US =O ) 2 CH 3,b5-Me 0 A-4971 H H H H 0 (=O)H 200H 3 H 2-OS(=H) 2 CH 3 ,6-Me 0 A-4972 H H H H 0 C= U)CH 20H 3 H 2-OH 2SCH 3 5-F 0 A-4973 H H H H 0 (=U)CH 200H 3 H 2-CH 2 SCH 3,16-e 0 A-4974 H H H H f C(= U)CH 200H 3 H 2-OH 2SCH 3,5-M e U A-4975 H H H H 0 C(= 0)CH 20H 3 H 2- H 2 SCH 3,6-Me 0 A-4976 H H H H D C(= )CH 20CH 3 H 2-NM e 2 ,b-F 0 A-4977 H H H H C H(= 20H 3 )CH H 2-NM e2 ,6-F e A-4978 H H H H f G(= )GH 20H 3 H 2-NM e 2 ,b-M e 0 A-4979 H H H H G(=O )GH 20H 3 H 2-NM4e 2 6-Ae 0 A-4980 H H H H G(=O )H 20H 3 H 2-ON 4-F 0 A-4981 H H H H f0 (=O)CH 200H 3 H 2-ON,5-F 0 A-4982 H H H H 0 C(=0)CH 200H 3 H 2-ON,6-F 0 A-4983 H H H H f C(= )CH 200H 3 H 2-ON,6-M e 0 A-4984 H H H H f C(= 0)CH 200H 3 H 2-ON,6-OM e 0 A-4985 H H H H 0 C=0 )CH 20CH 3 H 2-ON,6-OMe 0 A-4986 H H H H 0 C(= 0)CH 200H 3 H 3-ON,6-M e U A-4987 H H H H iF 0 = )CH 20H 3 H 3-N,6-OM e 0 A-4988 H H H HF (=U)CH 20CH 3 H 4-ON,2-M e 0 A-4989 H H H H 0 C(=U)GH 20H 3 H 4-N,2-OMN e A-4990 H H H H H C(= U)CH 20H3 H 2-N0 2,A-F 0 A-4991 H H H H D0 )HC H= 2 0H 3 H 2-NU 2,b - 0 A-4992 HfH ifH if0 C(=0)C H 200CH 3 H 2-N 0 2,64F F A-4993 H H H H C0 (=0)CH 20H 3 H 2-N02,4-vAe 0 A-4994 H H H H 0 C0(= U)CH 20H 3 H 2-N0 2,b-ivMe 0 A-4995 H H H H 0 C(= 0)CH 200H 3 H 2-N0 2,6- Ae 0 A-4996 H H H H CG(= U)CH20H3 H 2-M e,4,b-2 0 A-4997 H H H H f0 C= O)CH 20H 3 H 2-M e,6-Et 0 A-4998 H H H H 0 C(= O)CH 20H 3 H 2-cyclopropyl,6-OM e 0 A-4999 H H H H D Gff UCO)GH 2 UGH 3 H 2-M e,b-Et A-000 H H H H (=U)CH 20H 3 H 2,6-Et 2 0 A-6001 H H H H Df C(= U)CH 200H 3 H 2-Et,6-F 0 A-5002 H H H H 0 C = )CH 20CH 3 H 2-OH 20H 3,6-'l 0 A-5003 H H H H Df C(= 0)CH 20CH 3 H 2-GH 20H 2CH 3 ,6- I 0 A-5004 H H H H C(= U)CH 20H 3 H 2-CH 2 NM e 2 A-6005 H H H H 0 C(=0)cycbpropyl H H 0 A-5006 H H H H f0 C(=0)cycbpropyl H 2-F0 A-b00/ H H H H f0 C(=0)cycbpropyl H 2-G 0I A-6008 H H H H 0 C(=0)cycbpropyl H 2-Br 0 A-b009 H H H H f C(= 0)cycbpropyl H 2-OH 0 A-b010 H H H H 0 C(=U)cycbpropyl H 2-M e 0 A-bUll H H H H f0 C(=0)cycbpropyl H 2-Et 0
[0214]
[Table 89]
com pound RI R2 R R R A R R' (R)m P A-5012 H H H H H 0 C(=0)cycbpropyl H 2-Pr 0 A-5013 H H H H H 0 C(=0)cycbpropyl H 2-CF, 0 A-5014 H H H H H 0 C(=0)cycbpropyl H 2-CHF 2 0 A-5015 H H H H H 0 C(=0)cycbpropyl H 2-CH 2F 0 A-5016 H H H H H 0 C(=0)cycbpropyl H 2-CF 2C1 0 A-501 7 H H H H H 0 C(=0)cycbpropyl H 2-cycbpropyl 0 A-5018 H H H H H 0 C(=0)cycbpropyl H 2-cycobbutyl 0 A-5019 H H H H H 0 C(=0)cycbpropyl H 2-cycbpentyl 0 A-5020 H H H H H 0 C(=0)cycbpropyl H 2-ethenyl 0 A-5021 H H H H H 0 C(=0)cycbpropyl H 2-allyl 0 A-5022 H H H H H 0 C(=0)cycbpropyl H 2-(prop-1-en-1-yD 0 A-5023 H H H H H 0 C(=0)cycbpropyl H 2-(trifLoroethenyD 0 A-5024 H H H H H F0 C(=0)cycbpropyl H 2-0Me 0 A-5025 H H H H H 0 C(=0)cycbpropyl H 2-0Et 0 A-5026 H H H H H 0 C(=0)cycbpropyl H 2-0Pr 0 A-5027 H H H H H 0 C(=0)cycbpropyl H 2-0 (/-Pr) 0 A-5028 H H H H H 0 C(=0)cycbpropyl H 2-OCF0 0 A-5029 H H H H H 0 C(=0)cycbpropyl H 2-0CHF 2 0 A-5030 H H H H H 0 C(=0)cycbpropyl H 2-(cycbpropy bxy) 0 A-5031 H H H H H 0 C(=0)cycbpropyl H 2-(cycbbutybxy) 0 A-5032 H H H H H 0 C(=0)cycbpropyl H 2-(cycbpentybxy) 0 A-5033 H H H H H 0 C(=0)cycbpropyl H 2-((2,2-dichbrocycobpropyl)oxy) 0 A-5034 H H H H H 0 C(=0)cycbpropyl H 2-(oxiran-2-y) 0 A-5035 H H H H H 0 C(=0)cycbpropyl H 2-SMe 0 A-5036 H H H H H 0 C(=0)cycbpropyl H 3-SMe 0 A-5037 H H H H H 0 C(=0)cycbpropyl H 2-S(=0)Me 0 A-5038 H H H H H 0 C(=0)cycbpropyl H 3-S(=0)Me 0 A-5039 IH H H H H 0 C(=0)cycbpropyl H 2-S(=0) 2Me 0 A-5040 H H H H H 0 C(=0)cycbpropyl H 3-S(=0) 2Me 0 A-5041 H H H H H 0 C(=0)cycbpropyl H 2-SCF3 0 A-5042 H H H H H 0 C(=0)cycbpropyl H 3-SCF3 0 A-5043 H H H H H 0 C(=0)cycbpropyl H 3-S(=0)CF 3 0 A-5044 H H H H H 0 C(=0)cycbpropyl H 3-SCF(CF3) 2 0 A-5045 H H H H H 0 C(=0)cycbpropyl H 2-(cycbpropythio) 0 A-5046 H H H H H 0 C(=0)cycbpropyl H 2-(cycbpropysulfinyD 0 A-5047 H H H H H 0 C(=0)cycbpropyl H 2-(cycobpropylsulfonyD 0 A-5048 H H H H H 0 C(=0)cycbpropyl H 2-C(=0)Me 0 A-5049 H H H H H 0 C(=0)cycbpropyl H 2-CH 2C(=0)CH 3 0 A-5050 H H H H H 0 C(=0)cycbpropyl H 2-CH 2C(=0)CF 3 0 A-5051 H H H H H 0 C(=0)cycbpropyl H 2-CH 2 0H 0 A-5052 H H H H H 0 C(=0)cycbpropyl H 2-CH 2 0CH 3 0 A-5053 H H H H H 0 C(=0)cycbpropyl H 2-CH 2 0CH 2CH 3 0 A-5054 H H H H H 0 C(=0)cycbpropyl H 2-CH 2SCH 3 0 A-5055 H H H H H 0 C(=0)cycbpropyl H 2-CH 2S(=0)CH 3 0 A-5056 H H H H H 0 C(=0)cycbpropyl H 2-CH 2S(=0)2CH 3 0 A-5057 H H H H H 0 C(=0)cycbpropyl H 2-(benzybxy) 0 A-5058 H H H H H 0 C(=0)cycbpropyl H 2-NH 2 0 A-5059 H H H H H 0 C (=0)cycbpropyl H 2-NH M e 0 A-5060 H H H H H 0 C(=0)cycbpropyl H 2-N (Me)2 0 A-5061 H H H H H 0 C(=0)cycbpropyl H 2-(1,3-dioxolan-2-yD 0 A-5062 H H H H H 0 C(=0)cycbpropyl H 2-(1,3-dioxan-2-y) 0 A-5063 H H H H H 0 C (=0)cycbpropyl H 2-(l1H-m idazol-2-yD 0 A-5064 H H H H H 0 C(=0)cycbpropyl H 2-(thiazol-2-y) 0 A-5065 H H H H H 0 C(=0)cycbpropyl H 2-(oxazol-2-y) 0 A-5066 H H H H H 0 C(=0)cycbpropyl H 2-CH=N0H 0 A-5067 H H H H H 0 C (=0)cycbpropyl H 2-CH= NOM e 0 A-5068 H H H H H 0 C(=0)cycbpropyl H 2-(4,b-dihydro-3-isoxazolyD 0
[0215]
[Table 90]
com pound RI R2 R R R A R R' (R)m P A-5069 H H H H H 0 C(=O)cycbpropyl H 2-CN 0 A-5070 H H H H H 0 C(=0)cycbpropyl H 2-N0 2 0 A-507 1 H H H H H 0 C(=0)cycobpropyl H 2-F,6-CI 0 A-5072 H H H H H C 0(=0)cycbpropyl H 2-F,6-Me 0 A-5073 H H H H H 0 C(=O)cycbpropyl H 3-F,6-Me 0 A-5074 H H H H H 0 C(=O)cycbpropyl H 4-F,2-M e 0 A-5075 H H H H H 0 C(=O)cycbpropyl H 2-F,6-0Me 0 A-5076 H H H H H 0 C(=O)cycbpropyl H 3-F,6-0Me 0 A-5077 H H H H H 0 C(=O)cycbpropyl H 2,6-Cl2 0 A-5078 H H H H H 0 C(=O)cycbpropyl H 2-CI,6-M e 0 A-5079 H H H H H 0 C(=O)cycbpropyl H 3-CI,6-M e 0 A-5080 H H H H H 0 C(=O)cycbpropyl H 4-CI,2-M e 0 A-5081 H H H H H 0 C(=O)cycbpropyl H 2-CIb-CF, 0 A-5082 H H H H H 0 C0(=)cycbpropyl H 2-C,6-CF, 0 A-5083 H H H H H 0 C(=0)cycbpropyl H 2-C1,6-0Me 0 A-5084 H H H H H 0 C(=0)cycbpropyl H 3-C1,6-0Me 0 A-5085 H H H H H 0 C(=0)cycbpropyl H 4-CI,2-0Me 0 A-5086 H H H H H 0 C(=O)cycbpropyl H 2,4-M e 2 0 A-5087 H H H H H 0 C(=O)cycbpropyl H 2,b-M e 2 0 A-5088 H H H H H 0 C(=O)cycbpropyl H 2,6-M e 2 0 A-5089 H H H H H 0 C(=O)cycbpropyl H 2-Me,4-CF3 0 A-5090 H H H H H 0 C(=0)cycbpropyl H 2-Me,5-CF3 0 A-5091 H H H H H 0 C(=O)cycbpropyl H 2-Me,6-CF3 0 A-5092 H H H H H 0 C(=0)cycbpropyl H 2-MAe,4-0Me 0 A-5093 H H H H H 0 C(=0)cycbpropyl H 2-e,5-0Me 0 A-5094 H H H H H 0 C(=0)cycbpropyl H 2-MAe,6-0Me 0 A-5095 H H H H H 0 C(=0)cycbpropyl H 3-MAe,6-0Me 0 A-5096 H H H H H 0 C(=0)cycbpropyl H 4-Me,2-0Me 0 A-5097 H H H H H 0 C(=0)cycbpropyl H 2,5-0Me 2 0 A-5098 H H H H H 0 C(=0)cycbpropyl H 2,6-0Me 2 0 A-5099 H H H H H 0 C(=0)cycbpropyl H 2-0Me,6-CF3 0 A-5100 H H H H H 0 C(=0)cycbpropyl H 2-CHF 2,5-F 0 A-5101 H H H H H 0 C(=0)cycbpropyl H 2-CHF 2,6-F 0 A-5102 H H H H H 0 C(=0)cycbpropyl H 2-CHF 2,b-Me 0 A-5103 H H H H H 0 C(=0)cycbpropyl H 2-CHF 2,6-Me 0 A-5104 H H H H H 0 C(=0)cycbpropyl H 2-cycbpropyl,5-F 0 A-5105 H H H H H 0 C(=0)cycbpropyl H 2-cycobpropyL,6-F 0 A-5106 H H H H H 0 C(=O)cycbpropyl H 2-cyclopropyL,5-Me 0 A-5107 H H H H H 0 C(=O)cycbpropyl H 2-cyclopropyL,6-Me 0 A-5108 H H H H H 0 C(=O)cycbpropyl H 2-ethenyl,6-F 0 A-5109 H H H H H 0 C(=O)cycbpropyl H 2-ethenyl,6-M e 0 A-5110 H H H H H 0 C(=0)cycbpropyl H 2-0Et,5-F 0 A-5111 H H H H H 0 C(=0)cycbpropyl H 2-0Et,6-F 0 A-5112 H H H H H 0 C(=0)cycbpropyl H 2-0Et,5-CI 0 A-5113 H H H H H 0 C(=0)cycbpropyl H 2-0Et,6-CI 0 A-5114 H H H H H 0 C(=0)cycbpropyl H 2-0Et,5-M e 0 A-5115 H H H H H 0 C(=0)cycbpropyl H 2-0Et,6-M e 0 A-5116 H H H H H 0 C(=0)cycbpropyl H 2-0CHF2,5-F 0 A-5117 H H H H H 0 C(=0)cycbpropyl H 2-0CHF 2,6-F 0 A-5118 H H H H H 0 C(=0)cycbpropyl H 2-0CHF 2 ,b-MAe 0 A-5119 H H H H H 0 C(=0)cycbpropyl H 2-0CHF 2 ,6-MAe 0 A-5120 H H H H H 0 C(=0)cycbpropyl H 2-(cycbpropyloxy),5-F 0 A-5121 H H H H H 0 C(=0)cycbpropyl H 2-(cycbpropyloxy),6-F 0 A-5122 H H H H H 0 C(=O)cycbpropyl H 2-(cyclopropyloxy),5-M e 0 A-5123 H H H H H 0 C(=O)cycbpropyl H 2-(cyclopropyloxy),6-M e 0 A-5124 H H H H H 0 C(=O)cycbpropyl H 2-SMe,5-F 0 A-5125 H H H H H 0 C(=0)cycbpropyl H 2-SMe,6-F 0
[0216]
[Table 91]
com pound R' R2 R R A R R' (R)m p A-bl26 H H H H 0 C(=0)cycbpropyl H 2-SMe,b-Me 0 A-bl2/ H H H H 0 C(=0)cycbpropyl H 2-SMe,6-Me A-bl28 H H H H 0 C(=0)cycbpropyl H 2-S(=0)Me,b-F W A-bl29 H H H H i 0 C(=U)cycbpropyl H 2-S(=0)Me,6-F 0 A-bl30 H H H H 0 C(=0)cycbpropyl H 2-S(=0)Me,b-M e 0 A-bl31 H H H H 0 C(=0)cycbpropyl H 2-S(=0)Me,6-M e 0 A-bl32 H H H H f Di C(=0)cycbpropyl H 2-S(=0) 2Me,b-F 0 A-bl33 H H H H 0 C(=0)cycbpropyl H 2-S(=0) 2Me,6-F 0 A-bl34 H H H H 0 C(=0)cycbpropyl H 2-S(=0) 2 Me,b-Me 0 A-bl3b H H H H 0 C(=0)cycbpropyl H 2-St=U) 2 Me,6-M e F A-bl36 H H H H H C(=U)cycbpropyl H 2-SCF 3,b-F 0 A-bl3/ H H H H 0 C(=0)cycbpropyl H 2-SCF 3,6-F 0 A-bl38 H H H H C(=U)cycbpropyl H 2-SCF 3 ,b-Me 0 A-bl39 H H H H C0 (=0)cycbpropyl H 2-SGF3,6-M e 0 A-bl40 H H H H 0 C(=0)cycbpropyl H 2-S(=U)C3,b-F 0 A-bl41 H H H H 0 C(=U)cycbpropyl H 2-S(=O)GH 3 ,6- 0 A-bl42 H H H H H C(=U)cycbpropyl H 2-S(=O)CF 3 ,b-Me 0 A-bl43 H H H H 0 C(=0)cycbpropyl H 2-S(=0)CF 3 ,6-Me 0 A-bl44 H H H H C0 (=0)cycbpropyl H 2-S(=U)203,b-H 0 A-bl4b H H H H 0 C(=0)cycbpropyl H 2-S(=0) 20F 3 ,6-F 0 A-bl46 H H H H C0 (=0)cycbpropyl H 2-S(=U) 20F3,b-Me 0 A-bl4/ H H H H F C(=U)cycbpropyl H 2-S(=0) 2 CF 3 ,6-Me 0 A-b48 H H H H 0 C(=0)cycbpropyl H 2-(cycobpropylthb),b-F 0 A-bl49 H H H H H C(=U)cycbpropyl H 2-(cycobpropylthlo),6-F 0 A-bb0 H H H H 0 C(=0)cycbpropyl H 2-(cycobpropylthio),b-M e 0 A-bibi H H H H C(=0)cycbpropyl H 2-(cycobpropylthio),6-M e 0 A-bib2 H H H H H C(=0)cycbpropyl H 2-0(=U)Me,b-F 0 A-blb3 H H H H i 0 C(=0)cycbpropyl H 2-0(=U)Me,6-F 0 A-b1b4 H H H H D C(=0)cycbpropyl H 2-G(=0)Me,b-Me 0 A-bibb H H H H 0 C(=0)cycbpropyl H 2-0(=0)Me,6-Me 0 A-b1b6 H H H H D C(=0)cycbpropyl H 2-GH 20H,b-F 0 A-bib] H H H H 0 C(=0)cycbpropyl H 2-GH 20H,6-F 0 A-bib8 H H H H C(=0)cycbpropyl H 2-CH 20H,b-M e 0 A-blb9 H H H H H C(=0)cycbpropyl H 2-CH 2UN,6-M e 0 A-bl60 H H H H D C(=0)cycbpropyl H 2-GH 20H 3 ,4-F 0 A-b61 H H H H 0 C(=0)cycbpropyl H 2-GH 20H 3 ,b- 0
A-bl62 H H H H C(=U)oyobpropyl H 2-GH 20H 3 ,6- 0 A-bl63 H H H H D C(=0)cycbpropyl H 2-GH 200H 3 ,4-M e 0 A-bl64 H H H H 0 C(=0)cycbpropyl H 2-GH 20CH 3,b-M e 0 A-bl6b H H H H H 0 C(=0)cycbpropyl H 2-GH 20H 3 ,6-M e 0 A-bl66 H H H H 0 C(=0)cycbpropyl H 2-UC(=0)CH 3,b-F 0 A-b6/ H H H H 0 C(=0)cycbpropyl H 2-UC(=0)CH 3 ,6-F 0 A-bl68 H H H H C(=)ocycbpropyl H 2-UC(=U)CH 3 ,b-M e 0 A-bl69 H H H H C G(=U)cycbpropyl H 2-UC(=U)GH3,6-M e 0 A-bi 0 H H H H D C(=0)cycbpropyl H 2-USt=U) 20H 3,b-F A-bl1 H H H H f C(=U)cycbpropyl H 2-U S=U) 20H 3,6-- 0 A-b1/2 H H H H 0 C(=0)cycbpropyl H 2-US(=0) 2CH 3,b-M e 0 A-b/3 H H H H 0 C(=0)cycbpropyl H 2-US(=0) 2CH 3,6-M e 0 A-b1/4 H H H H 0 C(=0)cycbpropyl H 2-GH 2 SCH 3 ,b-4 0 A-blb H H H H 0 C(=0)cycbpropyl H 2-CH 2SCH 3 ,6- 0 A-b1/6 H H H H 0 C(=0)cycbpropyl H 2-GH 2SCH 3,b-M e 0 A-bl/ H H H H 0 C(=0)cycbpropyl H 2-CH 2SCH 3,6-M e 0 A-b/8 H H H H 0 C(=0)cycbpropyl H Z-NMe 2 ,b- 0 A-b/9 H H H H 0 C(=0)cycbpropyl H 2-NMe 2 ,6-F 0 A-b80 H H H H 0 C(=U)cycbpropyl H 2-NMe 2 ,b-M e 0 A-b81 H H H H 0 G(=U)cycbpropyl H 2-NMe 2 ,6-MAe 0 A-bi82 H H H H G(=0)Cycbpropyl H 2-ON,4-F 0
[0217]
[Table 92]
com pound R' R2 R R A R R' (R)m p A-5183 H H H H 0 C(=0)cycbpropyl H 2-ONb-F 0 A-5184 H H H H 0 C(=0)cycbpropyl H 2-ON,6-F 0 A-b18b H H H H 0 C(=0)cycbpropyl H 2-ON,6-Me A-5186 H H H H 0 C(= U)cycbpropyl H 2-ON,b-OM e 0 A-bl8 if H H H H 0 (=0)cycbpropyl H 2-ON,6-OM e 0 A-bl88 H H H H 0 C(=0)cycbpropyl H 3-ON,6-M e 0 A-b89 H H H H f Di C(=0)cycbpropyl H 3-ON,6-OM e 0 A-b190 H H H H 0 C(=0)cycbpropyl H 4-ON,2-M e 0 A-b91 H H H H H 0 C(=0)cycbpropyl H 4-GN,2-OM e 0 A-bl92 H H H H 0 C(=0)cycbpropyl H 2A0 2,4-F F A-b93 H H H H H C(= U)cycbpropyl H 2-N0 2 ,54 0 A-bl94 H H H H D C(=0)cycbpropyl H 2N0 2,6-F 0 A-bl95 H H H H C(= U)cycbpropyl H 2AU 2,4-MA e 0 A-bl96 H H H H 0 C(=0)cycbpropyl H 2-0 2,b-Me 0 A-bl9/ H H H H 0 C(=0)cycbpropyl H 2-N0 2,6-M e 0 A-b98 H H H H f C(= )cycbpropyl H 2-M e,4,b-F 2 0 A-bl99 H H H H H C(= )cycbpropyl H 2-M e,6-Et 0 A-b200 H H H H D C(=0)cycbpropyl H 2-cyclopropyl,6-OM e 0 A-b201 H H H H 0 C(=0)cycbpropyl H 2-M e,b-Et 0 A-b202 H H H H 0 C (=0)cycbpropy I H 2,6-Et 2 0 A-b203 H H H H H C(=0)cycbpropyl H 2-Et,6-F 0 A-b204 H H H H H C(= )cycbpropyl H 2-OH 20H 3 ,6-Cl 0 A-20b H H H H 0 C(=0)cycbpropyl H 2-OH 20H 2CH 3 ,6-C 1 0 A-b206 H H H H f C(= )cycbpropyl H 2-OH 2 NM e 2 0 A-b207 H H H H E 0 (=U)UGH 3 H H 0 A-b208 H H H H H0f 7(=U)UGH 3 H 2-F 0 A-b209 H H H H f0 G(=U)UGH 3 H 2-C1 0 A-b210 H H H i 0 C(= 0)0CH 3 H 2-Br 0 A-b211 H H H H Di C(= U)0CH 3 H 2-OH 0 A-b212 H H H H 0 C(= 0)0CH 3 H 2-M e 0 A-b213 H H H H Df C(= U)0CH 3 H 2-Et 0 A-b214 H H H H H 0 C(=U)UCH 3 H 2-Pr 0 A-b21b H H H H 0 C =U)UCH 3 H 2-F 3 0 A-b216 H H H H E0 f G(=U)0GH3 H 2-GHF2 0
A-b21 H H H H f D0i (=U)0CH 3 H 2-GH 2F 0
A-b218 H H H H Df G(=U)CH3 H 2-0F 201 0 A-b219 H H HH iff G(=U)UGH 3 H 2-cycbpropy1 0 A-b220 H H H H f C(= 0)0CH 3 H 2-ycobbutyl 0 A-b221 H H H H 0 C(=U)UCH 3 H 2-cycbpentyl 0 A-b222 H H H H 0 C0(= U)UGH 3 H 2-eth enyl 0 A-b223 H H H H D C(= 0)0CH 3 H 2-alyl 0 A-b224 H H H H D C(= 0)CH 3 H 2-(prop-l-en-1-y D 0 A-b22b H H H H iff G(= )0H 3 H 2-(trifboroethenyD 0 A-b226 H H H H 77 G(= U)0GH 3 H 2-0Me 0 A-b227 H H H HF 0=O)CH3 H 2-0Et A-b228 H H H H iff G(= )0H3 H 2-0Pr 0 A-b229 H H H H D C(= 0)0CH 3 H 2-0(/-Pr) 0 A-b230 H H H H D C(= 0)0CH 3 H 2)-0 C3 A-b23 1 H H H H 0(= )CH 3 H 2-CHF 2 0
A-b232 H H H H f0 C = )0GH 3 H 2-(cycbpropy bxy) 0 A-b233 H H H H f (= U)UCH 3 H 2-(cycobbutloxy) 0 A-b234 H H H H f G(=U)UGH 3 H 2-(cycbpentybxy) 0 A-b23b H H H H G (= U)UH 3 H 2-((2,2-d ch brocycbpropy I)oxy) 0 A-b236 H H H H D C(= 0)0CH 3 H 2-(oxiran-2-y D0 A-b237 H H H H iff C(=U)UGH3H 2-SMe 0 A-b238 H H H H f C(=U)UGH 3 H 3-SMe 0 A-b239 H IH IH H (= U)UGH 3 H 2-S(=U)Me 0
[0218]
[Table 93]
com pound R' R2 R R A R R' (R)m p A-5240 H H H H 0 C( 0)0H 3 H 3-S(= D)Me 0 A-5241 H H H H H C(= U)00H 3 H 2-S(= ) 2 Me 0 A-5242 H H H H 0 (=U)UGH3 H 3-S(= )2Me 0 A-5243 H H H H f 0 C(= U)00H 3 H 2-SG 3 A-5244 H H H H DF0 )UGH C(= 3 H 3-SCF3 A-5245 H H H H D0f )UGH C(= 3 H 3-S(= 0) C3 A-5246 H H H H f Di )UGH C(= 3 H 3-SCF(CF3) 2 A-5247 H H H H if0 C(= )UGH 3 H 2-(cycobpropy thb) 0 A-524 Hf8 H H H 0 C0(=U)0H 3 H 2-(cycbpropylsufinyD 0 A-5249 H H H H D F0 CU)UGH3 H 2-(cycobpropy u fony D 0 A-525 Hf0 H H H f 0 C(= U)00H 3 H 2-C(= U)Me 0 A-5251 H H H H f 0 U)UH 0(= 3 H 2-GH 2 0(= )GH 3 0
A-5252 H H H H H C C (=U)UGH 3 H 2-GH 20(= )0CF 3 A-5253 H H H H D C = 0)UH 3 H 2-0H 20H A-5254 H H H H DI0 )UGH C(= 3 H 2-0H 20H 3 0
A-52 55 i HHHH G(=U)GH3 H Z-H 2GH2H3 0
A-5256 H H H H H GO)UGH 3 H Z-GH 2 H 3 0
A-5257 H H H H D0 C (=0 )GH 3 H 2-CH 2S (=0 )H 3 A-5258 H H H H G(= U)UGH 3 H 2-CH 2S(0 CH 3 0 A-5259 H H H H 0 C(= U)UH 3 H 2-(benzy bxy) 0 A-5260 H H H H Hf C(= U)UGH 3 H 2-NH 2 0 A-5261 H H H H HF C=0 )0GH 3 H 2-NHMe 0 A-5262 H H H H f C(= 0)0GH 3 H 2 MN e)2 0 A-5263 H H H H f C(=U)UGH 3 H 2-0,3-d bxoan-2-yD 0 A-5264 H H H H f 0 G(=U)0GH 3 H 2-0,3-dbxan-2-y D 0 A-5265 H H H H f0 G(=U)UGH 3 H 2-(1H- idazokF2-yD 0 A-5266 H H H H f0 G(=U)UGH 3 H 2-(thiazo b-2-y1 0 A-5267 H H H H i 0 C(= 0)UGH 3 H 2-(oxazo -2-y D 0 A-5268 H H H H D C(= 0)0H 3 H 2-CH= N0H 0 A-5269 H H H H C(= 0)0GH 3 H 2-CH= NOM e 0 A-5270 H H H H 0 0 C 0)UGH3 H 2-(4,b-dihydro-3-oxazo D 0 A-5271 H H H H H 0 C= 0)0GH 3 H 2-GN 0 A-5272 H H H H HFf C(=0)0GH 3 H 2-NO 2 0 A-5273 H H H H H C(= U)0H3 H 2-F,6-1 0 A-5274 H H H H Ef 0 (=U)0GH3 H 2-F,6-i e 0 A-5275 H H H H C(= U)UH3 H 3-F,6-i e 0 A-5276 H H H H iff 3(=U)U H 4-F,2-i e 0 A-5277 H H H H 0 0(=U)UH 3 H 2-F,6-0Me 0 A-5278 H H H H Df 0(= )0GH 3 H 3-F,6-0Me 0 A-5279 H H H H DI C(=0)GH3 H 2,6-C 0 A-5280 H H H H 0 C( =)0 H 3 H 2- 1,6-M e 0 A-5281 H H H H ifi fD (=U)UGH3 H 3-1,6-M e 0 A-5282 H H H H 0 C =0)0 H3 H 4-01,2-M e 0 A-5283 H H H H H C(= 0)0H3 H 2-Clb- 3 0
A-5284 H H H H D007 (=U)U3 H 2-C1,6- 3 0 A-5285 H H H H 0 =7)03 H 2-C 1,6-M e 0 A-5286 H H H H 0 =0 )UGH 3 H 3-C ,6-M e 0 A-528 / H H H H 0 C(=0 )UGH 3 H 4-C 1,2-M e 0 A-5288 H H H H DI0 C(=U)UGH 3 H 2,4-M e 2 0 A-5289 H H H H 0(=U)0H 3 H 2,b-M e 2 0 A-5290 H H H H iff C(=U)00H3 H 2,6-M e2 0 A-5291 H H H H G(= U)U3 H 2-M e,4-GH 3 A-5292 H H H H f0 G(=U)U3 H 2e,b-GH 3 0 A-5293 H H H H f 0 (= O)UH 3 H 2-M e,6-CF 3 0 A-5294 H H H H iff 0(=O)UH3 H 2 -Me,4-UMe 0 A-5295 H H H H 0 0 G(= U)UGH3 H 2- e,b-OMe 0 A-5296 H H H H f0 0 (=O)UGH 3 H 2-M e,6-OMe 0
[0219]
[Table 94]
com pound R' R2 R R A R R' (R)m p A-5297 H H H H 0 C(=U)UGH 3 H 3 -Me,6-OMe 0 A-5298 H H H H F C(=U)OCH 3 H 4-M e,2-UMe 0 A-5299 H H H H D C(=U)OCH 3 H 2,b-UMe 2 0 A-5300 H H H H f 0 C(=O)UGH 3 H 2,6-UMe 2 0 A-5301 H H H H D C(=U)UCH 3 H 2-0Me,6-CF 3 0 A-5302 H H H H 0 C(=U)UCH 3 H 2-CHF 2,b-F 0 A-5303 H H H H D0 (= 0)0CH3 H 2-CHF2,6-F 0 A-5304 H H H H if0 (=U)CH 3 H 2-CHF2,b-Me 0 A-5305 H H H H f 0 C(= 0)0CH 3 H 2-CHF 2,6-Me 0 A-5306 H H H H D F GC(=OU)UGH 3 H 2-cycbpropy 1,b-F 0 A-5307 H H H H Hf 0 U)UH 0(= 3 H 2-cycbpropy1,6-F 0 A-5308 H H H H f 0 (=0)UGH3 H 2-cyclopropylb-M e 0 A-5309 H H H H C (=U)UGH3 H 2-cyclopropyl,6-M e 0 A-5310 H H H H D C(=U)UCH 3 H 2-ethenyl,6-F 0 A-5311 H H H H 0 C(=U)UCH 3 H 2-ethenyl,6- e 0 A-5312 H H H H G(= U)UGH 3 H 2-UEt-F 0 A-5313 H H H H f0 G(=U)UGH 3 H 2-UEt6-F 0 A-5314 H H H H D C(= 0)0CH 3 H 2-0Etb-CI 0 A-5315 H H H H Hf G(=U)0G3 H 2-0Et6-C1 0 A-5316 H H H H 0 C(= U)CH 3 H 2-0Etb- e 0 A-5317 H H H H f C(=U)CH 3 H 2-0Et6- e 0 A-5318 H H H H H0Cf C(=U)CH 3 H 2-UCH H2,b-F 0 A-5319 H H H H D0f C(=U)0CH 3 H 2-UCH F 2,6-F 0 A-5320 H H H H C 0(= U)0CH3 H 2-OCH F2,b-Me 0 A-5321 H H H H 0 G(=U)U 3 H 2-UGHH 2 ,6-Me A-5322 H H H H H G(= U)00H 3 H 2-(cycobpropyloxy),b-F 0 A-5323 H H H H 0 G(=U)UGH 3 H 2-(cycbpropyloxy),6-F 0 A-5324 H H H H H i f= 0 U)UCH 3 H 2-(cyclopropy oxy),b-M e 0 A-5325 H H H H 0 C =0)0CH 3 H 2-(cyclopropy bxy),6-M e 0 A-5326 H H H H 0 C(=U)UCH 3 H 2-SMe,b-F 0 A-5327 H H H H C(= 0)0CH 3 H 2-SMe,6-F 0 A-5328 H H H H 0 C(= U)UCH 3 H 2-SMe,b-Me 0 A-5329 H H H H H C(= 0)0CH 3 H 2-SMe,6-M e 0 A-5330 H H H H 0 C(= U)H 3 H 2-S(= 0)Me,b-F 0 A-5331 H H H H (= U)UCH 3 H 2-S(=0)Me,6-F 0 A-5332 H H H H D C(= U)UGH3 H 2-S(= 0)Me,b-Me 0 A-5333 H H H H H G(=0 )0U03 H 2-S(= 0)Me,6-Me 0 A-5334 H H H H D C(= 0)0CH 3 H 2-S(= 0) 2Me,b-F 0 A-5335 H H H H 0 C(=U)UCH 3 H 2-S(= 0) 2Me,6-F 0 A-5336 H H H H 0 C(= U)CH 3 H 2-S(= 0) 2 Me,b-Me 0 A-5337 H H H H 0 C(=U)UCH 3 H 2-S(= 0) 2Me,6-Me 0 A-5338 H H H H D0f )UGH C(= 3 H 2-SCF3,b-F 0 A-5339 H H H H HFf G(=0)UGH 3 H 2-SCF 3 ,6-F 0 A-5340 H H H H H C(=U)00H3 H 2-SCF 3 ,b5-Me 0 A-5341 H H H H D (=U)U 3 H Z-SGH 3, e A-5342 H H H H f0 G(=U)UGH 3 H 2-S(=U)C3,b-F A-5343 H H H H DIf C(=U)UGH 3 H 2-S (= 0)CF 3 ,6-F 0 A-5344 H H H H 0 C(= 0)CH 3 H 2-S(= 0)C1 3,b-Me 0 A-5345 H H H H 0 C(= U)CH 3 H 2-S(= 0)CF 3 ,6-M e 0 A-5346 H H H H H0f G(=0)UGH 3 H 2-S =0 ) 20 3 ,b-H A-5347 H H H H D Cf )UGH H(= 3 H 2-S(= 0) 2CF 3 ,6-F W A-5348 H H H H 0G(0)0H3 H 2-S(=0) 20F3,b-M e 0 A-5349 H H H H G0 0)UGH 3 H 2-S(=0) 20F 3 ,6-M e 0 A-5350 H H H H D C(= U)0CH 3 H 2-(cycobpropy1thb),b-F 0 A-5351 H H H H H C(= U)0CH 3 H 2-(cycobpropy ltho),6-F 0 A-5352 H H H H H G(= U)GH 3 H 2-(cycobpropy thio),b-M e 0 A-5353 H F FH IH0 C(= 0)0CH 3 H 2-(cycobpropy thio),6-M e
[0220]
[Table 95]
com pound R' R2 R R A R R' (R)m p A-5354-i H H H H 0 0(=U)UGH 3 H 2-0(=O)Me,b-F 0 A-5355 H H H H H if 0 C(=U)0GH 3 H 2- 0(= )M e,6-F 0 A-5356 H H H H Df C=0 )0H3 H 2-(=0)M e,b5- e 0 A-5357 H H H H f G(= )0H 3 H 2-(= U)Me,6-Me A-5358 H H H H Di0 )UGHC(= 3 H 2-GH 2UH,b-F A-5359 H H H H D0f )UGHC(= 3 H 2-GH 20H,6-F 0 A-5360 H H H H C U0G00CH 3 H 2-CH 2UH,b5-M e 0 A-5361 H H HHiff C(= )UGH3H 2-CH2UH,6 -Me 0 A-536 Hf2 H H H 0 C0(= 0)GH 3 H 2-0H 20H 3 ,4-F 0 A-5363 H H H H D F0 G(=U)UGH 3 H 2-GH20H3,5-F 0 A-536 Hf4 H H H i 0 C(= )00H3 H 2-GH 20H 3 ,6-F 0 A-5365 i H H H H f 0 G(=0 )GH3 H 2-CH20CH3,4-M e 0 A-5366 H H H H C =0 )0H3 H 2-CH 20CH 3 ,b-i e A-5367 H H H H f 0(= 0)UGH 3 H 2-GH 20CH 3 ,6-MAe 0 A-5368 H H H H DIf )UGHC(= 3 H 2-0C(0 )CH 3 ,b-F 0 A-5369 H H H H i0 G(=U)UGH 3 H Z-GC(=U)GH 3 ,6- 0
A-5370 H H H H 0 (=U)UH 3 H Z (=U)GH 3,b e 0 A-5371 H H H H 0 DG(= U)0UH3 H 2-00(=0)CH 3,6-M e 0 A-5372 H H H H H0f G(=U)UGH 3 H 2-OS =0 ) 2 H 3 ,b-H A-5373 H H H H Df C(= 0)0GH 3 H 2-OS =0 ) 2 H 3 ,6-F 0 A-5374 H H H H 00(=U)UGH3 H 2-S(= 0)2CH3,b- e 0 A-5375 H H H H F 0 U)0GH 3 H 2-S(= 0) 2 CH 3,6-M e 0 A-5376 H H H H Ef DH(= )UGH 3 H 2-0H 2 S0H 3 ,b-4 0 A-5377 H H H H Hf C(= )0GH 3 H 2-0H 2 S0H 3 ,6-F 0 A-b38 H H H H C =0 )0GH 3 H 2-CH 2SCH 3,5-M e 0 A-53/9 H H H H (= )UH3 H 2-CH 2SCH 3,6-Me 0 A-5380 H H H H f0 G(=U)UH 3 H Z-Me 2 ,b-H 0 A-5381 H H H H i 0 C0(= U)UGH 3 H 2-NM e 2 ,6-F 0 A-5382 H H H H D C(= 0)0H 3 H 2AM e 2 ,b-M e 0 A-5383 H H H H iff C(= )UGH3H 2-NM e2,6-M e 0 A-5384 H H H H 0 C = 0)UH 3 H 2-ON,4-F 0 A-5385 H H H H H 0 C= 0)0H 3 H 2-GN,b-F 0 A-5386 H H H H H C0)0GH =F 3 H 2-ON,6-F 0 A-5387 H H H H iff G(=U)UGH3 H 2-GN,6-M e 0 A-5388 H H H H f 0 0(=U)UGH 3 H 2-ONb-OMe 0 A-5389 H H H H D C= 0)0 H3 H 2-N,6-OM e 0 A-5390 H H H H H C(= 0)0GH 3 H 3-CN,6-M e 0 A-5391 H H H H 0 0 =0)0H 3 H 3-ON,6-OMe 0 A-5392 H H H H 0 C(=U)UGH 3 H 4-ON,2-Me 0 A-5393 H H H H D I C=0 )UGH3 H 4-ON,2-M e 0 A-5394 H H H H DIf )UGHC(= 3 H 2-0 2,4-F 0 A-5395 H H H H D0f )UGHC(= 3 H 2-N0 2 ,b-F 0
A-5396 H H H H H0f G(=0)UG3 H 2-N0 2 ,6-F 0 A-5397 H H H H f G(=0 )0H3 H 2-0 2,4-MAe 0 A-5398 H H HHifD G(=U)U 3 H 2-N02,1b- e 0 A-5399 H H H H G(= U)U 3 H 2-0 2,6-MAe 0 A-5400 H H H H f 0(= U)UGH 3 H 2-M e,4,b-F 2 0 A-5401 H H H H iff R(= U)UH3 H 2-M e,6-Et 0 A-5402 H H H H iff (= U)UH3 H 2-cyclopropyl,6-OM e 0 A-5403 H H H H f C(=U)0H 3 H 2-M e,b-Et 0 A-5404 H H H H D0f (= U)00H 3 H 2,6-Et 2 0 A-5405 H H H H H0f G(=U)0H 3 H 2-Et,6-F 0 A-5406 H H H H f0 G(=U)UGH 3 H Z-0H 2UGH 3,6-CI F A-5407 H H H H Ei0 C (=U)UGH 3 H 2-OH 20H 2CH 3 ,6-I1 0 A-5408 IfH H H H H0 (= 0)0GH 3 H 2-OH 2 NMe 2 0 A-5409 H H H H E000 C(= 0)U0H 2GH 3 H H A-5410 H H FH Hi0 (= 0)0H 2CH 3 H 2-F0
[0221]
[Table 96]
com pound R' R2 R R A R6 R(R°)m P A-5411 H H H H 0 C(=O)UGH 2CH 3 H 2-C 1 0 A-5412 H H H H C (=O)UGH 2CH 3 H 2-Br 0 A-5413 H H H H D C = )0GH 2CH 3 H 2-OH 0 A-5414 H H H H if 0 C0)=H00H 2GH 3 H 2-M e 0 A-5415 H H H H D C(=O)UH 2CH 3 Cf H 2-Et 0 A-5416 H H H H f C(= O)UH 2CH 3 H 2-Pr 0 A-5417 H H H H D fCO)UGH2CH3 H 2-CF3 0 A-5418 H H H H 0 C =O)UGH 2CH 3 H 2-UH F 2 A-5419 H H H H 0 C= O)UH 2CH 3 H 2-CH 2F 0
A-5420 H H H H D 0(=O)UGH20H3 H 2-GF201 0 A-5421 H H H H i 0 C(=O)UGH 20H 3 H 2-cycbpropyl 0 A-5422 H H H H D 0(=O)UGH20H 3 H 2-ycbbutl 0 A-5423 H H H H C(=O)UGH 2 0 3 H 2-cycbpentl 0 A-5424 H H H H 0 C(=O)UGH 2CH 3 H 2-ethenyl 0 A-5425 H H H H 0 C(=O)UGH 2CH 3 H 2-allyl A-5426 H H H H G O )0H20H 3 H 2-(prop-1-en-1-y D A-5427 H H H H i 0 = U()UGH 2 0H 3 H 2-(trifboroetheny D 0 A-5428 H H H H D0 =O )U0H2CH3 H 2-0M e A-5429 H H H H Hi0 G O)UH 20H 3 H 2-UEt A-5430 H H H H 0 C -=0)0H2CH 3 H 2-OPr 0 A-5431 H H H H H C(= U)0H 2CH 3 H 2-0(/-Pr) 0 A-5432 H H H H i C = )0GH 2CH 3 H 2-00G3 0 A-5433 H H H H D C = )0GH 2CH 3 H 2-0CH F 2 A-5434 H H H H C =0 )0GH 2CH 3 H 2-(cycbpropy bxy) 0 A-5435 H H H H ifE0if C= 2000H3 H 2-(cycobbutloxy) 0 A-5436 H H H H C(=O)UGH 2 0H 3 H 2-(cycbpentybxy) 0 A-5437 H H H H CtO)OCH 2CH3 Gi H 2-((2,2-d ch brocycbpropy )oxy) A-5438 H H H H i 0 C=U)0UH 2CH 3 H 2-(oxiran-2-y 0 A-5439 H H H H 0 C (=O)UH 2CH 3 H 2-SMe 0 A-5440 H H H H 0 C (=O)0H 2CH 3 H 3-SMe 0 A-5441 H H H H F C(=O)UGH 2CH 3 H 2-S(=O)Me 0 A-5442 H H H H 0 C(=O)0H 2CH 3 H 3-S(=O)M e 0 A-5443 H H H H C(=O)UGH 2CH 3 H 2-S(= ) 2M e 0 A-5444 H H H H E 0 C(=O)OCH2 CH 3 H 3-S =U) 2Me 0 A-5445 H H H H E 0 C (=O)UGH2CH 3 H 2-SGF3 0 A-5446 H H H H CO0U)UH 2 H3 H 3-SCF3 A-5447 H H H H Ei0 C(=OOCH2 CH 3 H 3-S(=O)CF 3 0 A-5448 H H H H Df C(= U)U0H 2CH 3 H 3-SCF(3 2 A-5449 H H H H 0 C(=O)UH 2CH 3 H 2-(cycbpropyth b) 0 A-5450 H H H H 0 C(=O)UH 2CH 3 H 2-(cycbpropysu finy D 0 A-5451 H H H H 0 C(=O)UH 2CH 3 H 2-(cycobpropy u fony D 0 A-5452 H H H H E D C(=O)UGH 2CH 3 H 2-C(=0)Me 0 A-5453 H H H H Hi C(=O)OCH 2CH 3 H 2-CH 2C(=O)CH 3 0 A-5454 H H H H Df C(=O)OCH 2CH 3 H 2 C(=O)CF 3 A-5455 H H H H G O CH 2CH 3 H 2-CH 2 GH3 A-5 4 56 HfH HfHif0 n7=)OC 2CMH 3 - H 2 -C H 200CH 3 0 A-5457 H H H H DIf C =H )GH 2H 3 H 2- C H 0H 223CH 0
A-5458 H H H H 0 C =O)0H 2CH 3 H 2-CH 2SCH 3 0 A-5459 H H H H D C(= U)0H 2CH 3 H 2-CH 2S = )CH 3 0
A-5460 H H H H H GC(=U)oCH 2CH 3 H 2-CH 2S= U) 2CH 3 0
A-5461 H H H H E D C(= U)0H 2CH 3 H 2-(benzybxy) A-5462 H H H H Hi C(=O)OCH 2C 3 H 2-NH 2 A-5463 H H H H E C(=O)OCH 2C3 H 2-NHMe 0 A-5464 H H H H E D C(=O)UGH 2CH 3 H 2 M(Ne)2 0 A-5465 H H H H 0 C(=O)UGH 2CH 3 H 2-(1,3-doxolan-2-yD 0 A-5466 H H H H H C(=O)OCH 2CH 3 H 2-(1,3-d bxan-2-y D A-5467 H f FIF H (= U)0H 2CH 3 H 2-(H-m idazokE2-yD
[0222]
[Table 97]
com pound R' R2 R R A R R' (R)m p A-5468 H H H H 0 C(=U)UGH 2CH 3 H 2-(thiazol-2-yl) 0 A-5469 H H H H i 0 C(=U)UGH 2CH 3 H 2-(oxazol-2-yD 0 A-5470 H H H H H D C(=0)0H 2CH 3 H 2-GH=N0H 0 A-5471 H H H H H 0 C(=U)0H 20H 3 H 2-CH=NOMe 0 A-5472 H H H H D if 0 ( )UCH 2CH3 H 2-(4,b-dihydro-3-isoxazolyD 0 A-5473 H H H H f D0i (=U)0H 2CH 3 H 2-N 0 A-5474 H H H H D C(=0)0H 2CH 3 H 2-NO 2 0
A-5475 H H H H D0 C0 (=U)0H 2CH3 H 2-F,6-GI 0 A-5476 H H H H 0 C(=0)UCH 2CH 3 H 2-F,6-Me 0 A-5477 H H H H i C (=O)OCH2 CH 3 H 3-F,6-Me 0 A-5478 H H H H i 0 G(=O)OCH 2CH 3 H 4-F,2-M e 0 A-5479 H H H H H C (=O)OCHCH 3 H 2-F,6-0Me 0 A-5480 H H H H C(=O)OCH 2CH 3 H 3-F,6-UMe A-5481 H H H H 0 C(=O)OCH 2CH 3 H 2,6- 012 A-5482 H H H H f D C(=U)OCH 2CH 3 H 2-GI,6-M e 0 A-5483 H H H H f0 (=U)GH 2CH 3 H 3-GI,6-M e 0 A-5484 H H H H f0 G(=U)GH 2 H 3 H 4-GI,2-M e 0 A-5485 H H H H H0f C(=U)UGH 2CH 3 H 2-Lb-F 3 0 A-b486 H H H H 0 G(=U)OCH 2CH 3 H 2-C,6-GF 3 0 A-b487 H H H H iff C(=)OCH2CH3 H 2-GI,6-0Me 0 A-5488 H H H H 0 C(=O)OCH 2CH 3 H 3-IL6-UMe 0 A-b489 H H H H H F C(=O)OCH 2CH 3 H 4-GI,2-UMe 0 A-b490 H H H H C (=O)OCH 2CH 3 H 2,4-M e 2 0 A-b491 H H H H f C(=U)OCH 2CH 3 H 2,b-M e 2 0 A-b492 H H H H H C(=U)OCH 2CH 3 H 2,6-M e 2 0
A-b493 H H H H G(=U)GCH 2CH 3 H 2-M e,4-GH 3 0 A-b494 H H H H H G(=U)CH 2CH 3 H 2-M e,b-GH 3 0 A-b495 H H H H Hf 0 0(=U)OCH 2CH 3 H 2-Me,6-F 3 0 A-b496 H H H H C0(=U)CH 2CH3 H 2-Me,4-0Me A-b497 H H H H iff C(=U)UCH 2CH3 H 2-Me,b-0Me 0 A-b498 H H H H CG(=U)CH2CH3 H 2-Me,6-0Me 0 A-b499 H H HHiff C(=U)UCH 2CH3 H 3-Me,6-0Me 0 A-bb 0 H H H H i 0 i0 C (=U)CH 2CH 3 H 4-M e,2-UMe 0 A-bb01 H H H H f 0 (=U)CH2CH3 H Z,b-UMe2 0 A-bb02 H H H H H C 0(=U)CH 2CH 3 H 2,6-UMe 2 0 A-bb03 H H H H H C(=U)CH 2CH 3 H 2-OMe,6-CF 3 0 A-bb04 H H H H Hi0 G(=U)UGH 2CH 3 H 2 ,b-H 0-HH
A-bbb H H H H D0f C(=U)UCH 2CH 3 H 2-GHF 2,6-F 0 A-bb06 H H HH iff C(=U)UCH 2CH3 H 2-GHF 2,b-Me 0 A-bb0 H H H H 0 C(=U)UCH 2CH 3 H 2-GHF 2,6-Me 0 A-bb08 H H H H iff C(=U)UCH 2CH3 H 2-cycbpropyLb-F 0 A-bb09 H H HH iff D (=U)UCH 2CH3 H 2-cycbpropyL,64 0 A-bbl H H H H if0 CG(=U)UH 2CH3 H 2-cyclopropyLb-Me 0 A-bbl1 H H H H if0f G(=U)UH2CH3 H 2-cyclopropyL,6-Me 0 A-bbl2 H H H H C G(=U)OCH2CH3 H 2-ethenyl,6-F 0 A-bbl3 H H H H 0 G(=U)OCH 2CH 3 H 2-ethenyl,6-Me 0 A-bbl4 H H H H f DI C(=)OCH 2CH 3 H 2-OEt,b-F 0 A-bb1b H H (=U)UCHH2CH3 HH 2-OEt,6-F DI0 0 A-bbl6 H H H H f DI C(=U)UCH 2CH 3 H 2-OEt,b-Cl 0 A-bbl H H H H 0i CG(=U)UCH 2CH 3 H 2-UEt,6-GI F A-bbl8 H H H H D (=)OCH 2CH 3 H 2-OEt,b-M e 0 A-bbl9 H H H H 0 G )OCH 2CH 3 H 2-UEt,6-M e 0 A-bb20 H H H H i0 G(=U)UGH 2CH 3 H Z-GHH2b-H 0 A-bb21 H H H H Hf D C(=U)OCH 2CH 3 H 2-CHF 2,6-F 0 A-bb22 H H H H H 0 C(=U)UCH 2CH 3 H 2-OCHF 2 ,b-M e 0 A-bb23 H H H H H 0 GTU)UCH 2CH 3 H 2-CHF 2 ,6-M e 0 A-bb24 H H H H 0 C(=U)UCH 2CH 3 H 2-(cyclopropyloxy),b-F 0
[0223]
[Table 98]
com pound R' R2 R R A R R' (R)m p A-5525 H H H H 0 C(=U)UGH 2CH 3 H 2-(cycobpropyloxy),6-F 0 A-5526 H H H H C (=O)OCH 2CH3 H 2-(cyclopropyloxy),b-M e 0 A-5527 H H H H i C (=O)OCH 2CH3 H 2-(cyclopropybxy),6-Me 0 A-5528 H H H H H 0 G(=O)UH 20H 3 H 2-SMe,b-F 0 A-5529 H H H H D F C ()OCH2CH3 H 2-SMe,6-F 0 A-5530 H H H H 0 C(=O)OCH 2CH 3 H 2-SMe,b-Me 0 A-5531 H H H H Df C(=O)OCH 2CH 3 H 2-SMe,6-M e 0 A-5532 H H H H 0 C(=)OCH 2CH 3 H 2-S(=0)Me,b-F 0 A-5533 H H H H i 0 C(=)OCH 2CH 3 H 2-S(=0)Me,6-F 0 A-5534 H H H H D G(=O)UH 20H 3 H 2-S(=0)Me,b-M e 0 A-5535 H H H H 0if 0 G(=U)0H 20H3 H 2-S(=U)Me,6-M e 0 A-5536 H H H H D G(=O)UH 20H 3 H 2-St=U) 2Me,5-F 0 A-5537 H H H H C=)U0H 20H 3 H 2-St=U) 2Me,6-F A-5538 H H H H D C(0)CH 2CH 3 H 2-S(=U) 2 Me,b-Me 0 A-5539 H H H H H D C(=0)CH 2CH 3 H 2-S(=U) 2Me,6--M e 0 A-5540 H H H H H0C (=U)UH 20H3 H 2-SCF 3,b-H A-5541 H H H H f0 n(=U)UH 20H 3 H 2-SCF 3 ,6-1 0 A-5542 H H H H H D c(0)CH 2CH 3 H 2-SCF 3 ,b-M e 0 A-5543 H H H H 0 =O) H20H 3 H 2-SCF 3 ,6-M e 0 A-5544 H H H H DIC0 (=U)OCH 2CH3 H 2-S(=O)CF 3,b-F 0 A-5545 H H H H 0 C (=O)OCH 2CH 3 H 2-S(=U)CF 3 ,6-F 0 A-5546 H H H H 0 C (=O)OCH 2CH 3 H 2-S(=O)CF 3 ,b-Me 0 A-5547 H H H H C (=U)OCH 2CH 3 H 2-S(=O)CF 3 ,6-Me 0 A-5548 H H H H C (=O)OCH 2CH 3 H 2-S(=U) 2CF 3 ,b-F 0 A-5549 H H H H C (=O)UGH 20H 3 H 2-S(=U) 20F 3 6- 2 A-bbb0 H H H H 0 C (=O)UGH 20H 3 H 2-S(=U) 20F 3 ,b-Me 0 A-bbb1 H H H H f C(=O)UGH 20H 3 H 2-S(=U) 20F 3 ,6-Me 0 A-5552 H H H H Hi0 C-(=U)OCH 2CH 3 H 2-(cyclopropyltho),b-F 0 A-5553 H H H H C 0(=O)OCH 2CH 3 H 2-(cycobpropylthb),6-F 0 A-5554 H H H H 0 C(=O)OCH 2CH 3 H 2-(cycobpropylthio),b-Me 0 A-bbbb H H H H F C(=O)OCH 2CH 3 H 2-(cycobpropylthio),6-Me 0 A-5556 H H H H 0 C(=O)OCH 2CH 3 H 2-C(=0)Me,b-F 0 A-bbb7 H H H H f C(=U)UCH 2CH 3 H 2-C(=U)Me,6-F 0 A-bbb8 H H H H H 0 C(=U)UCH 2CH 3 H 2-C(=O)Me,b-Me 0 A-5559 H H H H CDC(=U)UCH2CH3 H 2-C(=O)Me,6-Me 0 A-5560 H H H H H D C(=U)UGH 2 H3 H 2-CH 2UH,b-H 0 A-5561 H H H H 0 0 (=U)UCH 2CH3 H 2-CH2UN,6-H 0 A-5562 H H H H D C(=U)CH 2CH 3 H 2-CH 2UH,b-M e 0 A-5563 H H HH iff C(=U)UCH 2CH3 H 2-CH2UH,6-M e 0 A-5564 H H H H f DI C(=U)UCH 2CH 3 H 2-CH 20H 3 ,4-F 0 A-5565 H H H H f DI C(=U)UCH 2CH 3 H 2-CH 20H 3 ,b-F 0 A-5566 H H H H H0f D (=U)UCH 2CH 3 H 2-CH 20H 3 ,6-F 0 A-5567 H H H H f o (=U)UH 2CH3 H 2-CH 2UCH3,4-M e 0 A-5568 H H H H o(=U)UCH23H 2-CH2UCH3,b-M e 0 A-5569 H H H H CDG(=U)UCH2CH3 H 2-CH 2CH3,-A e 0 A-bb7 0 H H H H T G(=U)GCH 2CH 3 H 2-C(=U)CH 3,b-F A-bb71 H H H H D C(=O)CH 2CH 3 H 2-UC(=U)CH 3 ,6-F 0 A-5572 H H H H D CG(=O)CH 2CH 3 H 2-UC(=U)CH 3,b-Me 0 A-5573 H H H H D C(=U)UCH 2CH 3 H 2-UC(=U)CH 3 ,6-M e 0 A-5574 H H H H H0Cf (=U)UCH 2CH 3 H 2-U S=U) 2CH 3 ,b-F A-bb7b H H H H Hf DH(=U)UGH 2CH 3 H 2-US(=U) 2CH 3 ,6-F 0 A-5576 H H H H H C =)CH 2CH 3 H 2-U S=U) 2CH 3,b-e A-bb77 H H H H H C =)CH 2CH 3 H 2-U S=U) CH 2 3,6-Me A-bb78 H H H HfF0D (=U)CH 2CH 3 H 2-CH 2 SCH 3 ,b-F 0 A-5579 H H H H HF C (=U)UCH 2CH 3 H 2-CH 2 SCH 3 ,6-F 0 A-bb80 H H H H H CGT=U)GCH 2CH 3 H 2-CH 2SCH 3,b-Me 0 A-bb81 HH H H 10f C (=U)CH 2CH 3 H 2-CH 2SCH 3,6-Me 0
[0224]
[Table 99]
com pound R' R2 R R A R R' (R)m p A-5582 H H H H 0 O(=O)OH 2CH 3 H 2-NM e 2 ,b-F 0 A-5583 H H H H C (=O)UGH 2CH 3 H 2-NM e 2 ,6-F 0 A-5584 H H H H 0 (=O)UGH 2CH 3 H 2-NM e 2 ,b-Me 0 A-bb8b H H H H i 0 C(=O)OH OH 2 3 H 2-NMe 2 ,6-M e 0 A-5586 H H H H f Df O(=O)UGH 2CH 3 H 2-ON,4-F 0 A-bb8 H H H H ifDf O(=U)UH2CH3 H 2-ON,b-F 0 A-bb88 H H H H i Dif 0 (=U)UH 2CH 3 H 2-ON,6-F 0 A-bb89 H H H H ifI I O(=U)UH 2CH3 H 2-ON,6-M e 0 A-bb90 H H H H H if 0 O(=U)UH 2CH 3 H 2-ON,b-OMe 0 A-bb91 H H H H H D G(=O)UGH 2 0H 3 H 2-ON,6-OMe 0 A-bb92 H H H H i 0 G(=O)UGH 20H 3 H 3-ON,6-M e 0 A-bb93 H H H H i 0 0(=O)UGH 2 0H 3 H 3-ON,6-OMe 0 A-bb94 H H H H G(=O)UGH 20H 3 H 4-ON,2-M e 0 A-5595 H H H H 0 O(=O)UGH 2CH 3 H 4-ON,2-OMe 0 A-bb96 H H H H 0 O(=O)U0H 2CH 3 H 2-N0 2,4-F 0 A-bb9/ H H H H Hi0 G(=O)UH 20H 3 H 2-N0 2 ,b-H 0 A-bb98 H H H H Hi0 G(=U)UGH 20H 3 H 2-N0 2,6-F 0 A-bb99 H H H H H D O(=U)U0 H2CH 3 H 2-N0 2,4-MA e 0 A-5600 H H H H f0 0(=U)UH 20H 3 H 2-NU 2,b-MAe 0 A-b601 H H H H iff O(=U)G0H 2CH3 H 2-NU 2,6-M e 0 A-5602 H H H H 0 0C(=O)UGH2CH3H 2-Me,4,b-F2 0 A-5603 H H H H f 0 (=O)UH 2CH 3 H 2-Me,6-Et 0 A-b604 H H H H f 0 (=O)UH 2CH 3 H 2-cyclopropyl,6-OMe 0 A-560b H H H H f 0 (=O)UH 2CH 3 H 2-Me,b-Et 0 A-5606 H H H H Hf O(=O)UGH 20H 3 H 2,6-Et2 0 A-5607 H H H H i 0(=U)G0H 20H 3 H 2-Et,6-F 0 A-5608 H H H H f0 0(=U)UH 20H 3 H 2-GH 20H 3 ,6-C 1F A-5609 H H H H i 0 0(=U)G0H 2CH 3 H 2-OH 20H 2CH 3 ,6-OI 0 A-b610 if H Hf D C(=U)UGH2CH 3 H 2-OH 2 NMe 2 0 A-b611 H H H H Df O(=U)N (OH3 2 H H 0 A-b612 H H H H D0f O(=O)N (H 3) 2 H 2-F 0 A-b613 H H H H H 0 O(=0)N (H 3) 2 H 2-G1 0 A-5614 H H H H IF (=)N (H 3) 2 H 2-Br 0 A-5615 H H H H 0 G(=U)N (H 3) 2 H 2-OH 0 A-b616 H H H H H D C(=0)N (OH 3) 2 H 2-M e 0 A-b617 H H H H H D G=U)N(OH) 2 H 2-Et 0 A-5618 H H H H f0 C G(=)N(OH 3) 2 H 2-Pr 0 A-b619 H H H H O 0(=U)N (OH3)2H 2-OF3 0 A-b620 H H H H 0 O(=U)N (H 3) 2 H 2-HF 2 0
A-b621 H H H H 0 C(=0)N (OH 3) 2 H 2-GH 2F 0
A-b622 H H H H 0 (=U)N (H 3) 2 H 2-GF 2OI 0 A-b623 H H H H H D C(0)N(H 3 2 H 2-cycbpropyl 0 A-5624 H H H H H 0 G(=U)N (H 3 2 H 2-cyclobutyl 0 A-562b H H H H f0 C (=)N (H 3) 2 H 2-cyclopentyl 0 A-b626 H H H H D G()N (OH 3) 2 H 2-ethenyl1 A-5627 H H H H f0 G()N (H 3 2 H 2-aIlyl 0 A-b628 H H H H D0(=U)N (OH 32 H 2-(prop-1-en-1-y) 0 A-b629 H H H H D0 (=0)N (OH 3)2 H 2-(triffloroethenyD 0 A-b630 H H H H 0 C(=)N (H 3) 2 H 2-0Me A-5631 H H H H Hi0 G(=U)N(OH 3) 2 H 2-UEt 0 A-b632 H H H H H D c(=U)N(H 3 2 H 2-OPr 0 A-5633 H H H H f0 0(=)N(H 3 2 H 2-0 (/-Pr) 0 A-5634 H H H H i G(=U)N (OH 3) 2 H 2-GH 3 A-b63b H H H H i 0 C(=U)N (H 3) 2 H 2-UGHF 2 0
A-5636 H H H H 0 C(=U)N (OH 3 2 H 2-(cycbpropybxy) 0 A-5637 H H H H 0 0(=U)N(H 3 2 H 2-(cyclobutyloxy) 0 A-b638 H FfH if 0 0 (=U0)N (OH 3) 2 H 2-(cyclopentybxy) 0
[0225]
[Table 100]
com pound R' R2 R R A R R' (R)m p A-5639 H H H H 0 0(=O)N (H 3) 2 H 2-((2,2-dichbrocycbpropyI)oxy) 0 A-5640 H H H H i 0 O(=O)N (H 3 ) 2 H 2-(oxiran-2-yD 0 A-5641 H H H H Hif 0 (0)N (H 3) 2 H 2-SMe 0 A-5642 H H H H i 0 G(=U)N (H 3) 2 H 3-SMe 0 A-5643 H H H H D i 0 A()N (H 3)2H 2-S(=0)Me 0 A-5644 H H H H i O(=U)N (H 3) 2 H 3-S(=0)Me 0 A-5645 H H H H i 0 A()N (H 3) 2 H 2-S(=U) 2 Me 0 A-5646 H H H H i O(=U)N (H 3) 2 H 3-S(=U) 2 Me 0 A-5647 H H H H i 0 O(=U)N (H 3) 2 H 2-SOF 3 0 A-5648 H H H H HFf O(=U)N (H 3) 2 H 3-SGF 3 0 A-5649 H H H H H0f ((=U)N(OH 3) 2 H 3-S(=U)GH 3 0
A-5650 H H H H HFf D (=U)N (H 3) 2 H 3-SGF(GF 3) 2 0 A-5651 H H H H F O()N (H 3) 2 H 2-(cyclopropyltho) 0 A-5652 H H H H 0 A()N (H 3) 2 H 2-(cycbpropylsufinyD 0 A-5653 H H H H if0f 0 (()N(H 3)2 H 2-(cycbpropylsufonyD 0 A-5654 H H H H 0 ()N (H 3) 2 H 2-G(=U)Me 0 A-5655 H H H H f0 7(=U)N(OH 3) 2 H 2-GH 2G(=O)0H 3 0 A-5656 H H H H f0 0 (=O)N (H 3) 2 H 2-GH 20(=O)0F 3 0 A-5657 H H H H f G(=U)N (H 3) 2 H 2-CH 2 H 0 A-5658 H H H H 0 0(=U)N (H 3) 2 H 2-GH 20H 3 0 A-5659 H H H H 0 C(=O)N (H 3) 2 H 2-GH 2 UGH 20H 3 0 A-5660 H H H H Hf C (=O)N (OH 3) 2 H 2-GH 2SOH 3 0 A-5661 H H H H D C(=O)N (H 3) 2 H 2-GH 2S(=U)CH 3 0
A-5662 H H H H HF f ( =U)N(OH 3)2 H 2-GH2S(=U) 2CH3 0 A-5663 H H H H Hif 0 (0)N (H 3) 2 H 2-(benzybxy) 0 A-5664 H H H H I O G(=U)N (H3)2 H 2-NH 2 A-5665 H H H H f0 G()N (H 3) 2 H 2-NHMe 0 A-5666 H H HH i 0 C(=U)N (0H 3) 2 H 2-N (e) 2 0 A-5667 H H H H 0 N()N(H 3 2 H 2-(1,3-dioxolan-2-yD 0 A-5668 H H H H 0 0(=)N (H 3) 2 H 2-(1,3-dioxan-2-yD 0 A-5669 H H H H 0 C(=)N (H 32 H 2-(l#-idazol2-yDW A-5670 H H H H 0 O(=)N (H 3) 2 H 2-(thiazol-2-y)0 A-5671 H H H H F C (=O)N (H 3) 2 H 2-(oxazol-2-yD 0 A-5672 H H H H Hf G(=U)N (H 3) 2 H 2-GH=NUH 0 A-5673 H H H H f 0(=)N (H 3) 2 H 2-OH=NOMe 0 A-5674 H H H H f 0(U)N (H 3) 2 H 2-(4,b-dihydro-3-isoxazoyD 0 A-5675 H H H H 0 0(=U)N(OH 3) 2 H 2-N 0 A-5676 H H H H D0f ((=U)N(OH 3) 2 H 2-NO 2 0
A-5677 H H H H DIf ((=U)N(OH 3) 2 H 2-F,6-GI 0 A-5678 H H H H C (U)N (H 3) 2 H 2-F,6-Me 0 A-5679 H H H H 0 O(=U)N (H 3) 2 H 3-F,6-M e 0 A-5680 H H H H iF O(=U)N (H 3) 2 H 4-F,2-M e 0 A-5681 H H H H 0 G()N (H 3) 2 H 2-F,6-UMe 0 A-5682 H H H H f0 (0)N (H 3 2 H 3-F,6-UMe A-5683 H H H H D (=)N (OH 3) 2 H 2,6-C 2 A-5684 H H H H f G(=U)N (H 3) 2 H 2-GI,6-M e 0 A-5685 H H H H 0 C(=)N (H 3 2 H 3-GI,6-M e 0 A-5686 H H H H 0 C(=U)N (H 3 2 H 4-GI,2-M e 0 A-5687 H H H H 0 0(=O)N (H 3) 2 H 2-Ib-OF 3 0 A-5688 H H H H f 0 G(=U)N (H32 H 2-C,6-GH 3 0 A-5689 H H H H H D C(=0)N (H 3 2 H 2-GI,6-0Me 0 A-5690 H H H H f G(=U)N(H 3 2 H 3-I, 6-UMe 0 A-5691 H H H H G(=)N (OH 3) 2 H 4-OI,2-UMe 0 A-5692 H H H H 0 (=O)N (H 3) 2 H 2,4-M e 2 0 A-5693 H H H H H 0 O(=U)N (OH 3) 2 H 2,b-M e 2 0 A-5694 H H H H f0 G(0)N(H 3 2 H 2,6-M e 2 F A-569 H H FH Hi0 0 (=)N (OH 3) 2 H 2-Me,4-F 3 0
[0226]
[Table 101]
com pound ' R2 RR R A R R' (R)m P A-b696 H H H H D0 (=U)N (H3)2 H 2-M e,b-F3 0 A-569 H H H H 0 (=U)N (H 3) 2 H 2-M e,6-F 3 0 A-b698 H H H H f O(=U)N (H 3) 2 H 2-M e,4-0M e A-5699 H H H H H 0 G(=U)N (H 3) 2 H 2-M e,b-UM e A-b/00 H H H H O(=0)N (H 3) 2 H 2-M e,6-0M e 0 A-b/01 H H H H Df O(=0)N (H 3) 2 H 3-M e,6-0M e 0 A-b02 H H H H i 0 (=U)N (H 3) 2 H 4-M e,2-0M e A-b03 H H H H 0 C(0)N (H 3) 2 H 2,b-UM e 2 0 A-b/ 0 H H H i4 H i 0 O(=0)N (H 3) 2 H 2,6-UM e 2 0 A-b/ 0 i H H H H i 0 O(0)N (H3)2 H 2-UMe,6-F 3 0 A-b06 H H H H i 0 O(=U)N (H 3) 2 H 2-CH 2,b-H 0
A-b/ 70 / H H H H H if 0 (= )N (H3)2H 2-CHH2,6-F 0 A-b/08 H H H H F G()N (H 3) 2 H 2-CHF 2,b-M e 0 A-b/09 H H H H A()N (H 0 3) 2 H 2-CHF 2,6-M e 0 A-b/10 H H H H if0 ( )N(H 3)2 H 2-cycbpropylb-F 0 A-bll H H H H 0 O()N (H 3) 2 H 2-cycbpropyl,6-F 0 A-b12 H H H H Hi 0 G(U)N (H 32 H 2-cyclopropylb-Me 0 A-b/13 H H H H 0DG(=)N (H 3)2 H 2-cyclopropyl,6-Me 0 A-b/14 H H H H f0 G(U)N (H 3) 2 H 2-ethenyl,6-F 0 A-b/lb H H H H 0 C(0)N (H 3) 2 H 2-ethenyl,6-Me 0 A-b716 H H H H 0 C(=U)N (H 3) 2 H 2-Et,b-F 0 A-b1/ H H H H O(=U)N (OH 3) 2 H 2-Et,6-F 0 A-bi18 H H H H D ((=U)N(OH 3) 2 H 2-OEt,b-CI 0 A-b/19 H H H H i 0 O(=U)N (H 3) 2 H 2-UEt,6-CI 0 A-bi20 H H H H C ()N (H 3) 2 H 2-UEt,b-Me 0 A-bi21 H H H H 0 0()N (H 3) 2 H 2-UEt,6-Me 0 A-bi22 H H H H Hf O(=U)N (H 3) 2 H 2-UGHF 2,b-F A-bi23 H H H H i 0 C(=0)N (H 3) 2 H 2-UGHF 2,6-F 0 A-bi24 H H H H 00(0)N (H 3)2 H 2-OHF2,b-Me 0 A-bi2b H H H H f 0()N (H 3) 2 H 2-UGHF 2 ,6-MAe 0 A-bi26 H H H H D F (0)N (H 3)2 H 2-(cyclopropyloxy),b-F 0 A-bi2i H H H H f A()N (H 3) 2 H 2-(cyclopropyloxy),6-F 0 A-bi28 H H H H iff 0 (=U)N(OH 32 H 2-(cyclopropyloxy),b-M e 0 A-bi29 H H H H 0 0 (=O)N (H 3) 2 H 2-(cyclopropyloxy),6-M e 0 A-bi30 H H H H 0 C(=U)N (H 3 2 H 2-SMe,b-F 0 A-bi31 H H H H 0 G(=0)N(H 3) 2 H 2-SMe,6-F 0 A-bi32 H H H H iF O(=U)N (H 3) 2 H 2-SMe,b-Me 0 A-bi33 H H H H D C(=U)N (H 3) 2 H 2-SMe,6-M e 0 A-bi34 H H H H 0 C(=)N (H 3) 2 H 2-S(=0)Me,b-F 0 A-b/3b H H H H 0 (=U)N (H 3) 2 H 2-S(=0)Me,6-F 0 A-b/36 H H H H 0 O(=U)N (H 3) 2 H 2-S(=0)Me,b-M e 0 A-b/3/ H H H H FD (=U)N (H 3) 2 H 2-S(=0)Me,6-M e 0 A-b/38 H H H H if0f (=U)N(OH 3)2 H 2-St=U) 2Me,b-H 0 A-b/39 H H H H 0 ()N(H 3 2 H Z-S(=U) 2Me,6-H 0 A-b/40 H H H H D (=)N (OH 3) 2 H 2-S t=U) 2 M e,5-M e 0 A-b/41 H H H H if0 G(=U)N(H 3)2 H 2-S =U) 2Me,6-MA e 0 A-b/42 H H H H D0(=0)N(OH 3)2 H 2-SOF3,b-F 0 A-b/43 H H H H 0 0(=U)N (OH 3) 2 H 2-SC1 3 ,6-F 0 A-b/44 H H H H D0(0)N (H3)2 H 2-SOF3,b-Me 0 A-b/45 H H H H f0 C O(=)N (H 3) 2 H 2-SOF 3 ,6-M e 0 A-b/46 H H H H ODG(=U)N (H 3)2 H 2-S (=0)CF 3,b-F 0 A-b/4/ H H H H 7 (=U)N (H 3)2 H 2-S =U)F 3,6-F 0 A-b/48 H H H H iff7f (=)N (OH 3)2 H 2-S =U)GH3,b-MA e 0 A-b/49 H H H H O DC(=0)N (H 3)2 H 2-S(=0)CF 3,6-MAe 0 A-b/bO H H H H i0 0 0(=)N (H 3) 2 H 2-S(=0) 20F 3 ,b-F 0 A-b/bl H H H H i0 0 (=U)N (H 3) 2 H 2-S(=U) 20F 3 ,6- 0 A-b/b2 H H H H G (=U)N (OH 3) 2 H 2-S(=U) OF 2 3 ,b-M e 0
[0227]
[Table 102]
com pound R' R2 R R A R R' (R)m p A-b/b3 H H H H D0 (=)N (H 3)2 H 2-S(=U) 2OF3,6-M e 0 A-bib4 H H H H 0 (=O)N (H 3) 2 H 2-(cyclopropylthlo),b-F 0 A-bibb H H H H 0 (=O)N (H 3) 2 H 2-(cyclopropylthio),6-F 0 A-b/b6 H H H H 00G(=)N (H 3)2 H 2-(cyclopropylthio),b-M e 0 A-bib] H H H H D if C (= )N (H 3)2 H 2-(cyclopropylthio),6-Me 0 A-bib8 H H H H 0 O(=O)N (H 3) 2 H 2-0(=)Me,b-F 0 A-b/b9 H H HH ifDA (=U)N(H 3)2 H 2-0(=)Me,6-F 0 A-b/60 H H H H iff O(=O)N (H 3)2 H 2-G(=O)Me,b-M e 0 A-b/61 H H H H i 0 A(=U)N (H 3) 2 H 2-G(=O)Me,6-M e 0 A-b/62 H H H H f 0 (=O)N(H 3) 2 H 2-CH 2UH,b-H A-b/63 H H H H i 0 O(=O)N (H 3) 2 H 2-CH 2 H,6-F A-b/64 H H H H H D G(0)N (H 3) 2 H 2-GH 2 H,b-Me 0 A-b65 H H H H F G(U)N (H 3) 2 H 2-GH 2UN,6-M e A-b/66 H H H H Di 0 A(=O)N (H 3) 2 H 2-0H 20H 3 ,4-F 0 A-b/6/ H H H H HCf D (=O)N (H 3) 2 H 2-0H 20H 3 ,b4 0 A-b/68 H H H H 0 O(=O)N (H 3) 2 H 2-CH 20H 3 ,6-F 0 A-b/69 H H H H f0 OG()N(H 3 2 H 2-CH 2UGH 3 ,4-M e 0 A-b//0 H H H H H D O(=)N (H 3) 2 H 2-GH 20CH 3 ,b-Me 0 A-b/l H H H H f0 G(U)N (H 3) 2 H 2-CH 2UGH 3 ,6-M e 0 A-b//2 H H H H 0 0(=O)N (H 3) 2 H 2-UG(=O)H 3 ,b-F 0 A-b//3 H H H H i0 C(=O)N (H 3) 2 H 2-U0(=U)H 3 ,6-F 0 A-b//4 H H H H f 0 )(=O)N (OH 3) 2 H 2-0 (=U)CH 3 ,b-M e 0 A-b/b H H H H f D A()N (H 3) 2 H 2-0(=U)CH 3 ,6-M e 0 A-b//6 H H H H i A ((=O)N(OH 3) 2 H 2-OS(=U) 2CH 3 ,b 0 A-b]]] H H H H iff ( =O)N(OH 3)2 H 2-US(=U) 20H3,6-F 0 A-bi/8 H H H H if0f A ()N(H 3)2 H 2-US(=U) 2CH3,b-M e 0 A-bi/9 H H H H G(=U)N (H 3) 2 H 2-US(=U) 2CH 3,6-M e 0 A-bi80 H H H H if0 - (=O)N (H 3) 2 H 2-GH 2 SOH 3 ,b4 0 A-b/81 H H H H 0 0(=O)N(H 3) 2 H 2-GH 2 SOH 3 ,6-F 0 A-bi82 H H H H f A()N (H 3) 2 H 2-GH 2SOH 3,b-Me 0 A-bi83 H H H H 0(=U)N (H32 H D 2-GH2SCH3,6-Me 0 A-bi84 H H H H f A()N (H 3) 2 H 2-NM e 2 ,b-F A-b/785 H H H H O (=O)N (H3)2H 2-NMe 2,6-F 0 A-b786 H H H H G(=U)N (H 3) 2 H 2-NM e 2 ,b-M e 0 A-b 8/i H H H H D (=U)N (H 3)2 H 2-NMe2,6-M e 0 A-b Hi8i8 H H H (=O)N (H 3) 2 H 2-ON,4-F 0 A-b/89 H H H H i0 CG(=)N (OH 3) 2 H 2-GN,b-F 0 A-b/9 0 H H H H D 0(=U)N (OH3)2 H 2-GN,6-F 0 A-b/91 H H H H iff ( =O)N(OH 3)2 H 2-GN,6-M e 0 A-b/92 H H H H f DI O(=)N (H 3) 2 H 2-GN,b-OMe 0 A-b/93 H H H H 0 0(=)N (H 3) 2 H 2-GN,6-OMe 0 A-b/94 H H HHiff O(=U)N (H3)2 H 3-GN,6-M e 0 A-b/95 H H H H 0 0()N (H 3) 2 H 3-GN,6-OMe 0 A-b/96 H H H H f0 O(=)N (H 3) 2 H 4-GN,2-M e 0 A-b/9/ H H H H 0 0(U)N (OH 3)2 H 4-GN,2-0M e 0 A-b/98 H H H H i0 G(=)N (OH 3) 2 H 2-N0 2,4-F 0 A-b/99 H H H H 0 C(=O)N(OH 3) 2 H 2-N0 2 ,b-F 0
A-b800 H H H H 0 (=)N (OH 3) 2 H 2-NU 2 ,6- U A-b801 H H H H 0 0(=)N (H 3 2 H 2-NU 2,4-MAe 0 A-b802 H H H H 0 0 (=O)N (H 3) 2 H 2-NU 2,b-MAe 0 A-b803 H H H H 0DC(=0)N (H 32 H 2-NU 2,6-MAe 0 A-b804 H H H H f0 G(=O)N(OH 3) 2 H 2-M e,4,b-H2 0 A-b80b H H H H G(=)N (GH 3) 2 H 2-M e,6-Et 0 A-bBO6 ifiHifiHf0D 0(=U)N(OH 3) 2 H 2-cyclopropyl,6-OMe 0 A-b80/ H H H H 0 C(=O)N (H 3) 2 H 2-Me,b-Et A-b808 H H H H f G(=U)N(OH 3) 2 H 2,6-Et2 0 A-b809 H H H H i O(=O)N (OH 3) 2 H 2-Et,6-F 0
[0228]
[Table 103]
com pound RI R2 R R R A R R' (R)m P A-5810 H H H H H 0 C(=0)N(CH 3 ) 2 H 2-CH 20CH ,6-CI 0 A-5811 H H H H H0 C(=O)N(CH 3 ) 2 H 2-CH 20CH 2 CH ,6-CI 0 A-5812 H H H H H C (=O)N(CH 3 ) 2 H 2-CH 2 NMe 2 0 A-5813 H H H H H 0 C(=0)(4-CDPh H H 0 A-5814 H H H H H 0 C(=)(4-CDPh H 2-F 0 A-5815 H H H H H 0 C (=0)(4-CDPh H 2-CI 0 A-5816 H H H H H 0 C(=0)(4-CDPh H 2-Br 0 A-5817 H H H H H 0 C(=O)(4-CDPh H 2-OH 0 A-5818 H H H H H C 0(=O)(4-CDPh H 2-M e 0 A-5819 H H H H H 0 C(=0)(4-CDPh H 2-Et 0 A-5820 H H H H H 0 C (=0)(4-ClPh H 2-Pr 0 A-5821 H H H H H 0 C(=0)(4-CDPh H 2-GF 3 0 A-5822 H H H H H 0 C(=0)(4-ClPh H 2-CHF 2 0 A-5823 H H H H H 0 C(=0)(4-CDPh H 2-CH 2F 0 A-5824 H H H H H 0 C(=0)(4-CDPh H 2-CF 2C1 0 A-5825 H H H H H 0 C(=0)(4-CDPh H 2-cycbpropyl 0 A-5826 H H H H H F0 C(=0)(4-CDPh H 2-cycbbutyl 0 A-5827 H H H H H 0 C(=0)(4-CDPh H 2-cycbpentyl 0 A-5828 H H H H H 0 C(=0)(4-CDPh H 2-ethenyl 0 A-5829 H H H H H 0 C(=0)(4-CDPh H 2-aIlyl 0 A-5830 H H H H H 0 C(=0)(4-CDPh H 2-(prop-1-en-1-yl 0 A-5831 H H H H H 0 C(=0)(4-CDPh H 2-(trifboroethenyD 0 A-5832 H H H H H 0 C(=0)(4-CDPh H 2-0Me 0 A-5833 H H H H H F0 O(=0)(4-CDPh H 2-0Et 0 A-5834 H H H H H 0 C(=0)(4-CDPh H 2-0Pr 0 A-5835 H H H H H 0 C(=0)(4-CDPh H 2-0 (/-Pr) 0 A-5836 H H H H H 0 C(=0)(4-CDPh H 2-00F 3 0 A-5837 H H H H H 0 C(=0)(4-CDPh H 2-0CHF 2 0 A-5838 H H H H H 0 C(=0)(4-CDPh H 2-(cycbpropybxy) 0 A-5839 H H H H H 0 C(=0)(4-CDPh H 2-(cycbbutybxy) 0 A-5840 H H H H H 0 C(=0)(4-CDPh H 2-(cycbpentybxy) 0 A-5841 H H H H H 0 C(=0)(4-CDPh H 2-((2,2-dichbrocycobpropyDoxy) 0 A-5842 H H H H H 0 C(=0)(4-CDPh H 2-(oxiran-2-yD 0 A-5843 H H H H H 0 C(=0)(4-CDPh H 2-SMe 0 A-5844 H H H H H 0 C(=0)(4-CDPh H 3-SMe 0 A-5845 H H H H H 0 C(=0)(4-CDPh H 2-S(=0)Me 0 A-5846 H H H H H 0 C(=0)(4-C)Ph H 3-S(=0)Me 0 A-5847 H H H H H 0 C(=0)(4-CDPh H 2-S(=0) 2Me 0 A-5848 H H H H H 0 C(=0)(4-CDPh H 3-S(=0) 2Me 0 A-5849 H H H H H 0 C(=0)(4-CDPh H 2-SCF 3 0 A-5850 H H H H H 0 C(=0)(4-CDPh H 3-SCF 3 0 A-5851 H H H H H 0 C(=0)(4-CDPh H 3-S(=0)CF3 0 A-5852 H H H H H 0 C(=0)(4-CDPh H 3-SCF(CF 3 )2 0 A-5853 H H H H 0 C(=0)(4-CDPh H 2-(cycobpropylthio) 0 A-5854 H H H H H 0 C(=0)(4-CDPh H 2-(cycbpropysulfinyD 0 A-5855 H H H H 0 C(=0)(4-CDPh H 2-(cycobpropylsulfonyD 0 A-5856 H H H H H 0 C(=0)(4-CDPh H 2-C(=0)Me 0 A-5857 H H H H H 0 C(=0)(4-CDPh H 2-CH 2C(=0)CH 3 0 A-5858 H H H H H 0 C(=0)(4-CDPh H 2-CH 2C(=0)CF3 0 A-5859 H H H H H 0 C(=0)(4-CDPh H 2-CH20H 0 A-5860 H H H H H 0 C(=0)(4-CDPh H 2-CH 2 0CH3 0 A-5861 H H H H H 0 C(=0)(4-CDPh H 2-CH 2 00H 20H 3 0 A-5862 H H H H H 0 C(=0)(4-CDPh H 2-CH 2SCH 3 0 A-5863 H H H H H 0 C(=0)(4-CDPh H 2-CH 2S(=0)CH 3 0 A-5864 H H H H H F0 C(=0)(4-CDPh H 2-CH 2S(=0) 2 CH3 0 A-5865 H H H H H 0 C(=0)(4-CDPh H 2-(benzybxy) 0 A-5866 H FFHI H 0 C(=0)(4-CDPh H 2-NH 2 0
[0229]
[Table 104]
com pound RI R2 R R R A R R' (R)m P A-5867 iH H H H H 0 C(=0)(4-CDPh H 2-NHMe 0 A-5868 H H H H H 0 C(=0)(4-CDPh H 2-N(Me)2 0 A-5869 H H H H H 0 C(=0)(4-CDPh H 2-(1,3-dbxolan-2-yD 0 A-5870 iH H H H H 0 C(=0)(4-CI)Ph H 2-(1,3-dbxan-2-yD 0 A-5871 H H H H H 0 C(=0)(4-CDPh H 2-(1H--m idazol-2-yD 0 A-5872 H H H H H 0 C(=0)(4-CDPh H 2-(thiazol-2-y) 0 A-5873 H H H H H 0 C(=0)(4-CDPh H 2-(oxazol-2-yD 0 A-5874 H H H H H 0 C(=O)(4-CDPh H 2-CH=N0H 0 A-5875 iH H H H H 0 C(=0)(4-CDPh H 2-CH=NOMe 0 A-5876 iH H H H H 0 C(=0)(4-CDPh H 2-(4,5-dihydro-3-isoxazolyD 0 A-5877 H H H H H 0 C(=0)(4-CI)Ph H 2-CN 0 A-5878 iH H H H H 0 C(=0)(4-CDPh H 2-N0 2 0 A-587 9 H H H H H 0 C(=0)(4-CI)Ph H 2-F,6-CI 0 A-5880 H H H H H 0 C(=0)(4-CDPh H 2-F,6-M e 0 A-5881 H H H H H 0 C(=0)(4-CDPh H 3-F,6-M e 0 A-5882 H H H H H 0 C(=0)(4-CI)Ph H 4-F,2-M e 0 A-5883 H H H H H 0 C(=0)(4-CI)Ph H 2-F,6-0Me 0 A-5884 H H H H H 0 C(=0)(4-CDPh H 3-F,6-0Me 0 A-5885 H H H H H 0 C(=0)(4-CDPh H 2,6-C01 0 A-5886 H H H H H 0 C(=0)(4-CDPh H 2-CI,6-M e 0 A-5887 H H H H H 0 C(=0)(4-CDPh H 3-CI,6-Me 0 A-5888 H H H H H 0 C(=0)(4-CI)Ph H 4-CI,2-M e 0 A-5889 H H H H H 0 C(=0)(4-CDPh H 2-C1,5-CF, WF A-5890 H H H H H 0 C(=0)(4-CDPh H 2-C1,6-CF, 0 A-5891 H H H H H 0 C(=0)(4-CDPh H 2-C1,6-0Me 0 A-5892 H H H H H 0 C(=0)(4-CDPh H 3-C1,6-0Me 0 A-5893 H H H H H 0 C(=0)(4-CDPh H 4-CI,2-0Me 0 A-5894 H H H H H 0 C(=0)(4-CDPh H 2,4-M e 2 0 A-5895 H H H H H 0 C(=0)(4-CDPh H 2,5-M e 2 0 A-5896 H H H H H 0 C(=0)(4-CDPh H 2,6-M e 2 0 A-5897 H H H H H 0 C(=0)(4-CDPh H 2-M e,4-CF3 0 A-5898 H H H H H 0 C(=0)(4-CDPh H 2-M e,5-CF 3 0 A-5899 H H H H H 0 C(=0)(4-CDPh H 2-M e,6-CF3 0 A-5900 H H H H H 0 C(=0)(4-CDPh H 2-M e,4-0Me 0 A-5901 H H H H H 0 C(=0)(4-CDPh H 2-M e,5-0Me 0 A-5902 H H H H H 0 C(=0)(4-CDPh H 2-M e,6-0Me 0 A-5903 H H H H H 0 C(=0)(4-CIPh H 3-M e,6-0Me 0 A-5904 H H H H H 0 C(=0)(4-CDPh H 4-M e,2-0Me WF A-5905 H H H H H 0 C(=0)(4-CDPh H 2,5-0Me 2 0 A-5906 H H H H H 0 C(=0)(4-CDPh H 2,6-0Me 2 0 A-5907 H H H H H 0 C(=0)(4-CDPh H 2-OMe,6-CF3 0 A-5908 H H H H H 0 C(=0)(4-CDPh H 2-CHF 2,5-F 0 A-5909 H H H H H 0 C(=0)(4-CI)Ph H 2-CHF 2,6-F 0 A-5910 H H H H H 0 C(=0)(4-CI)Ph H 2-CHF 2,b-M e 0 A-5911 H H H H H 0 C(=0)(4-CDPh H 2-CHF 2,6-MA e 0 A-5912 H H H H H 0 C(=0)(4-CIPh H 2-cycobpropyl,5-F 0 A-5913 H H H H H 0 C(=0)(4-CDPh H 2-cycobpropyl,6-F 0 A-5914 H H H H H 0 C(=0)(4-CDPh H 2-cyclopropyl,5-Me 0 A-5915 H H H H H 0 C(=0)(4-CDPh H 2-cyclopropyl,6-M e 0 A-5916 H H H H H 0 C(=0)(4-CDPh H 2-ethenyl,6-F 0 A-5917 H H H H H 0 C(=0)(4-CDPh H 2-ethenyl,6-M e 0 A-5918 H H H H H 0 C(=0)(4-CDPh H 2-0Et,5-F 0 A-5919 H H H H H 0 C(=0)(4-CDPh H 2-0Et,6-F 0 A-5920 H H H H H 0 C(=0)(4-CDPh H 2-0Et,5-CI 0 A-5921 H H H H H 0 C(=0)(4-CI)Ph H 2-0Et,6-CI 0 A-5922 H H H H H 0 C(=0)(4-CI)Ph H 2-0Et,5-M e 0 A-5923 H H H H H 0 C(=0)(4-CDPh H 2-0Et,6-M e 0
[0230]
[Table 105]
com pound R' R2 R R A R R' (R)m p A-5924 iH H HH 0 C(=0)(4-CI)Ph H 2-CHF 2,b-F 0 A-5925 H H HH f0 C(=0)(4-C)Ph H 2-CHF 2,6-F 0 A-5926 H H HH 0 C(=0)(4-C)Ph H 2-OCHF 2 ,b-M e 0 A-5927 H H HH 0 C 0(=U)(4-CD)Ph H 2-OCHH 2 ,6-M e 0 A-5928 H H HH 0 C(=0)(4-C)Ph H 2-(cycobpropyloxy),b-F W A-5929 H H HH 0 C(=0)(4-C)Ph H 2-(cycobpropyloxy),6-F 0 A-5930 H H HH Df C(=0)(4-C)Ph H 2-(cyclopropyloxy),b-M e 0 A-5931 H H HH 0 C(=0)(4-CI)Ph H 2-(cyclopropybxy),6-M e 0 A-5932 H H HH 0 C(=0)(4-C)Ph H 2-SMe,b-F 0 A-5933 H H HH 0 C(=0)(4-C)Ph H 2-SMe,6-F 0 A-5934 H H HH f C(=0)(4-CDPh H 2-SMe,b-Me 0 A-5935 H H HH 0 C(=0)(4-DPh H 2-SMe,6-M e 0 A-5936 H H HH 0 C C(=0)(4-CDPh H 2-S(=0)Me,b-F 0 A-5937 H H HH 0 C(=0)(4-DPh H 2-S(=0)Me,6-F 0 A-5938 H H HH 0 C(=0)(4-DPh H 2-S(=0)Me,b-M e 0 A-5939 H H HH 0 C 0(=U)(4-DPh H 2-S(=0)Me,6-M e 0 A-5940 H H HH f0 C C(=0)(4-7Ph H 2-S(=U) 2Me,b-H 0 A-5941 H H H H D0 C(=0)(4-CI)Ph H 2-S(=0) 2Me,6-F 0 A-5942 H H H H f0 C(=0)(4-C)Ph H 2-S(=U) 2 Me,b-M e 0 A-5943 H H H H 0 C(=0)(4-C)Ph H 2-S(=0) 2 Me,6--M e 0 A-5944 H H H H i0 C(=0)(4-C)Ph H 2-SCH3,b-F 0 A-5945 H H H H Hi C 0(=U)(4-CDPh H 2-SCF 3 ,6-F 0 A-5946 H H H H 0 C(=0)(4-C)Ph H 2-SCF 3 ,b-M e 0 A-5947 H H H H F C(=0)(4-C)Ph H 2-SCF 3 ,6-M e 0 A-5948 H H H H H0 C(=0)(4-C)Ph H 2-S(=U)0F 3,b-F 0 A-5949 H H H H H0 C(=0)(4-C)Ph H 2-S(=U)0G 3,6-1 0 A-5950 H H H H 0 C(=0)(4-GI)Ph H 2-S(=U)CF 3 ,b-M e 0 A-5951 H H H H i 0 C(=0)(4-C)Ph H 2-S(=0)CF 3 ,6--M e 0 A-5952 H H H H 0 C(=0)(4-GI)Ph H 2-S(=0) 2CF3,b-F 0 A-5953 H H H H 0 C(=0)(4-GI)Ph H 2-S(=0) 2CF 3 ,6-F 0 A-5954 H H H H 0 C(=0)(4-GI)Ph H 2-S(=U) 2CF 3 ,b-Me 0 A-5955 H H H H 0 C(=0)(4-CI)Ph H 2-S(=0) 2CF 3 ,6-Me 0 A-5956 H H H H f C(=0)(4-GI)Ph H 2-(cycobpropylthb),b-F 0 A-5957 H H H H f C(=0)(4-G)Ph H 2-(cycobpropylthb),6-F 0 A-5958 H H H H 0 C(=0)(4-GI)Ph H 2-(cycobpropylthio),b-M e 0 A-5959 H H H H 0 C(=0)(4-GI)Ph H 2-(cycobpropylthio),6-M e F A-5960 H H H H f0 C(=)(4-0DIPh H 2-G(=0)Me,b-F 0 A-5961 H H H H D C(=0)(4-GI)Ph H 2-G(=0)Me,6-F 0 A-5962 H H H H 0 C(=0)(4-GI)Ph H 2-G(=0)Me,b-M e 0 A-5963 H H H H H 0 C(=0)(4-GI)Ph H 2-G(=0)Me,6-M e 0 A-5964 H H H H 0 C(=0)(4-GI)Ph H 2-GH 20H,b-F 0 A-5965 H H H H i0 C(=0)(4-GI)Ph H 2-GH 20H,6-F 0 A-5966 H H H H f0 C C(=0)(4-I)Ph H 2-CH 2H,b-Me 0 A-5967 H H H H FF C(=)(4-GI)Ph H 2-CH 2UN,6-M e 0 A-5968 H H H H 0 C(=0)(4-GI)Ph H 2-GH 20H 3,4-F 0 A-5969 H H H H CF (=U)(4-GI)Ph H 2-GH20GH3,b-H 0 A-5970 H H H H 0 C(=0)(4-GI)Ph H 2-GH 20H 3 ,6-F 0 A-5971 H H H H D0 C(=0)(4-GI)Ph H 2-GH 20CH 3,4-Me 0 A-5972 H H H H 0 C(=0)(4-GI)Ph H 2-0H 20CH 3 ,b-Me 0 A-5973 H H H H f0 C(=0)(4-GI)Ph H Z-GH 2UGH 3 ,6-e 0 A-5974 H H H H 0 C(=0)(4-CI)Ph H 2-UC(=0)CH 3 ,b-F 0 A-5975 H H H H H C(=0)(4-GI)Ph H 2-C(=U)0H 3,6-1 0 A-5976 H H H H f0 C(=0)(4-GI)Ph H 2-UC(=U)CH 3,b-MAe 0 A-5977 H H H H 0 C(=0)(4-GI)Ph H 2-UC(=0)CH 3 ,6-M e 0 A-5978 H H H H 0 C C(=0)(4-GI)Ph H 2-US(=0) 2CH3,b-F 0 A-5979 H H H H 0 C C(=0)(4-GI)Ph H 2-US(=U) 2CH3,6-F 0 A-5980 HHI HH i C(= 0) (4-G DPh H 2-OS(=0) 2CH3,b-Me 0
[0231]
[Table 106]
com pound R' R2 R R A R R' (R)m p A-5981 H H H H 0 C(= 0)(4-0 DPh H 2-OS(= 0) 2CH 3,6-M e 0 A-5982 H H H H 0 C(= 0)(4-G DPh H 2-OH 2 SCH 3 ,b-4 0 A-5983 H H H H 0 C(= 0)(4-G DPh H 2-0H 2 SCH 3 ,6-F 0 A-5984 H H H H 0 C 0(=0)(4-G DPh H 2-GH 2SCH 3,b- e 0 A-5985 H H H H 0 C(= 0)(4- DPh H 2-0H 2SCH 3,6-Ae 0 A-5986 H H H H 0 C(= 0)(4-0 DPh H 2-NM e 2 ,b-F 0 A-598 / H H H H f C(= 0)(4-0 DPh H 2-NM e 2 ,6-F 0 A-5988 H H H H 0 C(= 0)(4-0 DPh H 2AM e 2 ,b-M e 0 A-5989 H H H H H 0 C(= 0)(4- DPh H 2-NM e 2 ,6-M e 0 A-5990 H H H H if 0 C(0)(4-0 DPh H 2-ON,4-F 0 A-5991 H H H H f 0(= )(4-UODPh H 2-ONb-F 0 A-5992 H H H H 0 C(= 0)(4- DPh H 2-ON,6-F 0 A-5993 H H H H 0 C 0(= )(4-GODPh H 2-ON,6-M e 0 A-5994 H H H H 0 C(= 0)(4- DPh H 2-ON,b-0M e 0 A-5995 H H H H 0 C(= 0)(4- DPh H 2-ON,6-0M e 0 A-5996 H H H H 0 C 0(= )(4- DPh H 3-ON,6-M e 0 A-5997 H H H H f C 0(= )(4- DPh H 3-ON,6-OM e 0 A-5998 H H H H 0 C(= 0)(4- DPh H 4-ON,2-M e 0 A-5999 H H H H 0 C(= 0)(4- DPh H 4-ON,2-UM e 0 A-6000 H H H H 0 C(= 0)(4- DPh H 2-N0 2,4-F 0 A-6001 H H H H 0 C(= 0)(4- DPh H 2-N0 2 ,5-F A-6002 H H H H i0 C 0(=U)(4- DPh H 2-N0 2 ,64 0 A-6003 H H H H 0 C(=0)(4-DPh H 20 2,4-MvAe 0 A-6004 H H H H i iFC0)(4-DPh H 2-0 2,b-M e 0 A-6005 H H H H H0 C(=0)(4-C DPh H 2-AU 2,6-MAe 0 A-6006 H H H H 0 C(= 0)(4- DPh H 2-M e,4,b-F 2 0 A-6007 H H H H 0 C(= 0)(4- DPh H 2-M e,6-Et 0 A-6008 H H H H C(= 0)(4- DPh H 2-cyclopropyl,6-OM e 0 A-6009 H H H H D C(= 0)(4- DPh H 2-M e,b-Et 0 A-6010 H H H H 0 C(= 0)(4- DPh H 2,6-Et 2 0 A-6011 H H H H i0 C(=0)(4-DPh H 2-Et,6-F 0 A-6012 H H H H 0 C(=0)(4-C DPh H 2-OH 20H 3,6-I 0 A-6013 H H H H H 0 C(= 0)(4- DPh H 2-OH 20H 2CH 3 ,6- I 0 A-6014 H H H H 0 C(= 0)(4- DPh H 2-GH 2 NM e 2 0 A-6015 H H H H Ei0 C (=S)UCH 3 H H 0 A-6016 H H H H EH D =S)UH3 H 2-F A-6017 H H H H E 0Cf G(=S)UGH 3 H 2-C1 0 A-6018 H H H H D C(=S)0CH 3 H 2-Br 0 A-6019 H H H H 0 C(= S)CH 3 H 2-OH 0 A-6020 H H H H 0 C(=S)CH 3 H 2-M e 0 A-6021 H H H H 0 C(= S)CH 3 H 2-Et 0 A-6022 H H H H E D C(=S)CH 3 H 2-Pr 0 A-6023 H H H H E 0Cf G(=S)UGH 3 H 2-CH 3 0
A-6024 H H H H E 0 C(=S)OCH 3 H 2-GHF 2 0
A-6025 H H H H D G(=S)OCH 3 H 2-GH2 0 A-6026 H H H H H0f G(=)UGH 3 H 2-H2G F A-6027 H H H H DI0 (=S)CH 3 H 2-cycbpropy 1 0 A-602 8 H H H H 0 C S)CH S(= 3 H 2-ycobbutyl 0 A-6029 H H H H D C(= S)0CH 3 H 2-cycbpentyl 0 A-6030 H H H H Ff0 CH(=)UH 3 H 2-ethenyl 0 A-6031 H H H H E0 C (=S)CH 3 H 2-allyl A-6032 H H HH iff G(=S)OCH3 H 2-(prop-1-en-1-yD 0 A-6033 H H H H C(= S)UGH 3 H 2-(trifboroetheny D 0 A-6034 H H H H D C(= S)0CH 3 H 2-0Me 0 A-6035 H H H H 0 C(= S)CH 3 H 2-0Et 0 A-6036 H H Ef H H ifi (=)UGH3 H 2-0Pr 0 A-03/ H H H H G (=S)UGH 3 H 2-0(/-Pr) 0
[0232]
[Table 107]
com pound ' R2 RR R A R R' (R)m P A-6038 H H H H 0 0(= S)UGH 3 H 2-0 CF, A-6039 H H H H F C(=S)UGH 3 H 2-CHF 2 0 A-6040 H H H H f C(= S)UGH 3 H 2-(cycbpropy bxy) 0 A-6041 H H H H E 0 (=S)0)UH 3 H 2-(cycobbutybxy) 0 A-6042 H H H H D 0 C(=S)UGH 3 H 2-(cycbpentybxy) 0 A-6043 H H H H Df C( S)UGH 3 H 2-((2,2-dbh brocycbpropy Doxy) 0 A-6044 H H H H 0 C(=S)UGH 3 H 2-(oxiran-2-yD 0 A-6045 H H H H 0 C(= S)UGH 3 H 2-SMe 0 A-6046 H H H H 0 C(= S)UH 3 H 3-SMe 0 A-6047 H H H H Hif 0 (=S)UGH 3 H 2-S(=0)Me 0 A-6048 H H H H f 0 S (=S)0H 3 H 3-S(= 0)Me A-6049 H H H H if0 D (=)UGH3 H 2-S(= 0)2Me 0 A-6050 H H H H f G(=)0H 3 H 3-S =0 ) 2Me A-6051 H H H H D0I H(=S)U3GH H 2-SCF3 A-6052 H H H H 0 C(=S)CH 3 H 3-SH3 0 A-6053 H H H H E0 f G(=)UGH3 H 3-S( = U)GH3 A-6054 H H H H E07f (=5)UG3 H 3-SCF(C 3) 2 0
A-6055 H H H H 0 C(=S)CH 3 H 2-(cycobpropylthio) 0 A-6056 H H H H iff G(=S)UGH3 H 2-(cycbpropylsufinyD 0 A-6057 H H H H 0 C(=S)UCH 3 H 2-(cycobpropy u fony D 0 A-6058 H H H H f0 C(=S)CH 3 H 2-C(= 0)Me 0 A-6059 H H H H Hi0 C =S)UCH 3 H 2-CH 2C (=0)CH 3 0 A-6060 H H H H E0 C (=S)UCH 3 H 2-CH 2 C(= 0)0 3 A-6061 H H H H H C(=S)OCH 3 H 2-CH 2 UH 0 A-6062 H H H H (= )UH 3 H 2-H 2 UH 3 0 A-6063 H H H H H0 G(=S)UH 3 H 2-H 2 UGH 2 3 0
A-6064 H H H H H0 C G(=S)CH 3 H 2-CH 272H 3 0
A-6065 H H H H i 0 C =S)OCH 3 H 2-CH 2S (= )CH 3 0 A-6066 H H H H Di C(= S)OCH 3 H 2-CH 2S(= 0) 2 CH 3 A-6067 H H H H 0 C(=S)OCH 3 H 2-(benzybxy) 0 A-6068 H H H Hi Df C(=S)OCH 3 H 2-NH 2 A-6069 H H H H 0 C(=S)OCH 3 H 2-NHMe 0 A-6070 H H H H f C(=S)CH 3 H 2 M(Ne)2 0 A-6071 H H H H f0 C=S)OCH 3 H 2-0,3-dbxoan-2-yD 0 A-6072 H H H H 0 C =S)OCH 3 H 2-0,3-d bxan-2-y D A-6073 H H H H Df C =S)UGH 3 H 2-(1H- idazoE2-yD A-6074 H H HHifi f G(=S)OCH3 H 2-(thiazo-2-yl) 0 A-6075 H H H H F C(= S)OCH 3 H 2-(oxazol-2-yD 0 A-6076 H H H H 0 C(= S)OCH 3 H 2-CH= N0H 0 A-6077 H H H H f 0 C(= S)OCH 3 H 2-CH= NOM e 0 A-6078 H H H H 0 C( S)OCH 3 H 2-(4,b-dihydro-3-oxazo D 0 A-6079 H H H H Ei C (=S)OCH 3 H 2-N 0 A-6080 H H H H Ef G(=S)OH 3 H 2-NO 2 0
A-6081 H H H H 0 E C(=5)UGH3 H 2-F,6-C1 0 A-6082 H H H H iff D G(=5)UG3 H 2-F,6-i e 0 A-6083 H H H H 0 G(=5)H03 H 3-F,6 -Me 0 A-6084 H H H H C0 (=S)OCH3 H 4-F,2-i e 0 A-6085 H H H H DICW (=S)OCH 3 H 2-F,6-0Me 0 A-6086 H H H H 0 C(= S)OCH 3 H 3-F,6-0Me 0 A-6087 H H H H E0f G(=S)UGH 3 H 2,6-C A-6088 H H H H 0 C(= S)OCH 3 H 2- 1,6-M e 0 A-6089 H H H H f0 G =)UH 3 H 3- 1,6-M e 0 A-6090 H H H H 0 (=S)UGH 3 H 4-01,2-M e 0 A-6091 H H H H E0 C (=S)OCH 3 H 2-C1,b-CF 3 A-6092 IH H H H i0 C(=S)OCH 3 H 2-C1,6-CF 3 0 A-6093 H H H H f0 C T=5)U H 2-C 1,6-0M e 0 A-6094 H H H H 0 C(= S)OCH 3 H 3-C 1,6-0M e 0
[0233]
[Table 108]
com pound ' R2 RR R A R R' (R)m P A-6095 H H H H 0 C( S)UGH 3 H 4-C 1,2-0M e 0 A-6096 H H H H F C(=S)UGH 3 H 2,4-M e 2 0 A-6097 H H H H EH C=S)OCH 3 H 2,b-Me 2 0 A-6098 H H H H f 0 C(=S)OCH 3 H 2,6-M e 2 0 A-6099 H H H H D G (= S)OCH 3 H 2-M e,4-0F 3 0 A-6100 H H H H 0 C =S)OCH 3 H 2-M e,b-F 3 0 A-6101 H H H H CS)OCH =0 3 H 2-M e,6-0F 3 0 A-6102 H H H H D C(= S)OCH 3 H 2 -Me,4-0Me 0 A-6103 H H H H if 0 C(=S)OCH 3 H 2- e,b-0Me 0 A-6104 H H H H HiF 0 G(=5)UH3 H 2 -Me,6-0Me 0 A-6105 H H H H i 0 C(=5)UGH3 H 3-M e,6-UM e 0 A-6106 H H H H f 0 G(=5)UGH3 H 4-M e,2-0Me A-6107 H H H H 0(=5)UGH3 H 2,5-UMe 2 0 A-6108 H H H H D C(= S)OCH 3 H 2,6-0M e 2 0 A-6109 H H H H 0 C(= S)OCH 3 H 2-0Me,6-CF 3 0 A-6110 H H H H 0 C=5)UGH 3 H Z-GHH 2,b-H 0
A-611 1 H H H H (=5)UH 3 H ZNH 2,- 0 A-6112 H H H H D C(= S)OCH 3 H 2-CH1 2 b-MAe 0 A-6113 H H H H f G =5)UGH 3 H 2-CH 2,6-M e 0 A-6114 H H H H D0 C=S)OCH3 H 2-cycobpropy 1,b-F 0 A-6115 H H H H C S)UCH 0= 3 H 2-cycobpropy1,6-F 0 A-6116 H H H H if C S)OCH 3 H 2-cyclopropylb-M e 0 A-6117 H H H H D C =S)OCH 3 H 2-cyclopropyl,6-M e 0 A-6118 H H H H C(=S)OCH 3 H 2-ethenyl,6-F 0 A-6119 H H H H if 0 G(=5)CH 3 H 2-ethenyl,6-M e 0 A-6120 H H H H f0 0(=5)UH3 H 2-0Etb-FHF A-6121 H H H H 0 C(=5)CH 3 H 2-0Et6-F 0 A-6122 H H H H 0 C(= S)OCH 3 H 2-0Etb-CI 0 A-6123 H H H H Df C(= S)OCH 3 H 2-0Et6-CI 0 A-6124 H H H H 0 C(= S)OCH 3 H 2-0Etb- e 0 A-6125 H H H H 0 C(=S)OCH 3 H 2-0Et,6- e 0 A-6126 H H H H H 0 C(= S)OCH 3 H 2-UCH ' 2,b-F 0 A-6127 H H H H H0f C(= S)GH 3 H 2-UCH F 2,6-F 0 A-6128 H H H H 0 0 (=5)UH3 H 2-UGH H 2 ,b-M e 0 A-6129 H H H H 0 C(= S)OCH 3 H 2-CH F 2 ,6-MAe 0 A-6130 H H H H D C(=5)CH 3 H 2-(cycbpropyloxy),b-F 0 A-6131 H H H H iff G(=5)UGH 3 H 2-(cycobpropyloxy),6-F 0 A-6132 H H H H C 0 (= S)OCH3 H 2-(cyclopropy oxy),b-M e 0 A-6133 H H H H 0 C(= S)OCH 3 H 2-(cyclopropy bxy),6-M e 0 A-6134 H H H H C 0 (=S)OCH3 H 2-SMe,b-F 0 A-6135 H H H H 0 C(= S)OCH 3 H 2-SMe,6-F 0 A-6136 H H H H 0 C(= S)OCH 3 H 2-SMe,b-Me 0 A-6137 H H H H 0 C =5)CH 3 H 2-SMe,6-M e 0 A-6138 H H H H f C T=5)UH 3 H 2-S(= 0)Me,b-F 0 A-6139 H H H H0 G(=5)UH3 H 2-S(=0)Me,6-F 0 A-6140 H H H H iff 0(=5)UH3 H 2-S (=0 )Me,b- e 0 A-6141 H H H H C 0 (= S)OCH3 H 2-S(= 0)Me,6-Me 0 A-6142 H H H H C0 (= S)OCH3 H 2-S(= 0) 2Me,b-F 0 A-6143 H H H H 0 C(= S)OCH 3 H 2-S(= 0) 2Me,6-F 0 A-6144 H H H H 0 C (=5)UGH3 H 2-S =0 ) 2 Me,b-M e 0 A-6145 H H H H 0 C(= S)OCH 3 H 2-S(= 0) 2Me,6-Me 0 A-6146 H H H H i G(=5)0H 3 H 2-5GH3,b-H A-6147 H H H H i G(=5)0H3 H 2-5GH 3,6- 0 A-6148 H H H H 0 C (=S)OCH 3 H 2-SCF 3 ,b-Me 0 A-6149 H H H H f0 C(=S)OCH 3 H 2-SCF 3 ,6-Me 0 A-6150 H H H H H0 C(=5)UH3 H 2-5= 0)GHF 3 ,b-H A-6151 H H H H H0f C (= S)GH 3 H 2-S (=)CF 3 ,6-F 0
[0234]
[Table 109]
com pound R' R2 R R A R R' (R)m p A-6152 H H H H 0 0( S)UGH 3 H 2-S(= )CF3 ,b-M e 0 A-6153 H H H H 0(= S)UGH 3 H 2-S(= U)F 3 ,6-M e F A-6154 H H H H f 0 (= S)UGH 3 H U )2 2-S (=O ,b-F 0 A-6155 H H H H i 0 G(=S)UGH 3 H 2-S =0 ) 2 F 3 ,6-F A-6156 H H H H D 0(= S)UGH 3 H 2-S(= ) 20F 3 ,b- e 0 A-6157 H H H H 0 0(= S)UGH 3 H 2-S(=0) 2 0F 3 ,6-M e 0 A-6158 H H H H i0 0(= S)UGH 3 H 2-(cycbpropy1thb),b-F 0 A-6159 H H H H D 0(= S)UGH 3 H 2-(cycbpropy1thb),6-F 0 A-6160 H H H H 0 (= S)UGH 3 H 2-(cycbpropy thio),b-M e 0 A-6161 H H H H iF 0 G(=S)UGH 3 H 2-(cycbpropy thio),6-M e 0 A-6162 H H H H f 0 C(=S)UGH 3 H 2-(= U)Me,b-F 0 A-6163 H H H H if 0 G(=S)UGH 3 H 2-'(=0)Me,6-F 0 A-6164 H H H H f G(=S)UGH 3 H 2-(= U)M e,b-M e 0 A-6165 H H H H D C (=S)UGH 3 H 2-(= 0)M e,6 -Me 0 A-6166 H H H H 0 0(= S)UGH 3 H 2-GH 2UH,b-F 0 A-6167 H H H H E0 f G(=S)UGH 3 H 2-CH2UN,6-H 0 A-6168 H H H H f G(=)UGH 3 H 2-CH 20H,b-M e A-6169 H H H H D 0(= S)0H 3 H 2-0H 20H,6 -Me 0 A-6170 H H H H F0 G 0=)UH 3 H 2-GH 20H 3,4-F 0 A-6171 H H H H D- (= S)0H 3 H 2-0H 20H 3 ,b-4 0 A-6172 H H H H Hf 0(=S)GH 3 H 2-0H 20H 3 ,6-F 0 A-6173 H H H H 0 H(= S)UGH3 H 2-OH20H 3,4-Me 0 A-6174 H H H H 0 0(= S)UGH 3 H 2-OH 2 0H 3 ,b-Me 0 A-6175 H H H H 0 0(= S)UGH 3 H 2-OH 2 0H 3 ,6-Me 0 A-6176 H H H H Ef 0(=S)UGH 3 H 2-0(= 0)GH 3,b-F A-6177 H H H H 0(=S)UGH 3 H 2-0(= 0)GH 3,6 A-6178 H H H H G(=)UGH 3 H 2-00(=0)GH 3 ,b-M e 0 A-6179 H H H H i 0 (=S)GH 3 H 2-00(=U)CH 3 ,6-M e 0 A-6180 H H H H 0 0(=S)UGH 3 H 2-OS =OUH )2 3 ,b-F 0 A-6181 H H H H 0 0(= S)UGH 3 H 2-OS =OUH )2 3 ,6-F 0 A-6182 H H H H 00 (=S)0H3 H 2-OS(= )2GH3,b-M e 0 A-6183 H H H H H 0 (= S)UGH 3 H 2-US(= 0) 2 H 3,6-M e 0 A-6184 H H H H Hi 0(= S)UGH 3 H 2-OH 2 SOH 3 ,b-4 0 A-6185 H H H H Hf 0(=C)GH 3 H 2-GH 2S0H 3 ,6-F 0 A-6186 H H H H 0T (=S)UGH 3 H 2-OH 2S0H3,b-M e 0 A-6187 H H H H C 0 G(=C)GH 3 H 2-CH 2S0H 3,6-M e 0 A-6188 H H H H f0 G =S)0UH 3 H 2AM e 2 ,b-H 0 A-6189 H H H H D 0 (= S)UGH3 H 2-NMe2,6-F 0 A-6190 H H H H 0 0(=S)UGH 3 H 2-AMe 2 b2il e 0 A-6191 H H H H D 0 (= S)UGH3 H 2-NMe2,6-M e 0 A-6192 H H H H 0 0(= S)UGH 3 H 2-ON,4-F 0 A-6193 H H H H 0 G(= S)0H 3 H 2-ONb-F 0 A-6194 H H H H H0 f 0(=)UGH3 H 2-ON,6-F 0 A-6195 H H H H G(=S)0H 3 H 2-GN,6-M e 0 A-6196 H H H H G(=)UH 3 H 2-GNS5-OM e 0 A-6197 H H H H f0 0(=)UGH 3 H 2-GN,6-OM e 0 A-6198 H H H H D 0 (= S)UGH3 H 3-GN,6-Me 0 A-6199 H H H H D0 0(= S)UGH 3 H 3-GN,6-OM e 0 A-6200 H H H H 0 0(= S)UGH 3 H 4-GN,2-M e 0 A-6201 H H H H f 0(=7)H 3 H 4-GN,2-0M e 0 A-6202 H H H H Ei0 0 (=S)UGH 3 H 2-A0 2 ,4-F A-6203 H H H H H0f 0(=)UH 3 H 2A0 2 b-F 0 A-6204 H H H H Ei0 0 (=S)UGH 3 H 2U6 -F 0 A-6205 H H H H 0 E (S)UGH 3 H 2-0 2,4-A e 0 A-6206 H H H H 0 0(=S)UH 3 H 2-0 2,5-M e 0 A-6207 H H H H ifEf 0G(=)UH3 H 2-N02,6-A e 0 A-6208 H H H H 0 C(= S)UGH 3 H 2-M e,4,b-F2 0
[0235]
[Table 110]
com pound R' R2 R R A R R' (R)m p A-6209 H H H H 0 (=S)UGH 3 H 2-M e,6-Et 0 A-6210 H H H H 0 (=S)UGH 3 H 2-cyclopropyl,6-OMe 0 A-6211 H H H H 0 (=S)UGH 3 H 2-Me,b-Et 0 A-6212 H H H H i 0 G(=S)OH 3 H 2,6-Et2 0 A-6213 H H H H f Df 0(=S)UGH 3 H 2-Et,6-F 0 A-6214 H H H H 0 0(=S)U0H 3 H 2-0H 20H 3 ,6-CI 0 A-6215 H H H H 0 0(=S)UGH 3 H 2-0H 20H 2 CH 3 ,6-CI 0 A-6216 H H H H 0 O(=S)U0H 3 H 2-CH 2 NMe 2 0 A-6217 H H H H i 0 O(=S)N (H 3) 2 H H 0 A-6218 H H H H i 0 G(=S)N (H 3) 2 H 2-F 0 A-6219 H H H H i 0 G(=S)N (H 3) 2 H 2-Cl1 A-6220 H H H H i 0 G(=S)N (H 3) 2 H 2-Br 0 A-6221 H H H H G(=S)N (GH3) 2 H 2-OH 0 A-6222 H H H H D O(=S)N (H 3) 2 H 2-M e 0 A-6223 H H H H i0 O (=S)N (H 3) 2 H 2-Et 0 A-6224 H H H H 0 ()N (H 3) 2 H 2-Pr 0 A-6225 H H H H f0 0 (=S)N(OH 3) 2 H 2-G 3 0 A-6226 H H H H D (=S)N (OH3 2 H 2-UHF 2 A-6227 H H H H f0 0(=)N(OH 3) 2 H 2-CH 2F 0
A-6228 H H H H 0 O(=S)N (H 3) 2 H 2-0F 201 0 A-6229 H H H H f0 C (=S)N (OH33 2 H 2-cycbpropyl 0 A-6230 H H H H 0 (=S)N (OH 3) 2 H 2-cyclobutyl 0 A-6231 H H H H (S)N (H 3) 2 H 2-cycbpentyl 0 A-6232 H H H H C (=S)N (H 3) 2 H 2-ethenyl 0 A-6233 H H HHiif G(S)N(H3)2 H 2-aIlyl 0 A-6234 H H H H i 0 0(=)N (H 3) 2 H 2-(prop-1-en-1-yD 0 A-6235 H H H H f 0(=)N (H3)2 H 2-(trifLloroethenyD 0 A-6236 H H H H i 0 C(=S)N (OH3) 2 H 2-UMe 0 A-6237 H H H H Df )(=S)N (OH 3) 2 H 2-OEt A-6238 H H H H 0 (=S)N (H 3) 2 H 2-OPr 0 A-6239 H H H H 0 0(S)N (H 3) 2 H 2-0 (/-Pr) 0 A-6240 H H H H 0 0(= S)N (H 3) 2 H 2-0GF 3 0 A-6241 H H H H 0 O(=S)N (H 3) 2 H 2-UGHF 2 0 A-6242 H H H H IF i0 0(=S)N (H 3) 2 H 2-(cycbpropybxy) 0 A-6243 H H H H Ff 0 (S)N (H 3) 2 H 2-(cycobbutybxy) 0 A-6244 H H H H 0 (=S)N (H 3) 2 H 2-(cycbpentybxy) 0 A-6245 H H H H 0 0(=S)N (H 3) 2 H 2-((2,2-dichbrocyclopropyI)oxy) 0 A-6246 H H H H 0 0(S)N (H 3) 2 H 2-(oxiran-2-yD A-6247 H H H H 0 ( S)N (H 3) 2 H 2-SMe 0 A-6248 H H H H 0 0(= S)N (H 3) 2 H 3-SMe 0 A-6249 H H H H 0 0(=S)N (H 3) 2 H 2-S(=0)Me 0 A-6250 H H H H f 0 (=S)N (H 3) 2 H 3-S(=0)Me 0 A-6251 H H H H 0 C G(=S)N (H 3) 2 H 2-S(=U) 2Me 0 A-6252 H H HH i i0 (S)N (H3)2 H 3-S(=U) 2Me 0 A-6253 H H H H H D G(=S)N (OH 3) 2 H 2-SGH 3 0 A-6254 H H H H G(=)N(OH 3) 2 H 3-SGH 3 0 A-6255 H H H H 0 C(=S)N(OH 3) 2 H 3-S(=O)0F 3 0 A-6256 H H H H 0 0(=S)N(H 3) 2 H 3-SOF(F 3) 2 0 A-6257 H H H H 0 ( S)NT(H 3 2 H 2-(cycbpropythb) 0 A-6258 H H H H 0 (=S)N (H 3) 2 H 2-(cycbpropylsufinyD 0 A-6259 H H H H 0 (=S)N (H 3 2 H 2-(cycbpropysufonyD 0 A-6260 H H H H H0 G()N (H 3 2 H 2-C(=U)Me 0 A-6261 H H H Hi 0 G(=S)N (OH 3) 2 H 2-H 2 G(=U)GH 3 A-6262 H H H H i0 (=S)N (OH 3) 2 H 2-GH 2C(=O)F 3 0 A-6263 H H H H i0 C (=S)N (H 3) 2 H 2-CH 2 UH 0 A-6264 H H HH f 0(=S)N(OH 3) 2 H 2-0H 2 UGH 3 0
A-626b H H H H F 0 A(=S)N (OH 3) 2 H 2-0H 20H 2 CH 3 0
[0236]
[Table 111]
com pound R' R-2 R A R R' (R)m p A-6266 H H H H 0 0(=S)N (H 3)2 H 2-GH 2SOH 3 0 A-6267 H H H H 0 0(=S)N (H 3)2 H 2-GH 2S(=0)CH 3 0 A-6268 H H H H 0 C (=S)N (H 3) 2 H 2-GH 2S(=0G) 2 H3 A-6269 H H H H 0 (=S)N (H 3)2 H 2-(benzybxy) 0 A-6270 H H H H D 0 O(=S)N (OH32 H 2-NH 2 A-6271 H H H H 0 O(=S)N (H 3) 2 H 2-NHMe 0 A-6272 H H H H - O(=S)N (H 3) 2 H 2-N(e )20 A-6273 H H H H 0 0(S)N (H 3) 2 H 2-(1,3-dbxolan-2-yD 0 A-6274 H H H H i 0 0(=S)N (H 3) 2 H 2-(1,3-dbxan-2-yD A-6275 H H H H F G (S)N (H 3) 2 H 2-(1/-m idazol-2-yD A-6276 H H H H 0 (=S)N (H 3) 2 H 2-(thiazol-2-yl) 0 A-6277 H H H H D (S)N (H 3) 2 H 2-(oxazol-2-yD A-6278 H H H H 0 G(=S)N (H 3) 2 H 2-GH=N0H 0 A-6279 H H H H D ( S)N (H 3) 2 H 2-OH= NOM e 0 A-6280 H H H H 0 0(S)N (H 3) 2 H 2-(4,b-dihydro-3-isoxazolyl) 0 A-6281 H H H H H 0 G(=)N (H 3) 2 H 2-N 0 A-6282 H H H H 0 0(=S)N(OH 3) 2 H 2-NO 2 0 A-6283 H H H H H 0 c(=S)N (OH3) 2 H 2-F,6-GI 0 A-6284 H H H H H0 (=S)N(H 3) 2 H 2-F,6-M e 0 A-6285 H H H H 0 C(=S)N(H 3) 2 H 3-F,6-M e 0 A-6286 H H H H f0 C (=S)N (OH3 2 H 4-F,2-M e 0 A-6287 H H H H f C (=S)N (OH 3)2 H 2-F,6-UMe 0 A-6288 H H H H (S)N (H 3) 2 H 3-F,6-0Me 0 A-6289 H H H H 0 C (=S)N (H 3) 2 H 2,6-C12 0 A-6290 H H H H C G(=S)N (H 3) 2 H 2-GI,6-M e 0 A-6291 H H H H 0 G(=)N (H 3) 2 H 3-GI,6-M e 0 A-6292 H H H H H (=)N(H 3 2 H 4-GI,2-M e 0 A-6293 H H H H 0 C(=S)N(OH 3) 2 H 2-CIb-GF 3 0 A-6294 H H H H 0 0(=S)N (OH3) 2 H 2-CI,6-GF 3 0 A-629b H H H H 0 (=S)N (H 3) 2 H 2-GI,6-0Me 0 A-6296 H H H H 0 C(S)N (H 3) 2 H 3-GI,6-0Me 0 A-6297 H H H H H 0 C(S)N (H 3) 2 H 4-GI,2-0Me 0 A-6298 H H H H f C (=S)N (H 3) 2 H 2,4-M e 2 0 A-6299 H H H H F CG(=S)N (H 3) 2 H Z,b-M e 2 0 A-6300 H H H H f D (=S)N (H 3) 2 H 2,6-M e 2 0 A-6301 H H H H 0 (S)N (H 3) 2 H 2-M e,4-GF 3 0 A-6302 H H H H f0 G(=)N (H 3) 2 H 2-M e,b-C 3 0 A-6303 ifiHifiHfD (=S)N(OH 3) 2 H 2-M e,6-H 3 A-6304 H H H H D0 (S)N(H3) H 2- e,4-Me 0 A-630b H H H H D0 (=S)N(H3)2 H 2-M e,b-0Me 0 A-6306 H H H H ifIN (S)N (H H 2-M e,6-OMe 0 A -6 30/6 H H H H 3H D C(=S)N (GH3)2 H 3-M e,6-OM e 0 A-6307 H H H H 0 (=S)N (H 3) 2 H 3-M e,6-OMe 0 A-6308 ifi ifi if 0 C(S)N (H 3 )2 H 4-M e,2-OM e 0 A-6309 H H H H 0 F (=S)N (H)32 H 2,b-UMe2 0 A-6310 H H H H 0 (=S)N (OH 3) 2 H 2,6-UMe 2 0
A-6311 H H H H 0 G(=S)N (H 3) 2 H 2-OMe,6-GF 3 0 A-6312 H H H H 0 C(=S)N (H 3) 2 H 2-CHF 2,b-F 0 A-6313 H H H H 0 C(=S)N (H 3) 2 H 2-CHF 2,6-F 0 A-6314 H H H H 0 C(S)N (H 32 H 2-CHF 2,b-M e 0 A-631b H H H H 0 (=S)N (H 3) 2 H 2-CHF 2,6-MFe 0 A-6316 H H H H 0 0(S)N (H 3) 2 H 2-cycbpropylb-F 0 A-6317 H H H H 0 (=S)N (H 3) 2 H 2-cycbpropyl,6-F 0 A-6318 H H H H 0 G( S)N (OH 3) 2 H 2-cyclopropylb-Me 0 A-6319 H H H H 0 D G(=S)N (H3)2 H 2-cyclopropyl,6-Me 0 A-6320 H H H H 0 0(=S)N (H 3) 2 H 2-ethenyl,6-F 0 A-6321 H H H H 0 (=S)N (H 3) 2 H 2-ethenyl,6-Me 0 A-6322 H F FIFH 10 (=S)N (OH 3) 2 H 2-U tt,b-F
[0237]
[Table 112]
com pound R' R R RR A R R' (R)m P A-6323 i H H H H 0 0(=S)N (H3)2 H 2-OEt,6-F 0 A-6324 H H H H F C(=S)N (0H31 2 H 2-UEt,b-CI 0 A-6325 H H H H Hi D (=S)N (0H31 2 H 2-OEt,6-CI 0 A-6326 H H H H i 0 G(=S)N (H 3) 2 H 2-UEt,b-Me 0 A-6327 H H H H D O(=S)N (H 3) 2 H 2-OEt,6-M e 0 A-6328 H H H H 0 C(=S)N (H 3) 2 H 2-UGHF 2,b-F 0 A-6329 H H H H - C(=S)N (H 3) 2 H 2-UGHF 2,6-F 0 A-6330 H H H H 0 O(S)N (H 3) 2 H 2-OHF 2 ,b-M e 0 A-6331 H H H H i 0 O(=S)N (H 3) 2 H 2-UGHF 2 ,6 -M e 0 A-6332 H H H H i 0 (=S)N (H 3) 2 H 2-(cycbpropyloxy),b-F 0 A-6333 H H H H i 0 (=S)N (H 3) 2 H 2-(cyclopropyloxy),6-F 0 A-6334 H H H H i 0 0(S)N (H 3) 2 H 2-(cyclopropybxy),b-Me 0 A-6335 H H H H 0 0(S)N (H 3) 2 H 2-(cyclopropyloxy),6-M e 0 A-6336 H H H H D0 (S)N(H3)2 H 2-SMe,b-F 0 A-6337 H H H H 0 C(S)N (H 3) 2 H 2-SMe,6-F 0 A-6338 H H H H 0 G(=)N (H 3) 2 H 2-SMe,b-Me 0 A-6339 H H H H (=)N(H 3) 2 H 2-SMe,6-M e 0 A-6340 H H H H 0 0(=S)N (OH3) 2 H 2-S(=0)Me,b-F 0 A-6341 H H H H H0 0()N (H 3 2 H 2-S(=U)Me,6-F 0 A-6342 H H H H 0 O(=S)N (H 3) 2 H 2-S(=0)Me,b-M e 0 A-6343 H H H H 0 C(=S)N (H 3) 2 H 2-S(=U)Me,6-M e 0 A-6344 H H H H 0 0 (=S)N (OH 3) 2 H 2-S (=) 2M e,b-F 0 A-6345 H H H H 0 (=S)N (H 3) 2 H 2-S(=U) 2 Me,6-F 0 A-6346 H H H H 0 O(=S)N (H 3) 2 H 2-S(=U) 2 Me,b-Me 0 A-6347 H H H H C (=S)N (H 3) 2 H 2-St=0) 2 Me,6-M e 0 A-6348 H H H HIF 0 0(=)N (H 3) 2 H 2-SGH 3 ,b-H 0 A-6349 H H H H 0 0(=)N (H 3) 2 H 2-SGH 3 ,6-1 0 A-6350 H H H H i 0 0(=S)N (H 3 2 H 2-SF 3 ,b-Me A-6351 H H H H 0 (=S)N (OH33 2 H 2-SCF 3 ,6-Me 0 A-6352 H H H H 0 0(=S)N (H 3) 2 H 2-S(=O)CF 3 ,b-F 0 A-6353 H H H H i0 0(=S)N (H 3) 2 H 2-S(=U) 3 ,6- -F 0 A-6354 H H H H 0 0(=S)N (H 3) 2 H 2-S(=U)OC 3,b-M e 0 A-63b55 H H H H 0 0 C(=S)N (H3)2 H 2-S(=U)CF 3,6-M e 0 A-6356 H H H H i 0 0(=S)N (H 3) 2 H 2-S(=0) 20F 3 ,b-H A-63/57 H H H H i 0 (=S)N (H 3) 2 H 2-S(=U) 0F 3 ,6-F 2 0 A-6358 H H H H f 0(S)N (H 3) 2 H 2-St=0) 2 CF 3 ,5-M e 0 A-6359 H H H H G(=)N(OH 3) 2 H Z-S(=U) OF 2 3 ,6-e A-6360 H H H H 0 0(S)N (H 3) 2 H 2-(cycobpropylthio),b-F 0 A-6361 H H H H 0 0(S)N (H 3) 2 H 2-(cycobpropylthio),6-F 0 A-6362 H H H H 0 (=S)N (H 3) 2 H 2-(cycobpropythio),b-Me 0 A-6363 H H H H 0 0(S)N (H 3) 2 H 2-(cycobpropylthio),6-Me 0 A-6364 H H H H 0 C(S)N (H 3) 2 H 2-C(=0)Me,b-F 0 A-6365 H H H H 0 (=S)N (H 3) 2 H 2-C(=U)Me,6-F 0 A-6366 H H H H 7 O G(=7)N (H3)2 H 2-C(=O)Me,b-M e 0 A-6367 H H H H Ff 0 G(=)N (OH 3) 2 H 2-C(=O)Me,6-M e 0 A-6368 H H H H i G(=S)N (H 3) 2 H 2-CH 2UHb-H A-6369 H H H H Df 0(=S)N (H 3) 2 H 2-CH 2OH,6-F 0 A-6370 H H H H 0 0(=S)N (H 3) 2 H 2-OH 2OH,b-Me 0 A-6371 H H H H D 0(=S)N (H 3) 2 H 2-OH 2OH,6-M e 0 A-6372 H H H H 0 0G(=S)N (H 3)2 H 2-GH20H3,4-F 0 A-6373 H H H H i 0 (=S)N (H 3) 2 H 2-0H 20H 3 ,b-F 0 A-6374 H H H H i 0 (=S)N (H 3) 2 H 2-GH 20H 3,6-F 0 A-6375 H H H H 0G(=S)N (OH3)2 H 2-CH 20H3,4-M e 0 A-6376 H H H H Ff 0 (=S)N (H 3) 2 H 2-CH 2OGH 3 ,b-M e 0 A-6377 H H H H 0 (=S)N (H 3) 2 H 2-CH 2OGH 3 ,6-Me 0 A-6378 H H H H Hf 0G(=S)N (OH 3) 2 H 2-UG(=U)GH 3 ,b-F A-6379 H HF FH H (=S)N (OH 3)2 H 2-0(=U)H 3,6-F 0
[0238]
[Table 113]
com pound R' R2 R R A R R' (R)m p A-6380 H H H H D0 (S)N (H 3)2 H 2-0(=U)CH3,b-M e 0 A-6381 H H H H 0 (=S)N (H 3) 2 H 2-0(=U)CH 3 ,6-M e 0 A-6382 H H H H 0 (=S)N (H 3) 2 H 2-OS(=U) 2 CH 3 ,b 0 A-6383 H H H H i 0 0(=S)N (H 3) 2 H 2-OS(=U) 0H 3 ,6-F 2 0 A-6384 H H H H D C(=S)N (H 3) 2 H 2-US(=U) 2CH 3,b-M e 0 A-6385 H H H H 0 O(=S)N (H 3) 2 H 2-US(=U) 2CH 3,6-M e 0 A-6386 H H H H 0 0(=S)N (H 3) 2 H 2-CH 2 SOH 3 ,b- 0 A-6387 H H H H 0 0(=S)N (H 3) 2 H 2-CH 2 SOH 3 ,6-F 0 A-6388 H H H H i 0 0(=S)N (H 3) 2 H 2-CH 2SOH 3,b-Me 0 A-6389 H H H H i 0 (=S)N (H 3) 2 H 2-CH 2 S0H 3,6-M- e A-6390 H H H H i 0 0(=S)N (H 3) 2 H 2-NMe 2 ,b-H 0 A-6391 H H H H i 0 0(=S)N (H 3) 2 H 2-NMe 2 ,6-F 0 A-6392 H H H H G(=S)N (H 3) 2 H 2-NMe 2 ,b-MAe 0 A-6393 H H H H D C(S)N (H 3) 2 H 2-NMe 2 ,6-M e 0 A-6394 H H H H i0 0 (=S)N (H 3) 2 H 2-ON,4-F 0 A-6395 H H H H f0 G(=)N (H 3) 2 H 2-CN,b-F 0 A-6396 H H H H (=)N(H 3) 2 H 2-CN,6-F 0 A-6397 H H H H f0 (=S)N (OH3) 2 H 2-CN,6-Me 0 A-6398 H H H H f0 G()N (H 3 2 H 2-CN,b-OMe 0 A-6399 H H H H 0 (=S)N (H 3) 2 H 2-CN,6-OMe 0 A-6400 H H H H f0 C (=S)N (OH33 2 H 3-CN,6-Me 0 A-6401 H H H H 0 (=S)N (OH 3) 2 H 3-CN,6-OMe 0 A-6402 H H H H (=S)N (H 3) 2 H 4-CN,2-Me 0 A-6403 H H H H 0 (=S)N (H 3) 2 H 4-CN,2-OMe 0 A-6404 H H H H 0G(=S)N (H3)2H 2-N02,4--F 0 A-6405 H H H H 0 0G(=S)N (H3)2H 2-N02,b--F 0 A-6406 H H H H f0 0(=)N (H 3) 2 H 2-N0 2 ,6- 0 A-6407 H H H H Hi0 0(=S)N (OH 3) 2 H 2-NU 2,4-MiAe 0 A-6408 H H H H 00 (=S)N (H 3 32 H 2-NU 2,b-Me 0 A-6409 H H H H 0 0(S)N (H 3) 2 H 2-NU 2,6-Me 0 A-6410 H H H H 00(=S)N (H3)2H 2-Me,4,b-F2 0 A-6411 H H H H 0 C(S)N (H 3) 2 H 2-M e,6-Et 0 A-6412 H H H H 0D G(=S)N (H 3)2 H 2-cyclopropyl,6-OMe 0 A-6413 H H H H 0 G(=)N (H 3) 2 H 2-M e,b-Et 0 A-6414 H H H H 0D C(=S)N (OH3)2H 2,6-Et2 0 A-6415 H H H H Hi0 G(=)N(OH 3) 2 H 2-Et,6-F 0 A-6416 H HH f H H 0-G(=)N(OH 3)2 H 2-GH20H3,6-CI F A-6417 H H H H Df 0(=S)N (OH 3) 2 H 2-GH 20H 2CH 3 ,6-CI 0 A-6418 H H H H 0 C(S)N (H 3) 2 H 2-CH 2 NMe 2 0 A-6419 H H H H 0 S(= ) 2CH 3 H H 0 A-6420 H H H H 0 S(= ) 2CH 3 H 2-F A-6421 H H H H H D S(=U) 2CH 3 H 2-Cl 0 A-6422 H H H H F 0 0t=U) 20H 3 H 2-Br 0 A-6423 H H H H 0 =U) 20 3 H 2-OH 0 A-6424 H H H H f0 t) 20H 3 H 2-M e 0 A-6425 H H H H f0 S(=U) 20H 3 H 2-Et 0 A-6426 H H H H D S(=U) 2CH 3 H 2-Pr 0 A-6427 H H H H D S(=U) 2CH 3 H 2-CF 3 0 A-6428 H H H H D S(= ) 2CH 3 H 2-UHF 2 0 A-6429 H H H H H =U) 20H 3 H Z-GH 2 A-6430 H H H H H0 S(=U) 2CH 3 H 2-CF 2OI 0 A-6431 H H H H H 0 S(0=) 20H 3 H 2-cycbpropyl 0 A-6432 H H H H H F S 0) 20H 3 H 2-cyclobutyl 0 A-6433 H H H Hf S(0) 2CH 3 H 2-cyclopentyl 0 A-6434 H H H HF S(=U) 2CH 3 H 2-ethenyl 0 A-6435 H H H H f0 S 0) 20H 3 H 2-alyl 0 A-6436 H H H H F S(=U) 2CH 3 H 2-(prop-1-en-1-yD 0
[0239]
[Table 114]
com pound R' R-2 R A R R' (R)m p A-643/ H H H H D if S(=U)2CH3 H 2-(trf ioroethenyD 0 A-6438 H H H H F S(=0) 2CH 3 H 2-UMe 0 A-6439 H H H H H D S(=0) 2CH 3 H 2-OEt A-6440 H H H H H 0 S=U) 20H 3 H 2-UPr 0 A-6441 H H H H D S(=0) 2CH 3 H 2-0 (/-Pr) 0 A-6442 H H H H 0 S(=0) 2CH 3 H 2-0GF 0 A-6443 H H H H D f S(=0) 2CH3 H 2-CHF2 0
A-6444 H H H H 0 S(=0 ) 2CH 3 H 2-(cycbpropy bxy) 0 A-6445 H H H H H i 0 S 0)2CH 3 H 2-(cycobbutybxy) 0 A-6446 H H H H i 0 S(=U) 2 003 H 2-(cycbpentybxy) 0 A-6447 H H H H Hi 0 S( ) 20H 3 H 2-((2,2-dichbrocycbpropyI)oxy) 0 A-6448 H H H H f 0 S(=U) 20H 3 H 2-(oxiran-2-y) 0 A-6449 H H H H S(=U) 20H 3 H 2-SMe 0 A-6450 H H H H D S(=0) 2CH 3 H 3-SMe 0 A-6451 H H H H 0 S(=0) 2CH 3 H 2-S(=0)Me 0 A-6452 H H H H H =U) 20H 3 H 3-S(=0)Me 0 A-6453 H H H H 0 ST=) 20 3 H 2-S(=U) 2Me 0 A-6454 H H H H 0 S(=0)2CH 3 H 3-S (=0)2M e 0 A-6455 H H H H 0 T=) 20H 3 H 2-SGH3 A-6456 H H H H 0 S(= 0) 2CH 3 H 3-SCG3 0 A-6457 H H H H H 0 S(=U) 2CH 3 H 3-S(=0)GH3 0 A-6458 H H H H H 0 S(=0) 2CH 3 H 3-SCF(0F3 2 0 A-6459 H H H H 0 S(=0) 2CH 3 H 2-(cycbpropythio) 0 A-6460 H H H H 0 S(=0) 2CH 3 H 2-(cycbpropysufinyD 0 A-6461 H H H H H =U) 20H 3 H 2-(cycbpropylsulfony 0 A-6462 H H iH (H =U) 20H 3 H 2-C(=0)Me 0 A-6463 H H H H f0 S(=U) 20H 3 H 2-GH 2G(=O)GH 3 0 A-6464 H H H H i 0 S(=0) 2CH 3 H 2-GH 20(=U)0F 3 0 A-6465 H H H H D S(=0) 2CH 3 H 2-CH 2 UH 0 A-6466 H H H H 0 S(=0) 2CH 3 H 2-0H 20H 3 0
A-6467 H H H H f Di S(=0) 2CH 3 H 2-0H 20H 2CH 3 0
A-6468 H H H H 0 S(=0) 2CH 3 H 2-CH 2SCH 3 0
A-6469 H H H H H i S(=0) 2CH3 H 2-CH 2S(=0)CH3 0 A-6470 H H H H f0 S( =) 20H 3 H 2-CH 2S(=U) 0H 2 3 0 A-6471 H H HH ii D S(=0)2CH3 H 2-(benzybxy) F A-6472 H H H H H S t=)2CH3 H 2-NH 2 A-6473 H H H H S( =) 20H 3 H 2-NHMe 0 A-6474 H H H H 0 S(=0) 2CH 3 H 2-N(Me)2 A-6475 H H H H 0 S(=0) 2CH 3 H 2-(1,3-dioxolan-2-yD 0 A-6476 H H H H 0 S(=0) 2CH 3 H 2-(1,3-dioxan-2-yD 0 A-6477 H H H H 0 S(=0) 2CH 3 H 2-(1/-m idazol-2-yD 0 A-6478 H H H H 0 S(=0) 2CH 3 H 2-(thiazol-2-yl) 0 A-6479 H H H HF S(=) 20H 3 H 2-(oxazol-2-yD A-6480 H H H H H S (=O) 20H 3 H 2-CH=NUH 0 A-6481 H H H H Ff D (=U) 20H 3 H 2-CH=NOMe 0 A-6482 H H H H S Ot=U) 20H 3 H 2-(4,b-dihydro-3-soxazoyD 0 A-6483 H H H H F S(= 0) 2CH 3 H 2-N 0 A-6484 H H H IH DI S(=0) 2CH 3 H 2-NO 2 0
A-6485 H H H H DRf S(=0) 2CH 3 H 2-F,6-C1 0 A-6486 H H H H 5T=U) 20H 3 S(D H 2-F,6-Me 0 A-6487 H H H H Ei0 S=0)2CH3 H 3-F,6-i e 0 A-6488 H H H H S(S=U)20H3 H 4-F,2-Me 0 A-6489 H H H H 0 S (=) 20H 3 H 2-F,6-OMe 0 A-6490 H H H H 0 S(=0) 2CH 3 H 3-F,6-OMe 0 A-6491 H H H H H 0 S(=O) 2CH 3 H 2,6-C 1 0 A-6492 H H H H H (S=U)20H3 H 2-GI,6-Me 0 A-6493 H H H H 0 S(=O) 2CH 3 H 3-GI,6-M e 0
[0240]
[Table 115]
com pound ' R2 RR R A R R' (R)m P A-6494 i H HH H D S(=0)2CH3 H 4-C,2-Me 0 A-6495 H H H H Hf S(=U) 2CH 3 H 2-CIb-CF 3 0 A-6496 H H H H HD S (=U) 2CH 3 H 2-C,6-CF 3 0 A-6497 H H H H f0 S(=) 2 03 H 2-C,6-UMe 0 A-6498 H H H H D S(=U) 2CH 3 H 3-C,6-0Me 0 A-6499 H H H H D S (=U) 2CH 3 H 4-C,2-0Me 0 A-6b00 H H H H D f S(=U)2CH3 H 2,4-M2e 0 A-6b01 H H H H 0 S(=U) 2CH 3 H 2,b-M e 2 0 A-6b02 H H H H i 0 S(=U) 2CH 3 H 2,6-M e 2 0 A-6b03 H H H H i 0 S(=U) 2 03 H 2-M e,4-GF 3 0 A-6b04 H H H H i 0 S(=U) 2 03 H 2-M e,b-GH 3 0 A-6bb H H H H f 0 S(=U) 2 03 H 2-M e,6-GF 3 0 A-6b06 H H H H S(=U) 2 03 H 2-MAe,4-UMe 0 A-6b07 H H H H D S(=U) 2CH 3 H 2-M e,b-0Me 0 A-6b08 H H H H 0 S(=U) 2CH 3 H 2-M e,6-0Me 0 A-6b09 H H H H H =U) 20H 3 H 3-M e,6-UMe 0 A-6b10 H H H H S =U) 2 03 H 4-Me,2-UMe 0 A-6b11 H H H H H D S(=O) 2CH 3 H 2,b-UMe 2 0 A-6b12 H H H H 0 T=) 20H 3 H 2,6-UMe 2 0
A-6b13 H H H H 0 S(=U) 2CH 3 H 2-UMe,6-F 3 0 A-6b14 H H H H H 0 S(=U) 2CH 3 H 2-CHF 2,b-F 0 A-6blb H H H H H S(=U) 2CH 3 H 2-CHF 2,6-F 0 A-6b16 H H H H S(=U) 2CH 3 H 2-CHF 2,b-M e 0 A-6b1 7 H H H H ii S(=U)2CH3 H 2-CHF2,6-M e 0 A-6b18 H H H H if 0 (=U) 20H 3 H 2-cycbpropyLb-F 0 A-6b19 H H H H f0 S( =) 20H 3 H 2-cycbpropyL,6-F 0 A-6b20 H H H H 5(=) 20H 3 H 2-cyclopropyLb-Me 0 A-6b21 H H H H ifD S(=U) 2CH 3 H 2-cyclopropyL,6-Me 0 A-6b22 H H H H D S(=U) 2CH 3 H 2-ethenyl,6-F 0 A-6b23 H H H H S (=O ) 2CH 3 H 2-ethenyl,6- e 0 A-6b24 H H H H D S(=U) 2CH 3 H 2-OEt,b-F A-6b2b H H H H H S (=0) 2CH 3 H 2-OEt,6-F 0 A-6b26 H H H H H 0 S(=0) 2CH 3 H 2-UEt,b-CI 0 A-6b27 H H H HFi0 (=U) 20H 3 H 2-UEt,6-CI 1 A-6b28 H H H H Ff S(=0) 2CH 3 H 2-OEt,b-M e 0 A-6b29 H H H H D S(=U) 20H 3 H 2-OEt,6-M e 0 A-6b30 H H H H H f 5(=U) 2 03 H 2-CHH2,b-F A-6b31 H H H H D0 S (=0) 2CH 3 H 2-CHF 2,6-F 0 A-6b32 H H H H 0 S(=0) 2CH 3 H 2-OCHF 2,b-M e 0 A-6b33 H H H H DIi S(=U) 2CH 3 H 2-CHF 2 ,6-MAe 0 A-6b34 H H H H 0 S(=0) 2CH 3 H 2-(cycobpropyloxy),b-F 0 A-6b3b H H H H 0 S(=0) 2CH 3 H 2-(cycobpropyloxy),6-F 0 A-6b36 H H H H 0 5=U) 2CH 3 H 2-(cyclopropyoxy),b-M e 0 A-6b37 H H H H i f f 5( )2CH3 H 2-(cyclopropybxy),6-M e 0 A-6b38 H H H H S =) 2 CH3 H 2-SMe,b-F 0 A-6b39 H H H H 5=U) 2 CH3 H 2-SMe,6-F 0 A-6b40 H H H H D S(=0) 2CH 3 H 2-SMe,b-Me 0 A-6b41 H H H H D S(=0) 2CH 3 H 2-SMe,6-Me 0 A-6b42 H H H H D S(= 0) 2CH 3 H 2-S(=0)Me,b-F 0 A-6b43 H H H H f0 S( =) 2CH 3 H 2-S(=0)Me,6-F 0 A-6b44 H H H H D S (=0) 2CH 3 H 2-S(=0)Me,b-Me 0 A-6b4b H H H H ii f 5(0) 2CH3 H 2-S(=0)Me,6-Me 0 A-6b46 H H H H i if 5=U) 2CH3 H 2-S (=) 2M e,b-F A-6b47 H H H H 0 S(0) 2CH 3 H 2-S(=0) 2Me,6-F 0 A-6b48 H H H H 0 S(=0) 2CH 3 H 2-S(=0) 2 Me,b-M e 0 A-6b49 H H H H i f 0 S(=) 2CH3 H 2-S(=U) 2Me,6-M e 0 A-6bb0 H H H Hi 5 (=U) 2CH 3 H 2-SCF 3 ,b-F 0
[0241]
[Table 116]
com pound ' R2 RR R A R R' (R)m P A-6 55Tl H H H H 0 S(=0) 2CH 3 H 2-SGF 3 ,6-F 0 A-6552 H H H H F S(=0) 2CH 3 H 2-S0F 3 ,b-Me 0 A-6553 H H H H F S(=0) 2CH 3 H 2-S0F 3 ,6-Me 0 A-6554 H H H H i 0 S(=U) 2 03 H 2-S(=U)GH 3 ,b-H 0 A-6555 H H Hf H Di S(=0) CH 2 3 H 2-S(=U)0F 3 ,6-F 0 A-6556 H H H H f Di S(=0) 2CH 3 H 2-S(=U)0F 3 ,b-Me 0 A-6557 H H H H - Dii S(=0) 2CH 3 H 2-S(=U)0F 3 ,6-M e 0 A-6558 H H H H 0 S(=0) 2CH 3 H 2-S(=0) 20%3,b-F 0 A-6559 H H H H i 0 S(=0) 2CH 3 H 2-S(=0) 20F 3 ,6-F 0 A-6560 H H H H i 0 S(=U) 2 03 H 2-S(=U) 2CF 3,b-Me 0 A-6561 H H H H i 0 S(=U) 2 03 H 2-St=U) 2CF 3 ,6-M e 0 A-6562 H H H H if 0 St) 20H 3 H 2-(cycobpropylthb),b-F 0 A-6563 H H H H 0 S@O=) 20H 3 H 2-(cycobpropylthlo),6-F 0 A-6564 H H H H 0 S(=0) 2CH 3 H 2-(cycbpropylthio),b-Me 0 A-6565 H H H H 0 S(=0) 2CH 3 H 2-(cycbpropylthio),6-Me 0 A-6566 H H H H H =U) 20H 3 H 2-(=0)Me,b-F 0 A-6567 H H H H i 0 S(=U) 20H 3 H 2--(=0)Me,6-F 0 A-6568 H H H H 0D S(=0) 2CH 3 H 2-G(=0)Me,b-M e 0 A-6569 H H H H H0 7=) 2 0H 3 H 2-G(=U)Me,6-M e 0 A-6570 H H H H 0 S(=0) 2CH 3 H 2-OH 2UHb-F 0 A-6571 H H H H H 0 S(=0) 2CH 3 H 2-GH 2UH,6-F 0 A-6572 H H H H i f S(=0) 2CH3 H 2-0H 20H,b-M e 0 A-6573 H H H H S(=0) 2CH 3 H 2-0H 20H,6-M e 0 A-6574 H H H H Hf S(=0) 2CH 3 H 2-GH 20H 3 ,4-F 0 A-6575 H H H H S(=) 2 03 H 2-GH 2 0H 3,b-F A-6576 H H H H F S =U) 2 03 H 2-GH 2 0H 3,6-F 0 A-6577 H H H H if0 )203 H Z-G 2UGH3,4-Me A-6578 H H H H i 0 S(=0) 2CH 3 H 2-GH 20H 3 ,b-Me Y A-6579 H H H H 0 S(=0) 2CH 3 H 2-GH 20H 3 ,6-Me 0 A-6580 H H H H 0 S(=0) 2 CH 3 H 2-00(=U)CH 3 ,b-F 0 A-6581 H H H H 0 S(=0) 2 CH 3 H 2-00(=0)CH 3 ,6-F 0 A-6582 H H H H 0 S(=0) 2 CH 3 H 2-0(=0)CH 3,b-Me 0 A-6583 H H HH i i S(=0) 2CH3 H 2-0(=0)CH 3,6-M e 0 A-6584 H H H H F S =U) 2 03 H 2-OS=U) 2 03,b-H 0 A-6585 H H H Hf S(=0) 2CH 3 H 2-OS(=0) 2 CH 3 ,6-F 0 A-6586 H H H H D S(=U) 20H 3 H 2-USt=U) 2CH 3,5-M e 0 A-6587 H H H H Ff0 S =) 20H 3 H 2-OS=U) 2CH 3,6-M e 0 A-6588 H H H H 0 S(=0) 2CH 3 H 2-GH 2 S0H 3 ,b-4 F A-6589 H H H H 0 S(=0) 2CH 3 H 2-GH 2 S0H 3 ,6-F 0 A-6590 H H H H 0 S(=0) 2CH 3 H 2-GH 2SCH 3,b-Me 0 A-6591 H H H H 0 S(=0) 2CH 3 H 2-GH 2SCH 3,6-Me 0 A-6592 H H HHii D S(=0) 2CH3 H 2-NMe2,b-F W A-6593 H H H H 0 S( =) 0H 3 2 H 2-NMe 2 ,6- 0 A-6594 H H H H H 0 S=U) 2 0H 3 H 2-NMe 2 ,b-M e 0 A-6595 H H H H f0 St=) 20H 3 H 2-NMe 2 ,6-M e 0 A-6596 H H H H 5(=U) 2 03 H 2-ON,4-F 0 A-6597 H H H H 0 S(=U) 2CH 3 H 2-GN,b-F 0 A-6598 H H H H DIi S(=0) 2 CH3 H 2-ON,6-F 0 A-6599 H H H H 0 S(=0) 2 CH 3 H 2-GN,6-M e 0 A-6600 H H H H H 0 S(=U) 20H 3 H 2-GN,b-OMe 0 A-6601 H H H H 0 S(=0) 2CH 3 H 2-GN,6-OMe 0 A-6602 H H H H H =U) 20H 3 H 3-GN,6-M e 0 A-6603 H H H H H 0 ) 20 3 H 3-GN,6-OMe 0 A-6604 H H H H 0 S(=0) 2 CH 3 H 4-GN,2-M e 0 A-6605 H H H H 0 S(=0) 2 CH 3 H 4-ON,2-OMe 0 A-6606 H H H H5=U) 2 003 H 2-N0 2 ,4-F 0 A-660/ H IH IH H f S(=U) 20H 3 H 2-N0 2 ,b-F
[0242]
[Table 117]
com pound ' R2 RR R A R R' (R)m P A-6608 H H H H D S (=0) 2CH 3 H 2-N0 2 ,6-4 0 A-6609 H H H H S (=) 2 CH 3 H 2-N0 2,4-M e 0 A-6610 H H H H D S (=) 2CH 3 H 2-N0 2,b-M e 0 A-6611 H H H H if 0 S =U) OH 2 3 H 2-NU 2,6-M e 0 A-6612 H H H H D S(=0) 2CH 3 H 2-M e,4,b-F 2 0 A-6613 H H H H 0 S(=0) 2CH 3 H 2-M e,6-Et 0 A-6614 H H H H S (=) 2CH 3 H 2-cyclopropyl,6-OM e 0 A-6615 H H H Di H f S(=0) 2CH 3 H 2-M e,b-Et 0 A-6616 H HH f H S (=0) 2CH 3 H 2,6-Et2 0 A-661 7 H H H H iF H 0 (=) OH 3 2 H 2-Et,6-F F A-6618 H HH if 0 H S =U) OH 2 3 H 2-CH 20H 3 ,6-C 1 A-6619 H HH if H 0 S(=U) OH 3 2 H 2-CH 20H 2 H3,6-C 10 A-6620 H HH H S(=U) OH 2 3 H 2-CH 2 NMe 2 0 A-6621 H H H H D S(=0) 2 N(OH3 2 H H 0 A-6622 H H H H 0 S(=0) 2 N(H 3) 2 H 2-F 0 A-6623 H H H H f0 S =U) 2 N (H 3) 2 H 2-Cl 0 A-662 Hf4 H H H i 0 S(=U) 2N(OH 3) 2 H 2-Br 0 A-6625 H H H H 0 S(=U) 2 N(H 3) 2 H 2-OH 0 A-6626 H H H H f0 =U) 2 N (H 3) 2 H 2-M e 0 A-6627 H H H H 0 S(=0) 2 N(H 3) 2 H 2-Et 0 A-6628 H H H H H 0 S(=0) 2 N(H 3) 2 H 2-Pr 0 A-6629 H H H H S (=U) 2 N (OH 3) 2 H 2-CF 3 0 A-6630 H H H H 0 S(=0) 2 N(H 3) 2 H 2-UHF 2 0
A-6631 H H H H H f S(=0) 2 N (H 3) 2 H 2-GH 2F 0 A-6632 H H H H S =) 2 N (H 3) 2 H 2-GH 2O0 A-6633 H H H Hi if S(0) 2N(H3)2 H 2-cycbpropyl 0 A-6634 H H H H S(0=) 2 N (H 3) 2 H 2-cyclobutyl 0 A-6635 H H H H if S (=0) 2 N (H 3) 2 H 2-cyclopentyl 0 A-6636 H H H H f Df S(=0) 2 N(H 3 2 H 2-ethenyl1 A-6637 H H H H 0 S(=0) 2 N(H 3) 2 H 2-allyl1 A-6638 H H H H 0 S(=) 2 N(H 3) 2 H 2-(prop-1-en-1-y) 0 A-6639 H H H H H 0 S(=0) 2 N(H 3) 2 H 2-(trffboroethenyD 0 A-6640 H H H H 0 S(=0) 2 N (H 3) 2 H 2-UMe 0 A-6641 H H H HH i0 S=U) 2N(OH3)2 H 2-UEt 0 A-6642 H H H H 0 S(=) 2 N(H 3 2 H 2-OPr 0 A-6643 H H H H 0 S=) 2 N(H 3) 2 H 2-0 (/-Pr) 0 A-6644 H H H HH i0 S=U)2N(OH3)2 H 2-UGH3 0
A-6645 H H H H D0 S (=0) 2 N(H 3) 2 H 2-UGHF 2 0
A-6646 H H H H 0 S(0) 2 N(H 3) 2 H 2-(cycbpropybxy) 0 A-6647 H H H H 0 S(0) 2 N(H 3 2 H 2-(cycbbutybxy) 0 A-6648 H H H H 0 S(0) 2 N(H 3) 2 H 2-(cycbpentybxy) 0 A-6649 H H H H 5 s(=) 2N(H 3)2 H 2-((2,2-dichbrocycbpropy)oxy) 0 A-6650 H H H H F S =) 2 N (H 3 ) 2 H 2-(oxiran-2-yD A-6651 H H H H i i0 =) (H3)2 H 2N 2-SMe 0 A-6652 H H H H HD =) 2 N (OH 3) 2 H 3-SMe 0 A-6653 H H H H f0 S(0) 2 N(H 3) 2 H 2-S(=0)Me 0 A-6654 H H H H 0 S(=0) 2 N(H 3) 2 H 3-S(=0)Me 0 A-6655 H H H H F S(=0) 2 N(H 3) 2 H 2-S(=0) 2Me 0 A-6656 H H H H D0 S(0) 2N(H3)2 H 3-S(=0) 2Me 0 A-6657 H H H H i 5=U) 2 N(H 3) 2 H 2-SGF 3 A-6658 H H H Hf D S(=U) 2 N(H 3) 2 H 3-50F 3 0
A-6659 H H H H Hi0 S =U) 2N(OH 3) 2 H 3-S(=U)GH 3 0 A-6660 H H H H Hi0 S =U) 2 N (OH 3) 2 H 3-SF(GH 3) 2 0 A-6661 H H H H 0 S(=0) 2 N(H 3) 2 H 2-(cycbpropylthio) 0 A-6662 H H H H 0 S(=0) 2 N (H 3) 2 H 2-(cycbpropylsufinyD 0 A-6663 H H H H 0 S(O=) 2 N (H 3) 2 H 2-(cyclopropylsufonyD 0 A-6664 H H H H 0 S(=U) 2 N (OH 3) 2 H 2-G(=U)Me 0
[0243]
[Table 118]
com pound R' R2 R R A R R' (R)m p A-6665 H H H H 0 S(=U) 2N(H 3) 2 H 2-GH 2 3 0(=U)0H A-6666 H H H H H S(=U) 2 N (H 3) 2 H 2-CH 2 0(=U)0C 3 0 A-6667 H H H H H D S(=U) 2 N(H 3) 2 H 2-GH 2 0H A-6668 H H H H i 0 S(=U) 2 N (H 3) 2 H 2-GH 20H 3 0
A-6669 H H H H i S(=U) 2N(H 3)2 H D 2-GH20H2 3 CH 0
A-6670 H H H H 0 S(=U) 2 N(H 3) 2 H 2-GH 2SOH 3 0 A-6671 H H H H 0 S(=U) 2 N(H 3) 2 H 2-GH 2S(=U)CH 3 0
A-6672 H H H H 0 S(=U) 2 N(H 3) 2 H 2-GH 2S(=U) 2 CH 3 0 A-6673 H H H H i 0 S(=U) 2 N(H 3) 2 H 2-(benzybxy) 0 A-6674 H H H H i 0 S(=U) 2N(OH 3) 2 H 2-NH 2 A-6675 i H H H H 0 (=) 2N (H 3)2 H 2-NHMe 0 A-667 6 H H H H i 0 s(0) 2 N (H 3) 2 H 2-N (Me) 2 0 A-6677 H H H H f S(0) 2 N (H 3) 2 H 2-(1,3-dloxolan-2-yD A-6678 H H H H 0 S(=) 2 N(H 3 2 H 2-(1,3-dioxan-2-yD 0 A-6679 H H H H 0 S(=0) 2 N(H 3) 2 H 2-(1#-m idazol-2-yD 0 A-6680 H H H H (D=) 2N(H3)2H 2-(thiazol-2-yl) 0 A-6681 H H H H ( =)N (H 3 22 H 2-(oxazol-2-yD 0 A-6682 H H H H H0 S(=U) 2 N(H 3) 2 H 2-GH=N0H 0 A-6683 H H H H f0 (=) N(H 2 3 2 H 2-OH=NOMe 0 A-6684 H H H H 0 S(=) 2 N(H 3) 2 H 2-(4,b-dihydro-3-isoxazol) 0 A-6685 H H H H H 0 S(=U) 2 N (H 3) 2 H 2-N 0 A-6686 H H H HHi S(=U) 2N(OH3)2 H 2-NO 2 0 A-6687 H H H H H D S(=U) 2 N(H 3) 2 H 2-F,6-GI 0 A-6688 H H H H i 0 S(=U) 2N (H 3) 2 H 2-F,6-M e 0 A-6689 H H HHi if S0)2N(H32 H 3-F,6-M e 0 A-6690 H H H H S =U) 2 N (H 3) 2 H 4-F,2-M e 0 A-6691 H H H H S(0=) 2 N (H 3) 2 H 2-F,6-UMe 0 A-6692 H H H H iF S(=) 2N (H 3) 2 H 3-F,6-UMe 0 A-6693 H H H H DFf S(=O) 2 N(H 3) 2 H 2,6- W A-6694 H H H H 0 S(=0) 2 N(H 3) 2 H 2-GI,6-M e 0 A-6695 H H H H DFf S(=) 2 N(H 3) 2 H 3-GI,6-M e 0 A-6696 H H H H H 0 S(=U) 2 N(H 3) 2 H 4-GI,2-M e 0 A-6697 H H H H f S(=U) 2 N (H 3) 2 H 2-ILb-F 3 0 A-6698 H H H HHi0 3)2 H S=U) 2N(H Z-GI6-GH 3 A-6699 H H H H 0 S(=0) 2 N(H 3 2 H 2-GI,6-0Me 0 A-6700 H H H H f0 S 0) 2 N (H 3) 2 H 3-GI,6-0Me 0 A-6701 H H H HF = ) 2 N (H 3 ) 2 H 4-OI,2-UMe 0 A-6702 H H H H DFf S(=O) 2 N(H 3) 2 H 2,4-M e 2 0 A-6703 H H H H 0 S(=U) 2 N(H 3) 2 H 2,b-M e 2 0
A-6704 H H H H D S(=) 2 N(H 3) 2 H 2,6-M e 2 0 A-6705 H H H H 0 S(=0) 2 N(H 3) 2 H 2-Me,4-F 3 0 A-6706 H H H H D g S(=) 2N(H 3) 2 H 2-Me,b-F 3 0 A-6707 H H H H f0 S =U) 2 N (H 3) 2 H 2-M e,6-GH 3 0 A-6708 H H H H H 0 S(0=) 2 N (H 3) 2 H 2-M e,4-UMe A-6709 H H H H 0 t=) 2 N(OH 3) 2 H 2-M e,b-OMe 0 A-6710 H H H H f0 S=) 2 N (H 3) 2 H 2-M e,6-OMe 0 A-6/1l1 H H H H 0 S(=) 2 N(H 3) 2 H 3-M e,6-OMe 0 A-6712 H H H H DIi S(=U) 2 N(H 3) 2 H 4-M e,2-OMe 0 A-6713 H H H H 0 S(=0) 2 N(H 3) 2 H 2,b-UMe 2 0 A-6714 H H H H f0 S =U) 2 N (H 3) 2 H 2,6-UMe 2 0 A-6/lb H H H Hf S(=0) 2N(H 3) 2 H 2-OMe,6-F 3 0 A-6716 H H H H SF=U) 2 N (H 3 2 H 2-CHH 2,b-H 0 A-6717 H H H HF S(=U) 2 N (OH 3) 2 H 2-CH 2 ,6- F A-6718 H H H H Ff 0 S(=0) 2 N(H 3 2 H 2-OHF 2,b-Me A-6719 H H H H 0 S(=U) 2 N (H 3) 2 H 2-OHF 2,6-MA e 0 A-6720 H H H H H0 S(Ot=) 2 N (H 3) 2 H 2-cycbpropyLb-F 0 A-6721 H H H H 0 S(=U) 2 N (OH 3) 2 H 2-cycbpropyl,6-4 0
[0244]
[Table 119]
com pound R' R2 R R A R R' (R)m p A-6722 H H D i S(=)2N (H3)2 H 2-cyclopropylb-M e 0 A-6723 H H H H S (=) 2 N(H 3) 2 H 2-cyclopropyl,6-M e 0 A-6724 H H H H i 0 5(=U) 2 N (H 3) 2 H 2-ethenyl,6-F 0 A-6725 H H H H H 0 S=U) 2 N (H 3) 2 H 2-ethenyl,6-Me 0 A-6726 H H H H DifS(=U) 2N (H 3)2 H 2-OEt,b-F F A-6727 H H H H D i S(=) 2N(H 3)2 H 2-OEt,6-F 0 A-6728 H H H H - S(=U) 2 N(OH3 2 H 2-OEt,b-CI 0 A-6729 H H H H 0 S(=U) 2 N(H 3) 2 H 2-OEt,6-CI 0 A-6730 H H H H i 0 S(=U) 2 N (H 3) 2 H 2-OEt,b-M e 0 A-6731 H H H H 0 S 0) 2N(H 3 2 H 2-OEt,6-M e 0 A-6732 H H H H f0 A =U)2N(OH3)2 H 2-UGHH2,b-H 0
A-6733 H H H H D 2A=)N (H 3) 2 H 2-UGHH 2,6-F 0 A-6734 H H H H H 0 s=0) 2 N (H 3) 2 H 2-UGHF 2 ,b-M e 0 A-6735 H H H H 0 S(0) 2 N(H 3 2 H 2-UGHF 2 ,6-Me 0 A-6736 H H H H D S ( ) 2 N(H 3) 2 H 2-(cyclopropyloxy),b-F 0 A-6737 H H H H 0 =) 2 N (H 3 ) 2 H 2-(cyclopropyloxy),6-F 0 A-6738 H H H H 0 S(=) 2 N (H 3) 2 H 2-(cyclopropyloxy),b-M e 0 A-6739 H H H H 5 S(=U) 2N(H3)2 H 2-(cyclopropyloxy),6-Me 0 A-6740 H H H H 0 S=) N 2 (H 3 2 H 2-SMe,b-F 0 A-6741 H H H H 0 S(=0) 2 N(H 3 2 H 2-SMe,6-F 0 A-6742 H H H H 00 S(=U)2N(H3)2 H 2-SMe,b-Me 0 A-6743 H H H H 0 S(=U) 2 N(OH 3) 2 H 2-SMe,6-M e 0 A-6744 H H H H 0 S(0) 2 N(H 3 2 H 2-S(=0)Me,b-F 0 A-6745 HfHH H i 0 5(=U)2N(OH3)2 H 2-S(=U)Me,6-F 0 A-6746 H H H H 0 S =U) 2N (H 3) 2 H 2-S(=U)Me,b-M e 0 A-6747 H H H H i 0 S(=U) 2 N (H 3) 2 H 2-S(=U)Me,6-M e 0 A-6748 H H H H 0 S(=U) 2 N (H 3) 2 H 2-St=U) 2Me,b-F A-6749 H H H H i S (=U) 2N(OH 3) 2 H 2-S(=U) 2 Me,6-F 0 A-6750 H H H H D0S=) 2N(H 3)2 H 2-S(=O) 2Me,b-Me W A-6751 H H H H 0 S(0) 2 N(H 3) 2 H 2-S(=O) 2 Me,6-Me 0 A-6752 H H H H D S (=) 2N(OH 3) 2 H 2-50F 3 ,b-F 0 A-6753 H H H H H S (=0) 2 N(H 3) 2 H 2-SCF 3,6-F 0 A-6754 H H H H H 0 S(=0) 2 N(H 3) 2 H 2-SOF 3 ,b-Me 0 A-6755 H H H H Hf 50=U) 2 N(H 3) 2 H Z-SGH 3 ,6-e A-6756 H H H H H D s(=U) 2 N(OH 3) 2 H 2-S(=0)CF 3 ,b-F 0 A-6757 H H H H H D 5t=U) 2 N(H 3) 2 H 2-St=U)GF 3 ,6-F 0 A-6758 H H H H f 5=U) 2N(OH 3) 2 H 2-St=U)F 3 ,b-M e 0 A-6759 H H H H D S(=0) 2 N(H 3) 2 H 2-S(=0)CF 3 ,6-M e 0 A-6760 H H H H DI S (=0) 2 N(H 3) 2 H 2-S(=0) 20F 3 ,b-F 0 A-6761 H H H H 0 Sf0 (=0) 2 N(H 3) 2 H 2-S(=0) 20F 3 ,6-F 0 A-6762 H H H H 0 S(0) 2 N(H 3) 2 H 2-S(=0) 2OF 3 ,b-M e 0 A-6763 H H H H D S (0) 2 N(H 3) 2 H 2-S(=0) 2 CF 3 ,6-M e 0 A-6764 H H H H 0 5=U) 2 N (H 3 ) 2 H 2-(cyclopropylthb),b-F 0 A-6765 H H H H 0 5=U) 2 N (H 3 ) 2 H 2-(cyclopropylthb),6-F 0 A-6766 H H H H 0 5t = ) 2 N (OH 3) 2 H 2-(cyclopropy th io),b-M e 0 A-6767 H H H H 0 5=) 2 N(H 3) 2 H 2-(cyclopropylthio),6-M e 0 A-6768 H H H H D S (0) 2 N(H 3 2 H 2-C(=0)Me,b-F 0 A-6769 H H H H D S 0() 2 N(H 3 2 H 2-C(=0)Me,6-F 0 A-6770 H H H H S 0(=) 2N(H3)2 H 2-C(=0)Me,b-Me 0 A-6/l f H H H H i 0S(=U)2N (H 3)2 H 2-C(=0)Me,6- M e 0 A-6772 H H H H 0D S(=0) 2N(H 3) 2 H 2-CH 2UHb-F 0 A-6773 H H H H 0 5 2A=)N (H 3) 2 H 2-CH 2 H,6-F A-6774 H H H H 0 5 =) 2N (OH 3) 2 H Z-GH 2 N,b-Me A-6775 H H H H D S (0) 2 N(H 3 2 H 2-OH 2 0H,6-Me 0 A-6776 H H H H i S (=0) 2 N(OH3) 2 H 2-0H 20H 3 ,4-F 0 A-6777 H H H H 0 5=U) 2 N(H 3) 2 H 2-GH 20H 3 ,b-H 0
A-6778 H H H H i 0 5 (=U) 2N (OH 3) 2 H 2-0H 20H 3 ,6-F 0
[0245]
[Table 120]
com pound R' R2 R R A R R' (R)m p A-679 H H H H D S(=U) 2N(OH 3) 2 H 2-0H 2OOH 3 ,4-Me 0 A-6780 H H H H S (=) 2 N (H 3) 2 H 2-0H 2OOH 3 ,b-Me A-6781 H H H H D S (=) 2 N(H 3) 2 H 2-CH 2OOH 3 ,6-Me A-6782 H H H H i 0 S(=0) 2 N (H 3) 2 H 2-00(=0)GH 3 ,b-H A-6783 H H H H Dif S(=U) 2N(H3)2 H 2-0(=U)CH 3,6-F 0 A-6784 H H H H f Di S(=U) 2 N(H 3) 2 H 2-0(=U)CH 3 ,b-Me 0 A-6785 H H H H Di S (=U) 2 N(H 3) 2 H 2-0(=U)CH 3 ,6-M e 0 A-6786 H H H H Df S (=O) 2 N(H 3) 2 H 2-OS(=O) 2CH 3 ,b- 0 A-6787 H H H H D i S(=) 2N(H3)2 H 2-OS(=U) 2CH3,6-F 0 A-6788 H H H H 0 S(0=) 2N(H 3 2 H 2-0S=0) 2CH 3,5-M e 0 A-6789 H H H H i 0 (=) 2 N (H 3) 2 H 2-0S=0) 2CH 3,6-M e 0 A-6790 H H H H =0 ) 2 N (H 3) 2 H 2-CH 2SOH 3,b- 0 A-6791 H H f0 H H S(=0) 2 N (H 3) 2 H 2-CH 2SOH 3 ,6- 0 A-6792 H H H 0 H S(0) 2 N(H 3 2 H 2-CH 2SOH 3,b-Me 0 A-6793 H H H 0 H S(0) 2 N(H 3) 2 H 2-CH 2SOH 3,6-Me 0 A-6794 H H H H S (t=U) 2 N (H 3) 2 H 2-NMe 2 ,b-F A-6795 H H H H S(=U) 2 N (H 3 2 H 2-NMe 2 ,6 A-6796 H HFf H H S(=0) 2 N(H 3) 2 H 2-NMe 2 ,b-M e 0 A-6797 H H H H H (=U) 2 N (H 3) 2 H 2-NMe 2 ,6-M e 0 A-6798 H H H 0 H S(=U) 2 N(OH 3) 2 H 2-CN,4-F 0 A-6799 H H f0 H H S(=U) 2 N (H 3) 2 H 2-CN,b-F 0 A-6800 H H H H S(=U) 2 N (OH 3) 2 H 2-CN,6-F 0 A-6801 H H H H D S(=U) 2 N(H 3 2 H 2-CN,6-M e 0 A-6802 f H f H i S(=U) 2N(OH 3) 2 H 2-CN,b-UMe 0 A-6803 HfH(HfHif S(=) 2 N(H 3) 2 H 2-CN,6-UMe 0 A-6804 H H H H f0 S0) 2 N (GH 3) 2 H 3-CN,6-M e 0 A-6805 HfH HiHif S(=) 2 N (H 3 2 ) H 3-CN,6-UMe 0 A-6806 H H H H i S(=U) 2N (H 3) 2 H 4-CN,2-M e 0 A-6807 H H H H D S(=0) 2 N(H 3 2 H 4-CN,2-0Me 0 A-6808 H H H H DI S (=O) 2 N(H 3) 2 H 2-N0 2 ,4-F 0 A-6809 H H H H DFf0 5(=) 2 N(H 3) 2 H 2-N0 2 ,b-F 0
A-6810 H H H H H 0 S(=0) 2 N(H 3) 2 H 2-N0 2,6-F 0 A-6811 H H H H S (=0) 2 N (H 3) 2 H 2-N0 2,4-Me 0 A-6812 H H HH if0 )2N(OH3)2 H 2-N02,b-M e 0 A-6813 H H H H 0 S(=) 2 N(H 3 2 H 2-N0 2,6-M e 0 A-6814 H H H H 0 S0) 2 N (H 3) 2 H 2-M e,4,b- 2 0
A-6815 H H H H S(0=) 2 N (H 3) 2 H 2-M e,6-Et 0 A-6816 H H H H D S (0) 2 N(H 3 2 H 2-cyclopropyl,6-OMe 0 A-6817 H H H H 0 S(=0) 2 N(H 3) 2 H 2-M e,b-Et 0 A-6818 H H H H 0 S(=0) 2 N(H 3) 2 H 2,6-Et2 0 A-6819 H H H H 0 S(=0) 2 N(H 3) 2 H 2-Et,6-F 0 A-6820 H H H H Df S (=0) 2 N(H 3) 2 H 2-0H 20H 3 ,6-CI 0 A-6821 H H H H 5=0) 2 N (H ) 3 2 H -GH 20HCH 2 3 ,-CI A-6822 H H H H H 7 S0) 2 N (H 3) 2 H 2-CH 2 NM e 2 A-6823 H H H H 0 GH 2N (OH 3) 2 H H 0 A-6824 H H H H HiF GH 2N (GH 3) 2 H 2-F 0 A-6825 H H H H 0 CH 2N (OH 3) 2 H 2-Cl 0 A-682 Hf6 H H H 0 CH 2N (OH 3) 2 H 2-Br 0 A-6827 H H H H 0 CH 2N(OH 3 2 H 2-OH 0 A-6828 H H H H f0 GH 2N (OH 3) 2 H 2-M e 0 A-6829 H H H H F H D (OH3)2 H 2N 2-Et 0 A-6830 H H H H f0 GH 2N (OH 3) 2 H 2-Pr 0 A-6831 H H H H GH 2N (OH 3) 2 H 2-GH 3 0
A-6832 H H H0 H CH 2N (OH 3) 2 H 2-HF 2 0
A-6833 H H H Hi0 H CH 2N (OH 3) 2 H 2-CH 2F 0 A-6834 H H H Hi0 H GH 2N (OH 3) 2 H 2-GF 20 1F A-6835 H f FIFH 0 CH 2N (OH 3) 2 H 2-cycbpropyl 0
[0246]
[Table 121]
com pound R' R-2 R A R R' (R)m p A-6836 H H H H 0 OH 2N (OH 3) 2 H 2-cycobbutyl 0 A-6837 H H H H OH 2N (OH 3) 2 H 2-cycbpentyl 0 A-6838 H H H H D OH 2N (OH 3) 2 H 2-ethenyl1 A-6839 H H H H i 0 GH 2N (OH 3 ) 2 H 2-allyl1 A-6840 H H H H 0 OH 2N (OH 3) 2 H 2-(prop-1-en-1-yD 0 A-6841 H H H H 0 OH 2N (OH 3) 2 H 2-(trifboroethenyD 0 A-6842 H H H H D OH 2N (OH 3) 2 H 2-0Me A-6843 H H H H 0 OH 2N (OH 3) 2 H 2-OEt A-6844 H H H H 0 CH 2N (OH 3) 2 H 2-OPr 0 A-6845 H H H H DT- f GH2N(OH3)2 H 2-0 (/-Pr) 0 A-6846 H H H H i 0 OH 2N (OH 3) 2 H 2-UGH 3 0
A-6847 H H H H D OH 2N (OH 3) 2 H 2-GHF 2 0
A-6848 H H H H OH 2N (OH 3) 2 H 2-(cycbpropybxy) 0 A-6849 H H H H 0 OH 2N (OH 3) 2 H 2-(cycobbutybxy) 0 A-6850 H H H H 0 OH 2N (OH 3) 2 H 2-(cycbpentybxy) 0 A-6851 H H H H 0 OH 2N (OH 3) 2 H 2-((2,2-dichbrocycbpropyI)oxy) 0 A-6852 H H H OHGH2N (OH3)2 H 2-(oxiran-2-yD 0 A-6853 H H H HD 0HN 2(OH3)2 H 2-SMe 0 A-6854 H H H H I GH 2N (OH 3) 2 H 3-SMe 0 A-6855 H H H H 0 CH 2N (OH 3) 2 H 2-S(=0)Me 0 A-6856 H H H H H 0 H 2N (OH 3) 2 H 3-S(=0)Me 0 A-6857 H H H H 0 CH 2N (OH 3) 2 H 2-S (=0) 2Me 0 A-6858 H H H H D0 H 2N (OH3)2 H 3-S(=0) 2Me 0 A-6859 H H H H f0 CH 2N (OH 3) 2 H 2-SOF 3 0 A-6860 H H H H f0 GH 2N (OH 3) 2 H 3-SGH 3 0 A-6861 H H H H f0 GH 2N (H 3) 2 H 3-S(=U)GF 3 0 A-6862 H H H H f0 GH 2N (OH 3) 2 H 3-SF(GH 3) 2 0
A-6863 H H H H i 0 OH 2N (OH 3) 2 H 2-(cycbpropyltho) 0 A-6864 H H H H D0 H N 2 32 ( O H ) H 2-(cycbpropylsufinyD 0 A-6865 H H H H 0 OH 2N (OH 3) 2 H 2-(cycbpropylsufonyD 0 A-6866 H H H H D0 H 2N (OH3)2 H 2-G(=0)Me 0 A-6867 H H H H 0 CH 2N (OH 3) 2 H 2-0H 2 0(=U)CH 3 0
A-6868 H H H H Hi0 CH 2N (OH 3) 2 H 2-GH 2 0(=U)GF 3 0 A-6869 H H H H f0 GH 2N (OH 3) 2 H 2-CH 2 H 0 A-6870 H H H H D CH 2N (OH 3) 2 H 2-0H 20H 3 0
A-6871 H H H H D GH 2N (OH 3) 2 H 2-GH 20H 2CH 3 0
A-6872 H H H H GH 2N (OH 3) 2 H 2-CH 2SCH 3 F A-6873 H H H H 0 CH 2N (OH 3) 2 H 2-GH 2S(=0)CH 3 0
A-6874 H H H H 0 CH 2N (OH 3) 2 H 2-GH 2S(=0) 2 CH 3 0
A-6875 H H H H 0 OH 2N (OH 3) 2 H 2-(benzybxy) 0 A-6876 H H H H 0 CH 2N (OH 3) 2 H 2-NH 2 A-6877 H H H H 0 CH 2N (OH 3) 2 H 2-NHMe 0 A-6878 H H H H 0 GH 2N (OH 3) 2 H 2-N(Me) 2 A-6879 H H H H O GH2N (OH 3)2 H 2-(1,3-dboxolan-2-yD 0 A-6880 H H H H 0 OH 2N (OH 3) 2 H 2-(1 ,3-d ioxan-2-y D 0 A-6881 H H H H f0 GH 2N (OH 3) 2 H 2-(lH-i idazol-2-yD 0 A-6882 H H H H 0 CH 2N (OH 3) 2 H 2-(thiazol-2-y) 0 A-6883 H H H H 0 OH 2N (OH 3) 2 H 2-(oxazol-2-yD 0 A-6884 H H H H 0 CH 2N (OH 3) 2 H 2-GH= N0H 0 A-6885 H H H H f GH 2N (OH 3) 2 H 2-OH=NUMe 0 A-6886 H H H H 0 OH 2N (OH 3) 2 H 2-(4,b-dihydro-3-isoxazoyD 0 A-6887 H H H H f0 GH 2N (H 3) 2 H 2-N 0 A-6888 H H H H Hi0 GH 2N (OH 3) 2 H 2-NO 2 0
A-6889 FH H H H 0 CH 2N (OH 3) 2 H 2-F,6-GI 0 A-6890 FH H H H 0 CH 2N (OH 3) 2 H 2-F,6-M e 0 A-6891 H H HH f GH 2N (OH 3) 2 H 3-,6-iM e 0 A-6892 H H H H f0 CH 2N (GH 3) 2 H 4-F,2-Me 0
[0247]
[Table 122]
com pound R' RR RR A R R' (R)m P A-6893 H H H H 0 OH 2N (OH 3) 2 H 2-F,6-0Me 0 A-6894 H H H H O FH 2N (OH 3)2 H 3-F,6-UMe 0 A-6895 H H H H D CH 2N (OH 3) 2 H 2,6-C 12 A-6896 H H H H i 0 GH 2N (OH 3 ) 2 H 2-CI,6-M e 0 A-6897 H H H H 0 OH 2N (OH 3) 2 H 3-C,6-M e 0 A-6898 H H HHiff OH2N(H 3)2 H 4-C,2-Me 0 A-6899 H H H H D0f 2N (H (H 3) 2 H 2-CIb-C 3 A-6900 H H H H D0 H 2N (OH3)2 H 2-CI,6-C 3 A-690 Hf1 HH H 0 CH 2N (OH 3) 2 H 2-C,6-0Me 0 A-6902 H H H H D F GH2N (OH3)2 H 3-C,6-0Me 0 A-6903 H H H H i 0 OH 2N (OH 3) 2 H 4-CI,2-UMe 0 A-6904 H H H H O GH2N (O3H)2 H 2,4-M e2 0
A-6905 H H H H GH 2N (OH 3) 2 H Z,b-M e 2 0 A-6906 H H H H 0 CH 2N (OH 3) 2 H 2,6-M e 2 0 A-6907 H H H H iff OH2N(H 3)2 H 2-M e,4-CF 3 0 A-6908 H H H H 0 GH 2N (OH 3) 2 H Z-Me,b-C 3 0 A-6909 H H H H H GH 2N (OH 3) 2 H 2-M e,6-GH 3 0 A-6910 H H H H D0 H2N(0H3)2 H 2-M e,4-0Me A-6911 H H H H 0 GH 2N (GH 3) 2 H 2-M e,b-UMe 0 A-6912 HfHfH H DH 2N(H3)2 H 2-M e,6-0Me 0 A-6913 H H H H H 0 H 2 N (0H 3) 2 H 3-M e,6-UMe 0 A-6914 H H H H H 0 H 2 N (0H 3) 2 H 4-M e,2-UMe 0 A-6915 H H H H D CH 2N (OH 3) 2 H 2,b-UMe 2 0 A-6916 H H H H H 0 H 2N (OH 3) 2 H 2,6-UMe 2 0 A-6917 H H H H GH 2N (OH 3) 2 H 2-UMe,6-GF 3 0 A-6918 H H H H 0 GH 2N (OH 3) 2 H 2-CHH 2,b-H 0 A-6919 H H H H 0 GH 2N (OH 3) 2 H 2-CH 2,6-1 0 A-6920 H H H H HifC0HOH 2N(OH 3) 2 H 2-CHF 2,b-M e 0 A-6921 H H H H D0 H 2N (OH 3)2 H 2-CHF2,6-M e 0 A-6922 H i H H O H2N (OH3)2 H H 2-cycobpropylb-F 0 A-6923 H H H H O0H2N(OH3)2 H 2-cycobpropyl,64 0 A-6924 H H HHiff OH2N(H 3)2 H 2-cyclopropylb-Me 0 A-6925 H H H H i 0 CH 2N (OH 3) 2 H 2-cyclopropyl,6-Me 0 A-6926 H H H H 0 OH 2N (OH 3) 2 H 2-ethenyl,6-F 0 A-6927 H H H H 0 CH 2N(H 3) 2 H 2-ethenyl,6-Me 0 A-6928 H H H H D H 2N(OH 3) 2 H 2-OEt,b-F A-6929 H H H H f0 GH 2N(OH 3) 2 H 2-Et,6-F 0 A-6930 H H H H D0 H 2N (OH3)2 H 2-OEt,b-CI 0 A-6931 H H H H 0 CH 2N (OH 3) 2 H 2-OEt,6-CI 0 A-6932 H H H H D0 H 2N (OH3)2 H 2-OEt,b-Me 0 A-6933 H H H H 0 CH 2N (OH 3) 2 H 2-OEt,6-M e 0 A-6934 H H H H D0f 2N (H (H 3) 2 H 2-UGHF 2,b-F 0 A-6935 H H H H 0 GH 2N (OH 3) 2 H 2-UGHF 2,6-F 0 A-6936 H H H H H GH 2N (OH 3) 2 H 2-OHF 2 ,b-M e 0 A-6937 H H H H 0 GH 2N (OH 3) 2 H 2-UGHH 2 ,6-6Ae 0 A-6938 H H H H 0 OH 2N (OH 3) 2 H 2-(cyclopropyloxy),b-F 0 A-6939 H H H H DIf OH2N (H 3) 2 H 2-(cycbpropyloxy),6-F 0 A-6940 H H H H DIf OH2N(H 3) 2 H 2-(cyclopropybxy),b-Me 0 A-6941 H i H H O H2N (OH3)2 H IH 2-(cyclopropybxy),6-Me 0 A-6942 H H H H 0 GH 2N (OH 3) 2 H 2-SMe,b-F 0 A-6943 H H H H 0 CH 2N (OH 3) 2 H 2-SMe,6-F 0 A-6944 H H H H f0 GH 2N (H 3) 2 H 2-SMe,b-Me 0 A-6945 H H H H f0 GH 2N (OH 3 2 H 2-SMe,6-M e 0 A-6946 H H HHiff (H 2N(H 3)2 H 2-S(=0)Me,b-F 0 A-6947 H H H H iff (H 2N(H 3)2 H 2-S(=U)Me,6-F 0 A-6948 H H H IH H H2N (OH 3) 2 H 2-S(=U)Me,b-M e 0 A-6949 ifH H0 i H 2N (OH 3)2 H 2-S(=U)Me,6-M e 0
[0248]
[Table 123]
com pound R' R2 R R A R R' (R)m p A-6950 H H H H D 0 H2N (OH 3)2 H 2-S(=U) 2Me,b-F 0 A-6951 H H H H CH 2N (OH 3) 2 H 2-S(=U) 2Me,6-F 0 A-6952 H H H H D CH 2N (OH 3) 2 H 2-S(=U) 2 Me,b-Me 0 A-6953 H H H H i 0 GH 2N (OH 3 ) 2 H 2-S(=0) 2 Me,6-M e 0 A-69 5 4 H H H H 0 OH 2N (OH 3) 2 H 2-SOF 3,b-F 0 A-6955 H H H H 0 OH 2N (OH 3) 2 H 2-SOF 3 ,6-F 0 A-6956 H H H H 0 OH 2N (OH 3) 2 H 2-SOF 3 ,b-Me 0 A-6957 H H H H 0 OH 2N (OH 3) 2 H 2-SOF 3 ,6-Me 0 A-6958 H H H H 0 CH 2N (OH 3) 2 H 2-S(=U)0F 3 ,b-F 0 A-6959 H H H H DifGH2N(OH3)2 H 2-S(=0)0F 3,6-F 0 A-6960 H H H H i 0 OH 2N (OH 3) 2 H 2-S(=0)GF 3 ,b-M e 0 A-6961 H H H H D OH 2N (OH 3) 2 H 2-S(=0)GF 3,6-Me 0 A-6962 H H H H OH 2N (OH 3) 2 H 2-S(=0) 20F 3 ,b-F A-6963 H H H H 0 OH 2N (OH 3) 2 H 2-S(=U) 20F 3 ,6-F 0 A-6964 H H H H 0 CH 2N (OH 3) 2 H 2-S(=U) 2OF 3 ,b-Me 0 A-6965 H H H H 0 OH 2N (OH 3) 2 H 2-S(=0) 2OF 3 ,6-M e 0 A-6966 H H H H OGH2N(OH 3)2 H 2-(cyclopropylthlo),b-F 0 A-6967 H H H H 0 OH 2N (OH 3) 2 H 2-(cyclopropylthio),6-F 0 A-6968 H H H H 0 OH 2N (OH 3) 2 H 2-(cyclopropylthio),b-M e 0 A-6969 H H H H 0 OH 2N (OH 3) 2 H 2-(cyclopropylthio),6-Me 0 A-6970 H H H H H 0 H 2N (OH 3) 2 H 2-C(=U)Me,b-F 0 A-6971 H H H H H 0 H 2N (OH 3) 2 H 2-0(=U)Me,6-F 0 A-6972 H H H H DF H 2N(OH3)2 H 2-G(=O)Me,b-M e 0 A-6973 H H H H H 0 H 2N (OH 3) 2 H 2-G(=O)Me,6-Me 0 A-6974 H H H H Hi GH 2N (OH 3) 2 H 2-CH 2UH,b-H A-6975 H H H H 0 GH 2N (OH 3) 2 H 2-CH 2UN,6-F A-6976 H H H H 0 GH 2N (OH 3) 2 H 2-GH 2 0H,b-Me 0 A-6977 H H H H HifC0HOH 2N(OH 3) 2 H 2-OH 2OH,6-M e 0 A-6978 H H H H 0 CH 2N (OH 3) 2 H 2-GH 20H 3 ,4-F 0 A-6979 H H H H 0 CH 2N (OH 3) 2 H 2-GH 20H 3 ,b-4 0 A-6980 H H H H D 0 H2N(OH 3)2 H 2-GH20H3,6-F 0 A-6981 H H H H 0 CH 2N (OH 3) 2 H 2-GH 20CH 3 ,4-Me 0 A-6982 H H H H f0 CH 2N (OH 3) 2 H 2-GH 2OGH 3 ,b-Me 0 A-6983 H H H H I GH 2N (OH 3) 2 H 2-CH 20H 3 ,6-MAe 0 A-6984 H H H H 0 CH 2N (OH 3) 2 H 2-0(=U)0H 3 ,b-F 0 A-6985 iH H H H 0 GH2N(OH3)2 H 2-0(=U)0H3,6-F 0 A-6986 H H H H 0 GH 2N (OH 3) 2 H 2-U(=U)GH 3 ,b-Me A-6987 H H H H 0 CH 2N (OH 3) 2 H 2-0(=U)CH 3 ,6-M e 0 A-6988 H H H H 0 CH 2N (OH 3) 2 H 2-OS(=O) 2CH 3 ,b-F 0 A-6989 H H H H 0 CH 2N (OH 3) 2 H 2-OS(=U) 2CH 3 ,6-F 0 A-6990 H H H H 0 CH 2N (OH 3) 2 H 2-US(=U) 2CH 3,b-M e 0 A-6991 H H H H DF H 2N(OH3)2 H 2-US(=U) 2CH3,6-M e 0 A-6992 H H H H f0 GH 2N (OH 3) 2 H 2-CH 2SCH 3 ,b-H 0
A-6993 H H H H H GH 2N (OH 3) 2 H 2-CH 2SCH 3 ,6-F 0 A-6994 H H H H D GH 2N (OH 3) 2 H 2-CH 2SOH 3,5-M e 0 A-6995 H H H H f0 GH 2N (H 3) 2 H 2-CH 2SOH 3 ,6-M e 0 A-6996 H H H H 0 CH 2N (OH 3) 2 H 2-NM e 2 ,b-F 0 A-6997 H H H H 0 CH 2N (OH 3) 2 H 2-NM e 2 ,6-F 0 A-6998 H H H H 0 CH 2N (OH 3) 2 H 2-NM e 2 ,b-M e 0 A-6999 H H H H f0 GH 2N (OH 3) 2 H 2-NM e 2 ,6-M e 0 A-/000 H H H H 0 H 2N (H 3) 2 H 2-ON,4-F 0 A-7001 H H H H 0 2N (OH 3)2 H 2-ONb-F 0 A-7002 H H H H i0 GH 2N (OH 3 2 H 2-ON,6-F 0 A-7003 H H H H 0 OH 2N (H 3) 2 H 2-ON,6-M e 0 A-7004 H H H H 0 CH 2N (OH 3) 2 H 2-ON,b-UMe 0 A-700b H H H H f GH 2N (H 3) 2 H 2-ON,6-UMe 0 A-/006 H H H H CH 2N (OH 3) 2 H 3-ON,6-Me 0
[0249]
[Table 124]
com pound R' R R RR A R R' (R)m P A-/ H H if/ H H 0 CH 2N (OH 3) 2 H 3-GN,6-0Me 0 A-/008 H H H H OF H 2N (OH 3)2 H 4-ON,2-Me 0 A-/009 H H H H DF H2N(OH3)2 H 4-GN,2-0Me 0 A-710 H H H H i 0 GH 2N (OH 3 ) 2 H 2-N0 2,4-F 0 A-/011 H H H H 0 CH 2N (OH 3) 2 H 2-N0 2 ,b-F 0
A-7012 H H H H 0 CH 2N (OH 3) 2 H 2-N0 2 ,64 0 A-7013 H H H H 0 CH 2N (OH 3) 2 H 2-NU 2,4-MAe 0 A-7014 H H H H 0 OH 2N (OH 3) 2 H 2-NU 2,b-Me 0 A-/01b H H H H 0 CH 2N (OH 3) 2 H 2-N0 2,6-M e 0 A-7016 H H H H DF GH2N(OH3)2 H 2-M e,4,b-F2 0 A-l1 / H H H H i 0 GH 2N (OH 3) 2 H 2-M e,6-Et 0 A-/018 H H H H D OH 2N (OH 3) 2 H 2-cyclopropyl,6-OMe 0 A-70l9 H H H H GH 2N (OH 3) 2 H 2-M e,b-Et 0 A-7020 H H H H 0 CH 2N (OH 3) 2 H 2,6-Et2 0 A-7021 H H H H 0 CH 2N (OH 3) 2 H 2-Et,6-F 0 A-7022 H H H H 0 GH 2N (OH 3) 2 H 2-GH 2 UGH 3 ,6-C 1 A-7023 H H H H H00 GH 2N(OH 3) 2 H 2-CH 20H 2 H 3,6-C 10 A-7024 H H H H D0 H 2N (OH3)2 H 2-GH2NMe2 0
A-7025 H H H H f0 GH 2 G(=U)UH 3 H H 0 A-7026 H H H H D0 H 2C(=U)UGH3 H 2-F 0 A-02/ H H H H f0 CH 2 C(=U)UGH 3 H 2-CI 0 A-/028 H H H H f0 CH 2 C(=U)UGH 3 H 2-Br 0 A-/029 H H H H D CH 2 C(=U)UGH 3 H 2-OH 0 A-/030 H H H H i 0 CH 2 0(=U)UGH 3 H 2-M e 0 A-/031 H H H H Hi GH2G(=U)UGH3 H 2-Et 0 A-/032 H H H H H GH 2 G(0)UGH 3 H 2-Pr 0 A-/033 H H H H f0 GH 2 G(=U)UH 3 H 2-C 3 0
A-/034 H H H H i 0 CH 2 C(=U)UGH 3 H 2-UHF 2 0 A-/035 H H H H 0 CH 2 C(=U)UGH 3 H 2-CH 2F 0
A-/036 H H H H 0 CH 2 C(=O)OGH 3 H 2-CF 2OI 0 A-/03/ H H H H ifD0 H2(0)UGH 3 H 2-cycbpropyl 0 A-/038 H H H H D0 H 2C(0)GH3 H 2-ycobbutyl 0 A-/039 H H H H i 0 CH 2 0(=U)UGH 3 H 2-cycbpentyl 0 A-/040 H H H H f0 GH2 G()UGH 3 H 2-ethenyl1 A-/041 H H H H 0 CH2 C(0)GH 3 H 2-allyl A-/042 H H H H i0 GH2 G()UH 3 H 2-(prop-1-en-1-y) 0 A-/043 H H H H H GH 2 G(0)UGH 3 H 2-(trffbioroethenyD 0 A-/044 H H H H D 0 H2C(0)OH3 H 2-0Me A-/045 H H H H 0 CH 2 0(=O)OGH 3 H 2-OEt A-/046 H H H H 0 CH 2 (0)UGH 3 H 2-OPr 0 A-/04/ H H H H DICH0 H 2 (0)GH 3 H 2-0 (/-Pr) 0 A-/048 H H H H 0 CH 2 C(=U)UGH 3 H 2-UGF 3 0 A-/049 H H H H Hi0 GH 2 G(=U)UGH 3 H 2-GHF 2 0
A-/0b0 H H H H H GH 2 G(0)UGH 3 H 2-(cycbpropybxy) 0 A-/Obl H H H H 0 GH2 G()UGH 3 H 2-(cycobbutybxy) 0 A-/052 H H H f0 H GH2 G()UGH 3 H 2-(cycbpentybxy) 0 A-/053 H H H H 0 OH20(=O)GOH3 H 2-((2,2-dichbrocycbpropy)oxy) 0 A-/054 H H H H D0 H2O(=U)GOH 3 H 2-(oxiran-2-yl) 0 A-/Obb H H H H DIC0 H2 (0)UGH 3 H 2-SMe 0 A-/056 H H H H f0 GH2 G()UGH 3 H 3-SMe 0 A-l05/ H H H H 0 CH2 C(0)GH 3 H 2-S(=0)Me 0 A-7b8 H H H H f0 GH2 G()UGH 3 H 3-S(=U)Me 0 A-/0b9 H H H H f0 GH2 G()UGH 3 H 2-S =) 2Me A-/060 H H H H D0 H 2C(0)UGH3 H 3-S(=U)2Me 0 A-/061 H H H H 0 CH 2 C(=U)UGH 3 H 2-SOF 3 0 A-/062 H H H H 0 GH 2 G(=O)OH 3 H 3-SGH 3 A-/063 H H FH Hi0 1 H 2 O(=U)OOH 3 H 3-S(=O)OF 3 0
[0250]
[Table 125]
com pound R' R2 R R A R R' (R)m p A-7064 H H H H Dif 0 0H 20(=U)0H3 H 3-SCF(F32 0 A-7065 H H H H H F H 2 0(=U)0H 3 H 2-(cyclopropytho) 0 A-7066 H H H H D CH 2 0(=U)0 H 3 H 2-(cycbpropylsufinyD 0 A-06/ H H H H f GH 2 0(=U)0H 3 H 2-(cyclopropylsufonyD A-/068 H H H H 0 0H 2 0(=U)0H 3 H 2-C(=0)Me 0 A-/069 H H H H 0 0H 2 0(=U)0H 3 H 2-GH 2 0(=U)CH 3 A-J0/0 H H H H f Di 0H 2 0(=U)0H 3 H 2-GH 2 0(=U)CF 3 0 A-/0/1 H H H H 0 0H 2 0(=U)0H 3 H 2-0H 20H 0 A-/0/2 H H H H 0 0H 2 0(=U)U0H 3 H 2-0H 20H 3 0 A-/0/3 H H H H 0 H 2 G(=U)UH 3 H Z-GH 2 GH 2 H 3 0
A-/0/4 H H H H i 0 H 2 G(=U)UH 3 H Z-GH 2 H 3 0 A-J0/b H H H H 0 GH 2 G(=U)UH 3 H Z-GH 2 t=U)GH 3 A-/0/6 H H H H 0 GH 2 0(=U)0GH 3 H 2-CH 2S(=U) 2 CH 3 0
A-/0// H H H H 0 0H 2 0(=U)0GH 3 H 2-(benzybxy) 0 A-J0/8 H H H H 0 0H 2 0(=U)0GH 3 H 2-NH 2 A-/0/9 H H H H D 0GH 2 G(=U)0GH 3 H 2-NHMe 0 A-080 H H H HF GH 2 0(=U)0GH 3 H 2-N (Me)2 0 A-/081 H H H H D 0 H 2 0(=U)0GH 3 H 2-(1,3-dioxolan-2-yD 0 A-/082 H H H H f0 GH2 G(=U)U3 H 2-(1,3-dloxan-2-yD A-/083 H H H H D 0H 2 0(=0)0H 3 H 2-(1#-m idazol-2-yD 0 A-/084 H H H H H 0 H 2 0(=U)0GH 3 H 2-(thiazol-2-yl) 0 A-08b H H H H 0 0H 2 0(=U)0GH 3 H 2-(oxazol-2-yD 0 A-/086 H H H H D CH 2 0(=U)0GH 3 H 2-CH=N0H 0 A-08/ H H H H 0 0H 2 0(=U)0GH 3 H 2-CH=NUMe 0 A-/088 H H H H ifCH GH2G=U GH3 H 2-(4,b-dihydro-3-IsoxazolyD A-/089 H H H H f0 GH 2 0(=U)0GH 3 H 2-N 0 A-/090 H H H H f0 GH 2 G(=U)UH 3 H -NO 2 A-/091 H H H H i 0 0H 2 0(=U)0 H 3 H 2-F,6-C1 0 A-/092 H H H H 0 CH 2 0(=U)U0H 3 H 2-F,6-Me 0 A-/093 H H H H 0 CH 2 0(=0)0GH 3 H 3-F,6-Me 0 A-/094 H H H H D 0H 2 0(=U)UGH 3 H 4-F,2-M e 0 A-/095 H H H H 0 0H 2 0(=U)0GH 3 H 2-F,6-0Me 0 A-/096 H H H H i 0 0H 2 0(=U)0GH 3 H 3-F,6-UMe 0 A-/09/ H H H Hf 0 GH 2 G(=U)0GH 3 H 2,6-C F A-/098 H H H H 0 0H 2 0(=U)0GH 3 H 2-C,6-Me 0 A-/099 H H H H D 0H 2 G(=U)UGH 3 H 3-C,6-Me 0 A-/100 H H H H H 0 H 2 0(=U)0GH 3 H 4-CI,2-M e 0 A-/101 H H H H 0 0H 2 0(=U)0H 3 H 2-CIb-CF 3 0 A-/102 H H H H 0 0H 2 0(=U)0GH 3 H 2-CI,6-CF 3 0 A-/103 H H H H 0 0H 2 0(=U)UGH 3 H 2-C,6-0Me 0 A-/104 H H H H 0 0H 2 0(=U)0GH 3 H 3-C,6-0Me 0 A-/1Ob H H H H 0 0H 2 0(=U)0H 3 H 4-C,2-0Me 0 A-/106 H H H H GH 2 0(=U)0GH 3 H 2,4-M e 2 0 A-/10/ H H H H GH 2 G(=U)0GH 3 H 2,b-M e 2 0 A-/108 H H H H D 0H 2 G(=U)UGH 3 H ,6-Me 2 A-/109 H H H H 0 GH 2 G(=U)UH 3 H -Me,4-GH 3 A-/110 H H H H 0 CH 2 0(=U)U0H 3 H 2-Me,b-CF 3 0 A-/111 H H H H 0 CH 2 0(=U)U0 H3 H 2-M e,6-CF 3 0 A-/112 H H H H 0 0H 2 0(=U)0GH 3 H 2-M e,4-0Me A-/113 H H H H f0 GH 2 G(=U)UH 3 H 2-M e,b-UMe 0 A-/114 H H H H D 0 H2 0(=U)0 H3 H 2-M e,6-0Me 0 A-/ll5 H H H H 0 GH 2 G(=U)UH 3 H 3-M e,6-UMe 0 A-/116 H H H H 0 GH 2 G(=U)UH 3 H 4-M e,2-UMe 0 A-/11/ H H H H 0 0H 2 0(=U)0GH 3 H 2,b-UMe 2 0 A-118 H H H H 0 0H 2 0(=U)0GH 3 H 2,6-UMe 2 0 A-/119 H H H H 0 GH 2 G(=O)UGH 3 H 2-OMe,6-GH3 A-/120 H H 7H H 0 H2C (=0 )U CH 3 H 2-CH F 2,b-F 0
[0251]
[Table 126]
com pound R' R2 R R A R R' (R)m p A-/121 H H H H D if 0 0H 20(=U)0H 3H 2-CHF 2,6-F 0 A-J122 H H H H 0H 2 0(=U)0H 3 H 2-CHF 2,b-M e 0 A-J123 H H H H D CH 2 C(0)0H 3 H 2-CHF 2,6-Me 0 A-J124 H H H H H 0H 2 G(0)0H 3 H 2-cycbpropylb-F 0 A-J12b H H H H 0 0H 2 0(0)0H 3 H 2-cycbpropyl,6-F 0 A-J126 H H H H D 0H 2 C(0)0H 3 H 2-cyclopropylb-Me 0 A-/12J H H H H Df 0H2 C(0)0H 3 H 2-cyclopropyl,6-Me 0 A-/128 H H H H 0 0H2 C(0)0H 3 H 2-ethenyl,6-F 0 A-/129 H H H H 0 0H 2 0(=U)0H 3 H 2-ethenyl,6-M e 0 A-J130 H H H H D GH 2 G(=O)UGH 3 H 2-Ot-t,bFW A-J13 1 H H H H i 0 GH 2 0(=U)0GH 3 H 2-Et,6-F 0 A-J132 H H H H D GH 2 0(=U)0H 3 H 2-OEt,b-CI 0 A-J133 H H H H H GH 2 0(=U)0H 3 H 2-UEt,6-CI F A-J134 H H H H 0 0H 2 0(=U)0GH 3 H 2-OEt,b-Me 0 A-J13b H H H H 0 0H 2 0(=U)0GH 3 H 2-OEt,6-M e 0 A-J136 H H H H H0 H20(=U)0H3 H 2-UGHH2,b-H 0
A-13J H H H Hff GH 2G(=0)0H3 H 2-UGHH 2,6-F 0 A-J138 H H H H i fCH 2020(=)0H 3 H 2-OCH '2,b-M e 0 A-J139 H H H H D 0GH2 G0(=0)0GH 3 H 2-UGH H 2 ,6-M e A-J140 H H H H 0 0H 2 0(=U)0GH 3 H 2-(cycbpropyloxy),b-F 0 A-/141 H H H H 0 0H 2 0(=U)0H 3 H 2-(cycbpropyloxy),6-F 0 A-J142 H H H H f0 0H 20 (=U)0GH 3 H 2-(cyclopropybxy),b-M e 0 A-J143 H H H H D CH 2 0(=U)0GH 3 H 2-(cyclopropybxy),6-Me A-J144 H H H H i 0 0H 2 0(=U)0GH 3 H 2-SMe,b-F 0 A-J14b H H H H f GH 2 0(=U)0H 3 H 2-SMe,6-F 0 A-J146 H H H H GH 2G 0(= )GH 3 H 2-SM e,b-M e 0 A-/14J H H H H if0 GH20(=U)0H 3 H 2-SMe,6-M e F A-/148 H H H H i 0 0H 2 0(=U)0GH 3 H 2-S(=0)Me,b-F 0 A-J149 H H H H D 0H 2 0(=U)0GH 3 H 2-S(=0)Me,6-F 0 A-J150 H H H H CH 2C i 00(= )GH 3 H 2-S (=0)M e,b-M e 0 A-J1i51 H H H H D CH 2f 0(= )0GH 3 H 2-S (=0)M e,6-M e 0 A-Jlb2 H H H H 0 0H 2 0(=U)0GH 3 H 2-S(=0) 2Me,b-F 0 A-Jlb3 H H H H H 0H 2 0(=U)0H 3 H 2-S(=0) 2Me,6-F 0 A-Jl54 H H H H 0 GH 2 0(=U)0H 3 H 2-S(=0) 2 Me,b-M e 0 A-ibb H H H H f 0H 2 0(=U)0GH 3 H 2-S(=0) 2 Me,6--M e 0 A-/lb6 H H H H D GH 2 0(=U)0H3 H 2-SGF 3 ,b-F 0 A-Jib/ H H H H f0 GH 2 0(=U)0GH 3 H 2-SGH 3 ,6-1 0 A-/b8 H H H H 0 0H 2 0(=U)0GH 3 H 2-SCF 3 ,b-M e 0 A-Jib9 H H H H 0 0H 2 0(=U)0GH 3 H 2-SCF 3 ,6-M e 0 A-/160 H H H H 0 0H 2 0(=U)0GH 3 H 2-S(=0)C3,b-F 0 A-J161 H H H H 0 0H 2 0(=U)0GH 3 H 2-S(=0)0F 3,6-F 0 A-/162 H H H H 0 0H 2 0(=U)0GH 3 H 2-S(=0)F 3 ,b-M e 0 A-/163 H H H H H GH 2 0(=0)UGH 3 H 2-S(=0)GF 3 ,6-M e 0 A-/164 H H H H H GH 2 0(=0)UGH 3 H Z-S(=0) 20F 3 ,b-F A-J16b H H H H 0Di GH 2 0(=U)0GH 3 H 2-S(=0) 20F 3,6-F A-J166 H H H H H GH 2G(=0)0H 3 H 2-S(=0) 2 0F 3 ,b-Me A-/16/ H H H H 0 0H 2 0(=U)0GH 3 H 2-S(=0) 2CF 3 ,6-M e 0 A-J168 H H H H 0 0H 2 0(=U)0GH 3 H 2-(cycbpropylthb),b-F 0 A-J169 H H H H 0 0H 2 0(=U)0H 3 H 2-(cycbpropylthb),6-F 0 A-/1/ 0 H H H H H 0 H2G(=0)0 3 H 2-(cycbpropylthio),b-M e 0 A-1i/1 H H H H F 0H 2 0(=U)0GH 3 H 2-(cycbpropylthio),6-M e 0 A-/1/2 H H H H f0 GH 2 0(=U)0GH 3 H 2-C(=0)Me,b-F 0 A-/1/3 H H H H H GH 2G(=0)0H 3 H 2-C(=0)Me,6-F 0 A-14 H H H H 0 0H 2 0(=U)0GH 3 H 2-C(=0)Me,b-Me 0 A-/1/b H H H H f0 0H 2 0(=U)0GH 3 H 2-C(=U)Me,6-Me 0 A-J1/6 H H H H Hi0 GH 2 0(=U)0GH 3 H 2-GH 20H,b-F A-1/ H F FIFHi0 H2 0(=U)0GH 3 H 2-CH 2 H,6-F 0
[0252]
[Table 127]
com pound R' R2 R R A R R' (R)m p A-/1/8 H H H H 0 0H 2 0(0)0H 3 H 2-CH 2UH,b-M e 0 A-1/9 H H H H F 0H 2 0(=U)0H 3 H 2-0H 20H,6-M e 0 A-7180 H H H H f Df 0H 2 0(=U)0H 3 H 2-OH 20H 3 ,4-F A-7181 H H H H i 0 GH 2 0(=U)0H 3 H 2-GH 20H 3 ,b-H 0 A-7182 H H H H 0 0H 2 0(=U)0H 3 H 2-OH 20H 3 ,6-F 0 A-7183 H H H H 0 0H 2 0(=U)0H 3 H 2-OH 20H 3 ,4-M e 0 A-7184 H H H H 0Di 0H 2 0(=U)0GH 3 H 2-OH 20CH 3 ,b-M e 0 A-718b H H H H 0 0H 2 0(=U)0GH 3 H 2-OH 20H 3 ,6-M e 0 A-7186 H H H H 0 0H 2 0(=U)0GH 3 H 2-UC(=0)CH 3 ,b 0 A-/18/ H H H H D GH 2 G(=O)UGH 3 H 2-OC(=O)GH 3 ,6-F A-7188 H H H H i 0 GH 2 G(=U)0GH 3 H 2-UC(=U)CH 3 ,b-M e 0 A-7189 H H H H D GH 2 G(=O)UGH 3 H 2-C(=U)CH 3 ,6-M e 0 A-7190 H H H H GH 2 G(=U)GH 3 H 2-US(=U) 2CH 3 ,b-F A-7191 H H H H 0 0H 2 0(=U)0GH 3 H 2-US(=0) 2CH 3 ,6-F 0 A-7192 H H H H 0 0H 2 0(=U)0GH 3 H 2-US(=0) 2CH 3,b-M e 0 A-7193 H H H H f0 GH 2 G(=U)UH 3 H Z-US(=U) 2CH 3,6-e A-7194 H H H H f0 GH 2 G(=U)H 3 H Z-GH 2SCH 3,b-F A-7195 H H H H 0 CH 2 0(=U)U0H 3 H 2-OH 2 SCH 3,6-F 0 A-7196 H H H H f0 GH 2 G(=U)UH 3 H Z-GH 2 H 3,b-Me 0 A-7197 H H H H 0 CH 2 0(=U)U0H 3 H 2-OH 2SCH 3,6-Me 0 A-7198 H H H H f0 0H 2 0(=U)0GH 3 H 2-NMe 2 ,b-F 0 A-7199 H H H H H F H2 0(=U)0GH 3 H 2-NMe 2 ,6-F 0 A-7200 H H H H D CH 2 0(=U)0GH 3 H 2-NMe 2 ,b-Me 0 A-7201 H H H H 0H 2 0(=U)0GH 3 H 2-NMe 2 ,6-Me 0 A-7202 H H H H GH 2 0(=U)0GH 3 H 2-ON,4-F 0 A-7203 H H H H D 0GH 2 G(=U)U0H 3 H 2-ON,b-F 0 A-7204 H H H H D 0GH 2 G(=U)U0H 3 H 2-ON,6-F 0 A-7205 H H H H i 0 0H 2 0(=U)0GH 3 H 2-ON,6-Me 0 A-7206 H H H H D 0H 2 0(=U)0GH 3 H 2-ON5-0 Me 0 A-7207 H H H H if0 0H20(=U)0GH 3 H 2-ON,6-0Me 0 A-7208 H H H H D 0H 2 0(=U)0GH 3 H 3-ON,6-Me 0 A-7209 H H H H 0 0H 2 0(=U)0GH 3 H 3-ON,6-0Me 0 A-7210 H H H H i 0 0H 2 0(=U)0GH 3 H 4-ON,2-M e 0 A-7211 H H H H H GH2G(=0)0G H 4-ON,2-UMe 0 A-7212 H H H H D 0H 2 0(=U)0GH 3 H 2-N0 2 ,4-F 0 A-7213 H H H H WDi GH 2 0(=U)UGH3 H 2-N0 2 ,b-F 0 A-7214 H H H H i0 GH 2 G(=U)UH 3 H -NU 2 ,- 0 A-7215 H H H H 0 0H 2 0(=U)0GH 3 H 2-N0 2,4-M e 0 A-7216 H H H H 0 0H 2 0(=U)0GH 3 H 2-N0 2,b-Me 0 A-7217 H H H H 0 0H 2 0(=U)0GH 3 H 2-N0 2,6-M e 0 A-7218 H H H H 0 0H 2 0(=U)0GH 3 H 2-Me,4,b-F 2 0 A-7219 H H H H D 0H 2 0(=U)0GH 3 H 2-Me,6-Et 0 A-7220 H H H H H 0H2G(=0)0H3 H 2-cyclopropyl,6-OMe 0 A-7221 H H H H H GH2(=U)UGH3 H 2-Me,b-Et 0 A-7222 H H H H D 0H 2 G(=U)UGH 3 H Z,6-t 2 0
A-7223 H H H H f0 GH2 G(=U)U3 H 2-Et,6-F 0 A-7224 H H H H 0 CH 2 0(=U)U0H 3 H 2-OH 20H 3 ,6-I 0 A-7225 H H H H 0 CH 2 0(=U)U0H 3 H 2-OH 20H 2CH 3,6-OI 0 A-7226 H H H H 0 CH 2 0(=0)0GH 3 H 2-OH 2 NMe 2 0 A-7227 H H H H 0 GH 2G(=U)NH 2 H H 0 A-7228 H H H H 0 0H 2 0(=U)NH 2 H 2-F 0 A-7229 H H H H 0 GH 2G(=U)NH 2 H 2-CI F A-7230 H H H H GH 2G(=)NH 2 H 2-Br A-7231 H H H H 0 0H 2 0(=0)NH 2 H 2-OH 0 A-7232 H H H H f0 0H 2 0(=U)NH 2 H 2-M e 0 A-7233 H H H H Hi0 GH 2G(=U)NH 2 H 2-Et F A-7234 HIH 7H Hi0 H 2 0(=U)NH 2 H 2-Pr
[0253]
[Table 128]
com pound R' R2 R R A R6 R(R°)m P A-7235 H H H H 0 0H 2C(=)NH 2 H 2-CF 3 0 A-7236 H H H H 0H 2C (=)NH 2 H 2-H F 2 0 A-7237 H H H H D 0H 2C (=)NH 2 H 2-CH 2F 0
A-7238 H H H H i 0 GH 2 0= U)NH 2 H 2-GH2G 1 A-7239 H H H H D0 H 2(= )NH 2 H 2-cycbpropy 1 0 A-7240 H H H H 0 0H 2C 0= )NH 2 H 2-ycobbutyl 0 A-7241 H H H H D 0H 2 (= )NH 2 H 2-cycbpenty 1 0 A-7242 H H H H 0 0H 2C 0= )NH 2 H 2-ethenyl 0 A-7243 H H H H 0 0H 2C 0= )NH 2 H 2-allyl A-7244 H H H H D 0 GH20= U)NH2 H 2-(prop-1-en-1-y D 0 A-7245 H H H H GH 2 0= U)NH 2 H 2-(trffuoroetheny D 0 A-7246 H H H H D GH 2 =0 )NH 2 H 2-0M e A-7247 H H H H 0 GH 2 =0 )NH 2 H 2-UEt A-7248 H H H H 0 0H 2C 0= )NH 2 H 2-OPr 0 A-7249 H H H H 0 0H 2 0(=U)NH 2 H 2-0(/-Pr) 0 A-7250 H H H H H0 GH 2 0= U)NH 2 H 2-0GH A-7251 H H H H I GH 2G 0= U)NH 2 H 2-CH H 2 0 A-7252 H H 2C 0= U)NH2 H H H D0 H 2-(cycbpropy bxy) 0 A-7253 H H H H I GH 2( T=0 )NH 2 H 2-(cycbbuty loxy) 0 A-7254 H H H H 0 0H 2C 0= )NH 2 H 2-(cycobpenty bxy) 0 A-7255 H H H H f0 0H 2C 0= )NH2 H 2-((2,2,d ch brocycbpropy oxy) A-7256 H H H H f0 0H 2 0(=U)NH 2 H 2-(oxiran-2-yD 0 A-7257 H H H H 0 H2C 0= )NH 2 H 2-SMe 0 A-7258 H H H H 0 0H 2C 0= )NH 2 H 3-SMe 0 A-7259 H H H H I GH 2( T=0 )NH2 H 2-S =0 )M e A-7260 H H H H f0 GH 2 =0 )NH 2 H 3-S =0 )M e 0 A-7261 H H H H H GH 2( T=0 )NH 2 H 2-S =0) 2M e A-7262 H H H H i 0 0H 2C 0= )NH 2 H 3-S(= 0) 2M e 0 A-7263 H H H H 0 0H 2C 0= )NH 2 H 2-SCF3 0 A-7264 H H H H 0 0H 2C 0= )NH 2 H 3-SC F3 A-7265 H H H H 0 0H 2C 0= )NH 2 H 3-S (= 0)C 3 A-7266 H H H H 0 0H 2C 0= )NH 2 H 3-SCF(CF3) 2 A-7267 H H H H f0 0H 2C 0= )NH 2 H 2-(cycobpropy th) 0 A-7268 H H H H I GH 2( T=0 )NH 2 H 2-(cycbpropy Isu finy D 0 A-7269 H H H H 0 0H 2 0(=U)NH 2 H 2-(cycobpropysu TfonyD 0 A-7270 H H H H D GH 2 =0 )NH 2 H 2-C (=0)M e 0 A-7271 H H H H Hi0 GH 2 =0 )NH 2 H 2-GH 2 =0 )GH 3 0
A-7272 H H H H 0 0H 2C = U)NH 2 H 2-CH 2C =0 )CF 3 A-7273 H H H H 0 CH 2 (=0)NH 2 H 2-CH 20H 0 A-7274 H H H H 0 0H 2 0 (= )NH 2 H 2-CH 20H 3 0
A-7275 H H H H 0 0H 2c 0= )NH 2 H 2-CH 20H 2CH 3 0
A-7276 H H H H 0 0H 2 (= )NH 2 H 2-CH 2SCH 3 0 A-7277 H H H H f0 H 2 (=U)NH 2 H 2-CH 2S =0 )H 3 0
A-7278 H H H H H GH 2G(= 0)NH 2 H 2-CH 2S =0 ) 2 CH 3 A-7279 H H H H D GH 2 T=0U)NH 2 H 2-(benzy bxy) 0 A-7280 H H H H i0 GH 2 T=U)NH 2 H 2-NH 2 A-7281 H H H H 0 0H 2C 0= )NH 2 H 2-NH Me A-7282 H H H H 0 0H 2c 0= )NH 2 H 2-N Me) 2 A-7283 H H H H 0 0H 2C 0= )NH 2 H 2-(1,3-d bxo an-2-yD 0 A-7284 H H H H i 0 GH 2G (=)NH 2 H 2-(1,3-dbxan-2-y D 0 A-7285 H H H H 0 0H 2 0 (=U)NH 2 H 2-(1H-~ idazokE2-yD A-7286 H H H H 0 GH 2G(=U)NH 2 H 2-(thiazol-2-yl) 0 A-7287 H H H H 0 H 2G =U)NH 2 H 2-(oxazol-2-yD A-7288 H H H H 0 0H 2C 0= )NH 2 H 2-CH= N0H 0 A-7289 H H H H f0 0H 2C 0= )NH 2 H 2-CH= NUM e 0 A-7290 H H H H f GH 2Gt= U)NH2 H 2-(4,b-dihydro-3-soxazoD 0 A-7291 H H H Hi0 0H 2C = U)NH 2 H 2-N 0
[0254]
[Table 129]
com pound ' R2 RR R A R R' (R)m P A-7292 H H H H 0 0H C (=)NH 2 2 H 2-NU 2 0
A-7293 H H H H 0H 2C 0= )NH 2 H 2-F,6-CI 0 A-7294 H H H H D 0H 2C 0 U)NH 2 H 2-F,6-M e 0 A-7295 H H H H i 0 GH 2 tO)NH 2 H 3-F,6-M e 0 A-7296 H H H H D0 H 2C =)NH2 H 4-F,2-M e 0 A-7297 H H H H 0 0H 2C 0= )NH 2 H 2-F,6-M e 0 A-7298 H H H H D 0H 2C 0= )NH 2 H 3-F,6-M e 0 A-7299 H H H H 0 0H 2C 0= )NH 2 H 2,6-C 0 A-300 H H H H 0 0H 2C 0= )NH 2 H 2-C 1,6- e 0 A-7301 H H H H D 0 GH2=0)NH2 H 3-C 1,6- e 0 A-7302 H H H H i 0 GH 2 =0 )NH 2 H 4-C 1,2- e 0 A-7303 H H H H D GH 2 =0 )NH 2 H 2-C Ib-CF 3 A-7304 H H H H 0 GH 2G =O)NH 2 H 2-C1,6-CF 3 0 A-/30b H H H H 0 H2C =O)NH 2 H 2-C ,6-0M e 0 A-7306 H H H H 0 0H 2C =O)NH 2 H 3-C ,6-0M e 0 A-7307 H H H H f0 GH 2G =U)NH 2 H 4-C 1,2-0M e 0 A-/308 H H H H i0 H(=U)NH 2 H 2,4-e 2 A-/309 H H H H D0 H 20(=O)NH2 H 2,5-Me2 0
A-7310 H H H H GH 2G(= U)NH 2 H 2,6- e 2 0
A-7311 H H H H 0 0H 2 0(= )NH 2 H 2-M e,4-CF 3 0 A-7312 H H H H f0 0H 2C =O)NH 2 H 2-M e,b-CF 3 0 A-7313 H H H H 0H 2C =O)NH 2 H 2-M e,6-CF 3 0 A-7314 H H H H i D H 20(=U)NH 2 H 2 -Me,4-0Me 0 A-/ 31 H H H H i 0 0H 2C 0= )NH 2 H 2-M e,b-0M e 0 A-7316 H H H H GH 2 =0 )NH 2 H 2-M e,6-0M e 0 A-7317 H H H HIF GH 2 =0 )NH 2 H 3-M e,6-0M e 0 A-318 H H H H f GH 2 =0 )NH 2 H 4-M e,2-0M e 0 A-/319 H H H H i 0 0H 2C 0= )NH 2 H 2,b-M e 2 0 A-7320 H H H H D0 H C 2 2= ) N H H 2, 6 - 0 M e2 0 A-7321 H H H H 0 0H 2C 0= )NH 2 H 2-UM e,6-F 3 0 A-7322 H H H H 0 0H 2C = O)NH 2 H 2-CH F 2,b-F 0 A-7323 H H H H 0 0H 2C 0= )NH 2 H 2-CH ' 2,6-F 0 A-7324 H H H H f0 0H 2C 0= )NH 2 H 2-CH F 2,b-M e 0 A-732b H H H Hfi0 = 0G )NH 2 H 2-CH F 2,6-M e 0 A-7326 H H H H D0 H 2(= )NH 2 H 2-cycbpropy 1,b-F 0 A-7327 H H H H D GH 2G =U)NH 2 H 2-cycbpropy 1,6-F 0 A-7328 H H H H G2G= )NH 2 H 2-cyclopropylb-M e 0 A-7329 H H H H D0 H 20 (= O) N H2 H 2-cyclopropyl,6-Me 0 A-7330 H H H H 0 0H 2C(=O)NH 2 H 2-ethenyl,6-F 0 A-7331 H H H H D 0H 20 (=O)NH 2 H 2-ethenyl,6- e 0 A-7332 H H H H 0 0H 2C(=O)NH 2 H 2-0Etb-F 0 A-7333 H H H H D 0H 2C 0= )NH 2 H 2-OEt6-F 0 A-7334 H H H H H 0 GH 2 0= U)NH 2 H 2-0Etb- CI F A-733b H H H H 0 H 2 =0 )NH 2 H 2-0Et,6-CI1 A-7336 H H H H D GH 2 =0 )NH 2 H 2-0Etb--M e 0 A-7337 H H H H 0 GH 2G = U)NH 2 H 2-0Et6-M e 0 A-7338 H H H H 0 0H 2C 0= )NH 2 H 2-0CH b2,-F 0 A-7339 H H H H 0 0H 2c (= U)NH 2 H 2-CH 1 2,6-F 0 A-7340 H H H H 0 0H 2C = O)NH 2 H 2-OCH F2 ,b-M e 0 A-7341 H H H H ifi f 0 G A(= )NH 2 H 2-CH F2,6 -Me 0 A-7342 H H H H D CH 2C = U)NH 2 H 2-(cycobpropyloxy),b-F 0 A-7343 H H H H f GH 2 =0 )NH 2 H 2-(cycobpropyloxy),6-F 0 A-7344 H H H H f GH 2 0=U)NH 2 H 2-(cyclopropy bxy),b-M e 0 A-734b H H H H 0 CH 2C = )NH 2 H 2-(cyclopropy oxy),6-M e 0 A-7346 H H H H f0 CH 2C (=O)NH 2 H 2-SM e,b-F 0 A-7347 H H H H EF CG 0(U)NH = 2 H 2-SMe,6-F 0 A-/348 H H H H I0 H 2C(=O)NH 2 H 2-SM e,b5-e 0
[0255]
[Table 130]
com pound R' R2 R R A R R' (R)m p A-7349 i H H H H 0 0H2C0= )NH 2 H 2-SMe,6-M e 0 A-7350 H H H H 0H 2C =)NH 2 H 2-S =0 )M e,b-F 0 A-7351 H H H H D 0H 2C =)NH 2 H 2-S(=0)M e,6-F 0 A-7352 H H H H H GH 2G =0)NH 2 H 2-S = )Me,b-M e 0 A-7353 H H H H 0 0H 2C 0= )NH 2 H 2-S(=0)Me,6-M e A-7354 H H H H D 0H 2C 0 U)NH 2 H 2-S(= 0M e,b-F 0 A-7355 H H H H 0 0H 2C 0 )NH 2 H 2-S(= 0M e,6-F 0 A-7356 H H H H 0 0H 2C 0= )NH 2 H 2-S(= 0) 2 Me,b-M e 0 A-73 57 H H H H 0 0H 2C 0= )NH 2 H 2-S(= 0)M e,6--M e 0 A-7358 H H H H D 0H 2 (=0 )NH 2 G H 2-SCFb-F A-73 5 9 H H H H i 0 GH 2 =0 )NH 2 H 2-SC 3 ,6- 0 A-7360 H H H H D GH 2 (=0 )NH 2 H 2-SCF 3 b-M e 0 A-7361 H H H H H2 G=0)NH 2 H 2-SCF 3 ,6-M e 0 A-7362 H H H H 0 0H 2C =)NH 2 H 2-S (=)C3,b-F 0 A-7363 H H H H 0 0H 2C =)NH 2 H 2-S (=U)F 3 ,6-F 0 A-7364 H H H H H 2 = )NH 2 H Z-S(=U)GH 3 ,b- e A-7365 H H H H f0 GH 2G =)NH 2 H Z-S(=U)G,6-M e F A-7366 H H H H D0 H2c=0U)NH2 H 2-S =0 )23,b-F 0 A-7367 H H H H Hf GH 2G t=O)NH 2 H 2-S = ) 2 CG 3 6-H 0 A-7368 H H H H D0 H 2C (= U)NH2 H 2-S =0 2CF3,b-M e 0 A-7369 H H H H H0 H 2 0 (= )NH 2 H 2-S =0 ) 2 CF 3 ,6-M e 0 A-7370 H H H H 0 0H 2C 0= )NH 2 H 2-(cycbpropylth b),b-F 0 A-/3/1 H H H H D0 H2C 0= )NH 2 H 2-(cycbpropylth b),6-F 0 A-7372 H H H H H0 H 2C 0= )NH 2 H 2-(cycbpropy thio),b-M e 0 A-7373 H H H H H0 H 2 0= U)NH 2 H 2-(cycbpropy thio),6-M e 0 A-7374 H H H H H 2 = )NH 2 H 2 -(= U)M e,b-F 0 A-3/b H H H H 0 H 2G =U)NH 2 H 2-(= 0)M e,6-F 0 A-7376 H H H H i 0 0H 2C 0= )NH 2 H 2-(= )M e,b-M e 0 A-3/ H H H H 0 0H 2 (= )NH 2 H 2-(= 0)M e,6-i e 0 A-/3/8 H H H H 0 0H 2C 0= )NH 2 H 2-GH 20H,b-F 0 A-/3/9 H H H H 0 0H 2C 0= )NH 2 H 2-GH 20H,6-F 0 A-/380 H H H H 0 0H 2C 0= )NH 2 H 2-0H 20H, 5-M e 0 A-/381 H H H H H 0 H 2C 0= )NH 2 H 2-0H 20H,6 e 0 A-/382 H H H H i GH 2 0= U)NH 2 H 2-GH 20H 3 ,4-F 0 A-/383 H H H H D 0H 2C 0= )NH 2 H 2-GH 20H 3 ,b-4 0 A-/384 H H H H D GH 2 0(= U)NH2 H 2-GH 20H 3 ,6-H 0 A-/385 H H H H iH2 = 0G )NH 2 H 2-CH 2UCH 3 ,4-M e 0 A-/386 H H H H 0 0H 2 0(=U)NH 2 H 2-0H 20CH 3 ,b5- e 0 A-/38/ H H H H D 0H 2c(= 0)NH 2 H 2-CH 20CH 3,6-Me 0 A-/388 H H H H 0 H 2C= 0)NH 2 H 2-0C= U)CH 3 ,b- 0 A-/389 H H H H 0 0H 2c= 0)NH 2 H 2-0C= U)CH 3,6-F 0 A-/390 IfH H H H 0 H 2 0(=U)NH 2 H 2-0C(=0)CH 3 ,b-Me 0 A-/391 H H H H H GH2G(=U)NH 2 H 2-00(=U)GH 3 ,6-M e 0 A-/392 H H H H H GH 2G(= U)NH 2 H 2-US(= U) 2 H3,b-H A-/393 H H H H GH 2 (= )NH 2 H 2-OS (=O )2 H 3 ,6-F A-/394 H H H H f GH 2 T=O )NH 2 H 2-OS(= U) 2 H 3 ,b-M e 0 A-/395 H H H H 0 0H 2C 0= )NH 2 H 2-US(= 0) 2 H 3,6-M e 0 A-/396 H H H H 0 0H 2c 0= )NH 2 H 2-0H 2 S0H 3 ,b-4 0 A-/39/ H H H H 0 0H 2C 0= )NH 2 H 2-0H 2 S0H 3 ,6-F 0 A-/398 H H H H H2 F= )NH 2 H 2-CH 2SCH 3,b- e 0 A-/399 H H H H 0 0H 2 0 (= )NH 2 H 2-GH 2SCH 3,6-Ae 0 A-/400 H H H H f GH 2G = )NH 2 H 2-NM e 2 ,b-H 0 A-/401 H H H H H 2G = )NH 2 H Z-NMe 2 ,6- 0 A-/402 H H H H 0 0H 2C (= 0)NH 2 H 2NM e 2 ,b-M e 0 A-/403 H H H H H 0 H 2C = )NH 2 H 2NM e 2 ,6-Ae 0 A-/404 H H H H f0 GH 2G =O)NH 2 H 2-ON,4-F 0 A-/40b H H H H 0 H 2C = U)NH 2 H 2-ONb-F 0
[0256]
[Table 131]
com pound RI R2 R R R A R6 R(R)m P A-7406 H H H H H 0 CH 2C0(=)NH 2 H 2-CN,6-F 0 A-7407 H H H H H CH 2C(=0)NH 2 H 2-CN,6-M e 0 A-7408 H H H H H CH 2C(0)NH 2 H 2-CN,5-OMe 0 A-7409 H H H H H 0 0H 2C(0)NH 2 H 2-CN,6-OMe 0 A-7410 H H H H H 0 CH 2C(=0)NH 2 H 3-CN,6-M e 0 A-7411 H H H H H 0 CH 2C(=0)NH 2 H 3-CN,6-OMe 0 A-7412 H H H H H 0 CH 2C(=0)NH 2 H 4-CN,2-M e 0 A-7413 H H H H H 0 CH 2C(=0)NH 2 H 4-CN,2-OMe 0 A-7414 H H H H H 0 CH 2C(=0)NH 2 H 2-N0 2,4-F 0 A-7415 H H H H H F0 H 20(=O)NH 2 H 2-N0 2,b-F 0 A-7416 H H H H H 0 0H 2C0(=)NH 2 H 2-N0 2 ,6-4 0 A-7417 H H H H H 0 0H 20(=O)NH 2 H 2-N0 2,4-MAe 0 A-7418 H H H H H 0 H2C0(=)NH 2 H 2-N0 2,b-MAe 0 A-7419 H H H H H 0 CH 2C(=0)NH 2 H 2-N0 2,6-M e 0 A-7420 H H H H H 0 CH 2C(=0)NH 2 H 2-Me,4,5-F 2 0 A-7421 H H H H H 0 0H 20(=O)NH 2 H 2-M e,6-Et 0 A-7422 H H H H H 0 0H 20(=O)NH 2 H 2-cyclopropyl,6-OMe 0 A-7423 H H H H H 0 CH 2C(=0)NH 2 H 2-Me,5-Et 0 A-7424 H H H H H 0 H 20(=O)NH 2 H 2,6-Et2 0 A-7425 H H H H H 0 CH 2C(=0)NH 2 H 2-Et,6-F 0 A-7426 H H H H H 0 CH 2C(=0)NH 2 H 2-CH 20CH3 ,6-CI 0 A-7427 H H H H H 0 CH 2C(=0)NH 2 H 2-CH 20CH 2 CH 3 ,6-CI 0 A-7428 H H H H H 0 CH 2C(=0)NH 2 H 2-CH 2 NMe 2 0 A-7429 H H H H H 0 CH=NOH H H 0 A-7430 H H H H H 0 CH=NOH H 2-F 0 A-7431 H H H H H 0 CH=NOH H 2-C| 0 A-7432 H H H H H 0 CH=NOH H 2-Br 0 A-7433 H H H H H 0 CH=NOH H 2-OH 0 A-7434 H H H H H 0 CH=NOH H 2-M e 0 A-7435 H H H H H 0 CH=NOH H 2-Et 0 A-7436 H H H H H 0 CH=NOH H 2-Pr 0 A-7437 H H H H H 0 CH=NOH H 2-CF 3 0 A-7438 H H H H H 0 CH=NOH H 2-CH F 2 0 A-7439 H H H H H 0 CH=NOH H 2-CH 2F 0 A-7440 H H H H H 0 CH=NOH H 2-CF 2CI 0 A-7441 H H H H H 0 CH=NOH H 2-cycbpropy 1 0 A-7442 H H H H H 0 CH=NOH H 2-cycobbutyl 0 A-7443 H H H H H 0 CH=NOH H 2-cycbpenty 1 0 A-7444 H H H H H 0 CH=NOH H 2-etheny 1 0 A-7445 H H H H H 0 CH=NOH H 2-aIlyl 0 A-7446 H H H H H 0 CH=NOH H 2-(prop-1-en-1-y) 0 A-7447 H H H H H 0 CH=NOH H 2-(trifforoetheny D 0 A-7448 H H H H H 0 CH=NOH H 2-0M e 0 A-7449 H H H H H 0 CH=NOH H 2-0Et 0 A-7450 H H H H H 0 CH=NOH H 2-OPr 0 A-7451 H H H H H 0 CH=NOH H 2-0 (/-Pr) 0 A-7452 H H H H H 0 CH=NOH H 2-0CF 0 A-7453 H H H H H 0 CH=NOH H 2-0CHF 2 0 A-7454 H H H H H 0 CH=NOH H 2-(cycbpropybxy) 0 A-7455 H H H H H 0 CH=NOH H 2-(cycobbuty oxy) 0 A-7456 H H H H H 0 CH=NOH H 2-(cycbpentybxy) 0 A-7457 H H H H H 0 CH=NOH H 2-((2,2-dichbrocycbpropy)oxy) 0 A-7458 H H H H H 0 CH=NOH H 2-(oxiran-2-yl 0 A-7459 H H H H H 0 CH=NOH H 2-SM e 0 A-7460 H H H H H 0 CH=NOH H 3-SM e 0 A-7461 H H H H H 0 CH=NOH H 2-S(=0)Me 0 A-7462 H H H H H 0 CH=NOH H 3-S(=0)Me 0
[0257]
[Table 132]
com pound RI R2 R A R R R R' (R)m P A-7463 Hi- H H 0 H H CH=NOH H 2-S (=0) 2M e 0 A-7464 H H H H H 0 CH=NOH H 3-S (=0) 2M e 0 A-7465 H H H 0 H H CH=NOH H 2-SCF, 0 A-7466 H H H H H 0 CH=NOH H 3-SCF, 0 A-7467 H H H H H 0 CH=NOH H 3-S(=0)CF, 0 A-7468 H H H 0 H H CH=NOH H 3-SCF(CF,) 2 0 A-7469 H H H H H 0 CH=NOH H 2-(cycobpropy th b) 0 A-7470 H H H 0 H H CH=NOH H 2-(cycbpropylsulfinyD 0 A-7471 H H H H H 0 CH=NOH H 2-(cycobpropy u fony D 0 A-7472 H H H H H 0 CH=NOH H 2-C(=0)Me 0 A-7473 H H H H H 0 CH=NOH H 2-CH 20(=O0 H 3 0 A-7474 H H H H H 0 CH=NOH H 2-CH 20(=O)G 3 0 A-7475 H H H H H 0 CH=NOH H 2-CH 2OH 0 A-7476 H H H H H 0 CH=NOH H 2-CH 2 0CH 3 0 A-7477 H H H H H 0 CH=NOH H 2-CH 2 0CH 2CH 3 0 A-7478 H H H H H 0 CH=NOH H 2-CH 2SCH 3 0 A-7479 H H H H H 0 CH=NOH H 2-CH 2S(=0)CH 3 0 A-7480 H H H H H 0 CH=NOH H 2-CH 2S(=0) 2 CH3 0 A-7481 H H H H H 0 CH=NOH H 2-(benzy bxy) 0 A-7482 H H H H H 0 CH=NOH H 2-NH 2 0 A-7483 H H H H H 0 CH=NOH H 2-NH M e 0 A-7484 H H H H H 0 CH=NOH H 2-N (M e) 2 0 A-7485 H H H H H 0 CH=NOH H 2-(1,3-dbxolan-2-yD 0 A-7486 H H H H H 0 CH=NOH H 2-(1,3-dbxan-2-yl 0 A-7487 H H H H H 0 CH=NOH H 2-(1H--m idazol-2-yD 0 A-7488 H H H H H 0 CH=NOH H 2-(thiazol-2-y) 0 A-7489 H H H H H 0 CH=NOH H 2-(oxazol-2-yl 0 A-7490 H H H H H 0 CH=NOH H 2-CH= NOH 0 A-7491 H H H H H 0 CH=NOH H 2-CH= NOM e 0 A-7492 H H H H H 0 CH=NOH H 2-(4,5-dihydro-3-soxazolyD 0 A-7493 H H H H H 0 CH=NOH H 2-CN 0 A-7494 H H H H H 0 CH=NOH H 2-N0 2 0 A-7495 H H H H H 0 CH=NOH H 2-F,6-C| 0 A-7496 H H H H H 0 CH=NOH H 2-F,6-M e 0 A-7497 H H H H H 0 CH=NOH H 3-F,6-M e 0 A-7498 H H H H H 0 CH=NOH H 4-F,2-M e 0 A-7499 H H H H H 0 CH=NOH H 2-F,6-0Me 0 A-7500 H H H H H 0 CH=NOH H 3-F,6-0Me 0 A-7501 H H H H H 0 CH=NOH H 2,6-Cl2 0 A-7502 H H H H H 0 CH=NOH H 2-CI,6-M e 0 A-7503 H H H H H 0 CH=NOH H 3-CI,6-M e 0 A-7504 H H H H H 0 CH=NOH H 4-CI,2-M e 0 A-7505 H H H H H 0 CH=NOH H 2-Clb-GC 3 0 A-7506 H H H H H 0 CH=NOH H 2-CI,6-CF 3 0 A-7507 H H H H H 0 CH=NOH H 2-C1,6-0Me 0 A-7508 H H H H H 0 CH=NOH H 3-C1,6-0Me 0 A-7509 H H H H H 0 CH=NOH H 4-CI,2-0Me 0 A-7510 H H H H H 0 CH=NOH H 2,4-M e 2 0 A-7511 H H H H H 0 CH=NOH H 2,b-M e 2 0 A-7512 H H H H H 0 CH=NOH H 2,6-M e 2 0 A-7513 H H H H H 0 CH=NOH H 2-Me,4-CF3 0 A-7514 H H H H H 0 CH=NOH H 2-Me,b-CF 3 0 A-7515 H H H H H 0 CH=NOH H 2-Me,6-CF 3 0 A-7516 H H H H H 0 CH=NOH H 2-M e,4-0Me 0 A-7517 H H H H H 0 CH=NOH H 2-M e,5-OMe 0 A-7518 H H H H H 0 CH=NOH H 2-M e,6-OMe 0 A-7519 ifH HfHFf0 CH=NOH H 3-M e,6-OMe 0
[0258]
[Table 133]
com pound RI R2 R R R A R R' (R)m P A-7520 H H H H H 0 CH=NOH H 4-M e,2-0Me 0 A-7521 H H H H H 0 CH=NOH H 2,5-0M e 2 0 A-7522 H H H H H 0 CH=NOH H 2,6-0Me 2 0 A-7523 H H H H H 0 CH=NOH H 2-0Me,6-G 3 0 A-7524 H H H H H 0 CH=NOH H 2-CHF 2,5-F 0 A-7525 H H H H H 0 CH=NOH H 2-CHF 2,6-F 0 A-7526 H H H H H 0 CH=NOH H 2-CHF 2,5-Me 0 A-7527 H H H H H 0 CH=NOH H 2-CHF 2,6-Me 0 A-7528 H H H H H 0 CH=NOH H 2-cycbpropyl,5-F 0 A-7529 H H H H H 0 CH=NOH H 2-cycbpropyl,6-F 0 A-7530 H H H H H 0 CH=NOH H 2-cyclopropyl,5-Me 0 A-7531 H H H H H 0 CH=NOH H 2-cyclopropyl,6-Me 0 A-7532 H H H H H 0 CH=NOH H 2-ethenyl,6-F 0 A-7533 H H H H H 0 CH=NOH H 2-ethenyl,6-M e 0 A-7534 H H H H H 0 CH=NOH H 2-0Et,5-F 0 A-7535 H H H H H 0 CH=NOH H 2-0 Et,6-F 0 A-7536 H H H H H 0 CH=NOH H 2-0Et,5-CI 0 A-7537 H H H H H 0 CH=NOH H 2-0Et,6-CI 0 A-7538 H H H H H 0 CH=NOH H 2-0Et,5-Me 0 A-7539 H H H H H 0 CH=NOH H 2-0Et,6-Me 0 A-7540 H H H H H 0 CH=NOH H 2-0CHF2,5-F 0 A-7541 H H H H H 0 CH=NOH H 2-0CHF 2,6-F 0 A-7542 H H H H H 0 CH=NOH H 2-OCHF 2 ,5-Me 0 A-7543 H H H H H 0 CH=NOH H 2-0CHF 2 ,6-Me 0 A-7544 H H H H H 0 CH=NOH H 2-(cycbpropy loxy),5-F 0 A-7545 H H H H H 0 CH=NOH H 2-(cycobpropy loxy),6-F 0 A-7546 H H H H H 0 CH=NOH H 2-(cyclopropyoxy),5-M e 0 A-7547 H H H H H 0 CH=NOH H 2-(cyclopropyoxy),6-M e 0 A-7548 H H H H H 0 CH=NOH H 2-SMe,5-F 0 A-7549 H H H H H 0 CH=NOH H 2-SMe,6-F 0 A-7550 H H H H H 0 CH=NOH H 2-SMe,5-Me 0 A-7551 H H H H H 0 CH=NOH H 2-SMe,6-Me 0 A-7552 H H H H H 0 CH=NOH H 2-S (=0)M e,5-F 0 A-7553 H H H H H 0 CH=NOH H 2-S (=0)M e,6-F 0 A-7554 H H H H H 0 CH=NOH H 2-S(=0)Me,5-Me 0 A-7555 H H H H H 0 CH=NOH H 2-S(=0)Me,6-M e 0 A-7556 H H H H H 0 CH=NOH H 2-S(=O) 2Me,b-F 0 A-7557 H H H H H 0 CH=NOH H 2-S(=0) 2Me,6-F 0 A-7558 H H H H H 0 CH=NOH H 2-S(=0) 2 Me,5-M e 0 A-7559 H H H H H 0 CH=NOH H 2-S(=0) 2 Me,6--M e 0 A-7560 H H H H H 0 CH=NOH H 2-SC1`,5-F 0 A-7561 H H H H H 0 CH=NOH H 2-SCF 3 ,6-F 0 A-7562 H H H H H 0 CH=NOH H 2-SCF 3 ,b-M e 0 A-7563 H H H H H 0 CH=NOH H 2-SCF 3 ,6-M e 0 A-7564 H H H H H 0 CH=NOH H 2-S (=O)C%,b-F 0 A-7565 H H H H H 0 CH=NOH H 2-S3(=O0 3 ,6-F 0 A-7566 H H H H H 0 CH=NOH H 2-S(=0)CF 3 ,5-M e 0 A-7567 H H H H H 0 CH=NOH H 2-S(=0)CF 3 ,6-Me 0 A-7568 H H H H H 0 CH=NOH H 2-S(=0) 2CF3,5-F 0 A-7569 H H H H H 0 CH=NOH H 2-S(=0) 2CF 3 ,6-F 0 A-7570 H H H H H 0 CH=NOH H 2-S(=0) 2 CF3 ,5 -M e 0 A-7571 H H H H H 0 CH=NOH H 2-S(=O) 2CF 3 ,6-Me 0 A-7572 H H H H H 0 CH=NOH H 2-(cycbpropylthb),5-F 0 A-7573 H H H H H 0 CH=NOH H 2-(cycobpropylthb),6-F 0 A-7574 H H H H H 0 CH=NOH H 2-(cycobpropylthio),5-M e 0 A-7575 H H H H H 0 CH=NOH H 2-(cycobpropylthio),6-M e 0 A-7576 H H fFH H 0 CH=NOH H 2-C(=0)Me,5-F 0
[0259]
[Table 134]
com pound R' R2 R R A R R' (R)m p A-7b7/ H H H H 0 CH=NOH H 2-G(=0)Me,6-F 0 A-/b/8 H H H H 0 CH=N0H H 2-O(=U)Me,b-Me A-//9 H H H H 0 CH=N0H H 2-O(=0)Me,6-Me A-7b80 H H H H i 0 CH=NUH H 2-GH 2UHb-H A-/b81 H H H H 0 CH=N0H H 2-GH 20H,6-F 0 A-7582 H H H H 0 CH=N0H H 2-0H 20H, b-M e 0 A-7583 H H H H 0 CH=N0H H 2-0H 20H,6 -Me 0 A-7584 H H H H 0Di CH=N0H H 2-GH 20H 3 ,4-F 0 A-7bb H H H H H 0 CH=N0H H 2-GH 20H 3 ,b-F 0 A-7586 H H H H 0 CH=N0H H 2-GH 20H 3,6- 0 A-/587 H H H H i 0 CH=NUH H Z-GH 2UGH 3 ,4-e 0 A-b88 H H H H 0 CH=N0H H Z-GH 2UGH 3 ,b-e A-7589 H H H H H CH=NUH H Z-GH 2UGH 3 ,6-e 0 A-7590 H H H H 0 CH=N0H H 2-U0(=U)0H 3 ,b-F 0 A-7591 H H H H 0 CH=N0H H 2-0(=0)CH 3 ,6-F 0 A-7592 H H H H H CH=NUH H 2-00(=0)CH 3 ,b-e 0 A-7593 H H H H H CH=NUH H -U(=U)GH 3,6-Me 0 A-7594 H H H H 0 CH=N0H H 2-OS(=0) 2CH 3,b-F 0 A-7595 H H H H 0 CH=N0H H -US(=U) 20 3 6-- 0 A-7596 H H H H 0 CH=N0H H 2-OS(=0) 2CH 3,b-M e 0 A-/597 H H H H 0 H=N0H H 2-OS(=0) 2CH 3,6-M e 0 A-7598 H H H H f0 0H=NUH H 2-GH 2 S0H 3 ,b-F 0 A-7599 H H H H 0 0H=N0H H 2-GH 2 S0H 3 ,6-F 0 A-7600 H H H H f0 0H=NUH H 2-GH 2S0H 3,b-Me 0 A-7601 H H H H f0 0H=N0H H 2-OH 2 S3,6-Me 0 A-7602 H H H H f0 0H=N0H H 2-NMe 2 ,b-H A-7603 H H H H f0 0H=N0H H 2-NM e 2 ,6-F 0 A-7604 H H H H i 0 0H=N0H H 2-NMe 2 ,b-MAe 0 A-7605 H H H H 0 0H=N0H H 2-NMe 2 ,6-Me 0 A-7606 H H H H 0 0H=N0H H 2-ON,4-F 0 A-7607 H H H H 0 0H=N0H H 2-Nb-F 0 A-7608 H H H H 0 CH=N0H H 2-N,6-F 0 A-7609 H H H H H 0 0H=N0H H 2-ON,6-M e 0 A-7610 H H H H 0 H=N0H H 2-ON,b-OMe 0 A-7611 H H H H 0 0H=N0H H 2-ON,6-OMe 0 A-7612 H H H H 0 H=N0H H 3-ON,6-M e 0 A-7613 H H H H f0 0H=NUH H 3-ON,6-OMe 0 A-7614 H H H H D 0 H=N0H H 4-ON,2-Me 0 A-761b H H H H 0 0H=N0H H 4-ON,2-OMe 0 A-7616 H H H H H 0 0H=N0H H 2-N0 2 ,4-F 0 A-7617 H H H H 0 0H=N0H H 2-N0 2,b-F 0 A-7618 H H H H 0 0H=N0H H 2-N0 2 ,64 0 A-7619 H H H H f0 0H=NUH H 2-NU 2,4-MAe 0 A-7620 H H H H H 0 H=NUH H 2-N0 2,b-MAe 0 A-7621 H H H H 0 H=N0H H -NU 2,6- e A-7622 H H H H 0 H=NUH H -e,4,b-H 2 0 A-7623 H H H H 0 0H=N0H H 2-Me,6-Et 0 A-7624 H H H H 0 0H=N0H H 2-cyclopropyl,6-OMe 0 A-762b H H H H 0 0H=N0H H 2-Me,b-Et 0 A-7626 H H H H Hi0 0H=N0H H 2,6-Et 2 0 A-7627 H H H H 0 CH=N0H H 2-Et,6-F 0 A-7628 H H H H Hi0 0H=N0H H Z-GH 2UGH 3,-I 0 A-7629 H H H H Hi0 0H=N0H H Z-GH 2 UGH 2 0 3 -- I 0 A-7630 H H H H D 0 H=N0H H 2-OH2NMe2 0 A-7631 I H iHH H H 0 H=N0H 2CH 3 H H 0 A-7632 H H H H =NOECH 2 CH 3 H 2-F 0 A-7633 H H 7iH Hi0 H=N0H 2CH 3 H 2-CI 0
[0260]
[Table 135]
com pound R' R2 R R A R R' (R)m p A-7634 H H H H 0 CH=NUCH 2CH 3 H 2-Br 0 A-7635 H H H H H0f CH=NCH 2 CH 3 H 2-UH A-7636 H H H H D CH=NCH 2CH 3 H 2-M e A-7637 H H H H i 0 CH =N0CH 2 CH 3 H 2-Et 0 A-7638 H H H H D CH=NCH 2CH 3 H 2-Pr 0 A-7639 H H H H D CH= NCH 2CH 3 H 2-CF 3 0
A-7640 H H H H D CH=NCH 2CH 3 H 2-HF 2 0
A-7641 H H H H D CH= NCH 2CH 3 H 2-CH 2F 0
A-7642 H H H H H 0 CH=NCH 2CH 3 H 2-0F 201 0 A-7643 H H H H D CH=NOCH CH3 H 2-cycbpropyl W A-7644 H H H H i 0 CH=N0CH 2 CH 3 H 2-cycobbutyl 0 A-7645 H H H H D CH=NOCH CH3 H 2-cycbpentyl 0 A-7646 H H H H CH=NOCH 2 C 3 H 2-ethenyl 0 A-7647 H H H H iff CH=NCH2CH3 H 2-allyl 1 A-7648 H H H H D CH=NCH 2CH 3 H 2-(prop-1-en-1-yD 0 A-7649 H H H H i 0 CH2=3NOHC H 2-(trifloroetheny 0 A-7650 H H H H f0 CH2=3NOHC H 2-UMe A-7651 H H H H 0 CH=NCH 2CH 3 H 2-OEt A-7652 H H H H f0 CHNC 2 CH 3 H 2-OPr 0 A-7653 H H H H 0 CH=NCH 2CH 3 H 2-0 (/-Pr) 0 A-7654 H H H H H CH=NCH 2CH 3 H 2-0G3 0 A-7655 H H H H H0f CH=NCH 2 CH 3 H 2-CHF 2 0 A-7656 H H H H D CH=NCH 2CH 3 H 2-(cycbpropybxy) 0 A-7657 H H H H iff CH=NCH2CH 3 H 2-(cycobbutyloxy) 0 A-7658 H H H H H HIOCH 2CH 3 H 2-(cycbpentybxy) A-7659 H H H H iDii f OHNC2CHF H 2-((2,2-dichbrocycbpropyI)oxy) 0 A-7660 H H H H H D H0NOC 2 3 H 2-(oxiran-2-yD A-7661 H H H H Hif 0 CH=NCH 2CH 3 H 2-SMe 0 A-7662 H H H H D CH=NCH 2CH 3 H 3-SMe 0 A-7663 H H H H D CH=NCH 2CH 3 H 2-S(=0)Me 0 A-7664 H H H H D CH=NCH 2CH 3 H 3-S(=0)Me 0 A-7665 H H H H iff CH=NCH2CH3 H 2-S(=0) 2Me 0 A-7666 H H H H H CH=NCH 2CH 3 H 3-S(=0) 2 Me 0 A-7667 H H H H Hi0 CH =N0CH 2CH 3 H 2-SCF 3 0 A-7668 H H H H D CH=NCH 2CH 3 H 3-SC3 0 A-7669 H H H H D CH=N0CH 2CH H 3-S(=U)GH 3 0
A-7670 H H H H H 0 CH =N0CHf 2 CH 3 H 3-SCF(GH 3) 2 0 A-7671 H H H H D CH=NCH 2CH 3 H 2-(cycbpropylthio) 0 A-7672 H H H H D CH=NCH 2CH 3 H 2-(cycbpropylsufinyD 0 A-7673 H H H H H 0 CH= NCH 2CH 3 H 2-(cycbpropy u fony D 0 A-7674 H H H H D CH=NCH 2CH 3 H 2-C(=0)Me 0 A-7675 H H H H D0f CH=NCH 2 CH 3 H 2-GH 2 0(=U)CH 3 0
A-7676 H H H H CH= NOCHT2CH 3 H 2-GH 2 0(=U)GF 3 0 A-7677 H H H H f0 CH=N0CH 2CH 3 H 2-CH 2 H 0 A-7678 H H H H Df0fFM = 2CH3 H 2-GH 20H3 0
A-7679 H H H H Hi0 NOC 2 CH 3 H 2-GH 20H 20H 3 0
A-7680 H H H H D CH=NCH 2CH 3 H 2-CH 2SCH 3 0 A-7681 H H H H D CH=NCH 2CH 3 H 2-CH 2S(=0)CH 3 0
A-7682 H H H H D CH=NCH 2CH 3 H 2-CH 2S(=0) 2 CH 3 0
A-7683 H H H H f0 HNOFCH 2CHI 3 H 2-(benzybxy) 0 A-7684 H H H H 0 CH=NCH 2CH 3 H 2-NH 2 A-7685 H H H H f0 CHNC 2CH 3 H 2-NHMe 0 A-7686 H H H H f0 2H3NOHC H 2-N (M2 )
A-7687 H H H H 0 CH=NCH 2CH 3 H 2-(1,3-dbxolan-2-yD 0 A-7688 IfH H H H H CH=NCH 2CH 3 H 2-(1,3-dloxan-2-yD 0 A-7689 H H H H i fiiii0 =7NO 2H 3 H 2-(lH- idazol-2-yD 0 A-7690 H H fH H 0 H=NUGH 2CH 3 H 2-(thiazol-2-y1) 0
[0261]
[Table 136]
com pound R' R2 R R A R R' (R)m p A-/691 H H H H if CH=NCH 2CH 3 H 2-(oxazol-2-yD 0 A-/692 H H H H H CH=NCH 2CH 3 H 2-GH=NUH0 A-/693 H H H H D CH=NCH 2CH 3 H 2-CH=NOMe A-/694 H H H H i 0 CH=N0CHf 2 CH3 H 2-(4,b-dihydro-3-IsoxazolyD A-/695 H H H H D 0 if 0 H=NCH2CH3H 2-ON 0 A-/696 H H H H D CH=NCH 2CH 3 H 2-NO 2 0
A-/69/ H H H H D0 H CH=NCH2CH3 H 2-F,6-GI 0 A-/698 H H H H D CH=NCH 2CH 3 H 2-F,6-Me 0 A-/699 H H H H H 0 CH=NCH 2CH 3 H 3-F,6-M e 0 A-//00 H H H H D CH=NOCH CH3 H 4-F,2-Me 0 A-//0l H H H H 0 CH=N0CH 2 CH 3 H 2-F,6-UMe A-//02 H H H H D CH=NOCH CH3 H 3-F,6-0Me 0 A-//03 H H H H CH=N0CH 2 C 3 H 2,6-C 2 A-//04 H H H H D CH=N CH 2CH 3 H 2-GI,6-Me 0 A-//05 H H H H iff CH=NCH2CH3 H 3-GI,6-Me 0 A-//06 H H H H f0 CH2=3NOHC H 4-GI,2-Me 0 A-//0/ H H H H Hi0 CH= 3NOHC H Z-GIb-c 3 0 A-/08 H H H H 0 CH=NCH 2CH 3 H 2-GI,6-GF 3 0 A-//09 H H H H f0 CHD OC 2 CH 3 H 2-IL6-UMe 0 A-/10 H H H H 0 CH=NCH 2CH 3 H 3-GI,6-0Me 0 A-/ll H H H H f0 CH=NCH 2CH 3 H 4-GI,2-UMe 0 A-/12 H H H H 0 CH=NCH 2CH 3 H 2,4-M e 2 0 A-/13 H H H H D CH=NCH 2CH 3 H 2,b-M e 2 0 A-/14 H H H H 0 CH=NCH 2CH 3 H 2,6-M e 2 0 A-ill ifiHifiHf0 CH=NOCHCH I3 H 2-M e,4-CF 3 A-/16 H H H H CH=NOCH CH3 H 2-M e,b-CF 3 A-iil7 H H H H ifiHifi f CH2C 3 H 2-M e,6-CF 3 0 A-/1i8 H H H H Hif 0 CH=NCH 2CH 3 H 2-M e,4-UMe 0 A-i19 H H H H D CH=NCH 2CH 3 H 2-M e,b-0Me A-ii2 0 H H H H D CH=NCH 2CH 3 H 2-Me,6-0Me 0 A-ii21 H H H H CH=NCH 2CH 3 H 3-Me,6-0Me 0 A-ii22 H H H H D CH=NCH 2CH 3 H 4-Me,2-0Me A-ii23 H H H H H 0 CH=NCH 2CH 3 H 2,b-UMe 2 0 A-ii24 H H H H H 0 CH =N0CHf 2 CH 3 H 2,6-UMe 2 0 A-i2b H H H H f CH=NCH 2CH 3 H 2-OMe,6-F 3 0 A-ii26 H H H H D CH=N0CH 2 CH H Z-GHH 2 ,- 0
A-ii2i H H H H Hi 0HIFfNO 2 ICH3 H 2-CHF 2,6- 0 A-ii28 H H H H 0 CH=NCH 2CH 3 H 2-0HF 2,b-Me 0 A-ii29 H H H H 0 CH=NCH 2CH 3 H 2-0HF 2,6-Me 0 A-ii30 H H H H H 0 CH=NCH 2CH 3 H 2-cycbpropylb-F 0 A-i31 H H H H 0 CH=NCH 2CH 3 H 2-cycbpropyl,6-F 0 A-ii32 H H H H 0 CH=NCH 2CH 3 H 2-cyclopropylb-Me 0 A-ii33 H H H H H CHN0CH 2 CH 3 H 2-cyclopropyl,6-M e 0 A-ii34 H H H H H CHN0CH 2 CH 3 H 2-ethenyl,6-F 0 A-ii3b H H H H f Di CHNC 2CH 3 H 2-ethenyl,6-Me 0 A-ii36 H H H H Hi0 CHNC 2CH 3 H 2-UEt,b-F A-i3i H H H H 0 CH=NCH 2CH 3 H 2-OEt,6-F 0 A-ii38 H H H H 0 CH=NCH 2CH 3 H 2-0Et,b-Cl 0 A-ii39 H H H H 0 CH=NCH 2CH 3 H 2-0Et,6-GI 0 A-ii40 H H H H i fiiii0 NNO 2C3 H 2-UEt,b-M e 0 A-i41 H H H H 0 CH=NCH 2CH 3 H 2-0Et,6-Me 0 A-ii42 H H H H Hi0D =NO 2 H3 H 2-CHH2b-F A-ii43 H H H H Hi0 C 3 2H=NO H Z-UHF 2 ,6-F A-ii44 H H H H D CH=NCH 2CH 3 H 2-CHF 2 ,b-Me 0 A-ii45 H H H H 0 CH=NCH 2CH 3 H 2-CHF 2 ,6-Me 0 A-ii46 H H H H 0 NH OICHfI 2CH 3 H 2-(cyclopropyloxy),b-F A-/i/4i H FH Hi0 CH=NUCH 2CH 3 H 2-(cyclopropyloxy),6-F 0
[0262]
[Table 137]
com pound R' R2 R R A R R' (R)m p A-//48 H H HH i 0 CH=NUCH 2CH 3 H 2-(cyclopropybxy),b-Me 0 A-//49 H H H H H CH=N CH 2CH 3 H 2-(cyclopropybxy),6-M e A-//b0 H H H H 0 CH=NUCH 2CH 3 H 2-SMe,b-F W A-J/bl H H H H f0 CH=N0CHf 2CH 3 H 2-SMe,6-F 0 A-//52 H H H H D if 0 CH=N0H2CH3 H 2-SMe,b-Me 0 A-//53 H H H H D if 0 CH=N0H2CH3 H 2-SMe,6-M e 0 A-//54 H H H H D 0 H= N0H2CH3 H 2-S(=0)Me,b-F 0 A-bb H H H H D H= NU 0CH2CH3 H 2-S(=0)Me,6-F 0 A-//56 H H H H H 0 CH=N0H 2CH 3 H 2-S(=0)Me,b-M e 0 A-Jib/ H H H H D CHNOCH 2 CH 3 H 2-S(=0)Me,6-Me A-//b8 H H H H CHNCH 2CH 3 H 2-S(=U) 2Me,b-H 0 A-/759 H H H H CHNOCHCH 3 H 2-St=U) 2Me,6-F 0 A-//60 H H H H H H 2-S(=U) 2 Me,b-M e 0 A-//61 H H H H D CH=N0H 2 CH 3 H 2-S(=0) 2 Me,6--M e 0 A-//62 H H H H D CH=N0H 2 CH 3 H 2-SCG3,b-F 0 A-//63 H H H H H 0i 0 CH=NH 2 H3 H 2-SCF 3 ,6-F 0 A-//64 H H H H f0 2H3NOH H Z-GH 3,b-me A-/65 H H H H f CH=N0H 2 CH 3 H 2-SGF 3 ,6-M e 0 A-//66 H H H H Hi0D HNO 2 H3 H 2-S(=O)GH 3,b-H 0 A-//6/ H H H H 0 CH=N0H 2CH 3 H 2-S(=U)0F 3 ,6-F 0 A-//68 H H H H H CH=N0H 2CH 3 H 2-S(=U)HF 3 ,b-M e 0 A-//69 H H H H H CH=N0H 2CH 3 H 2-S (=0)0F 3 ,6-M e 0 A-/0 H H H H 0 CH=N0H 2CH 3 H 2-S(=U) 20F 3 ,b-F 0 A-//l H H H f0 H CH=N0H 2 CH 3 H 2-S(=0) 0F 3 ,6-F 2 0 A-///2 H H H H H CH=NOCH 2 CH37I H 2-S(=U) 2CF 3 ,b-e A-///3 H H H H F CH=NOCH 2 CH H 2-S(=U) 2CF 3 ,6-Me A-///4 H H H H CH=N0CH 2 C 3 H 2-(cycbpropylthb),b-F 0 A-///b H H H H Hif 0 CH=N0H 2CH 3 H 2-(cycobpropylthb),6-F 0 A-///6 H H H H D CH=N0 H 2CH 3 H 2-(cycbpropylthio),b-M e 0 A-//// H H H H iff CH=N0H 2CH3 H 2-(cycbpropylthio),6-M e 0 A-///8 H H H H D CH=N0H 2CH 3 H 2-C(=0)Me,b-F 0 A-///9 H H H H D CH=N0H 2CH 3 H 2-C(=0)Me,6-F 0 A-//80 H H H H 0 if 0 H=N0H2CH3 H 2-C(=U)Me,b-Me 0 A-i/8J1 H H H H f0 CH=N0CH 2 CH 3 H 2-C(=U)Me,6-Me 0 A-//82 H H H H D CH=N0H 2CH 3 H 2-CH 20H,b-F 0 A-//83 H H H H D CH=N0CH 2 CH H 2-CH 2UN,6-F A-//84 H H H H H 0 CI=FFiLNOC 2 C 3 H 2-CH 2 H,b-M e 0 A-/8b H H H H 0 CH= N0H 2CH 3 H 2-0H 20H,6 -Me 0 A-i/86 H H H H D CH=N0H 2CH 3 H 2-CH 20H 3 ,4-F 0 A-//8/ H H H H H 0 CH=N0H 2CH 3 H 2-CH 20H 3 ,b-F 0 A-//88 H H H H 0 CH=N0H 2CH 3 H 2-CH 20H 3 ,6-F 0 A-//89 H H H H D CH=N0H 2CH 3 H 2-CH 20CH 3 ,4-Me 0 A-//90 H H H H CHI=@NO CH 2CH 3 H 2-CH 2UCH 3 ,b-M e 0 A-//91 H H H H CHI=NO CH 2CH 3 H 2-CH 2 CH 3 ,6-M e 0 A-//92 H H H H D CH=O 2HCH 3 H 2-C(=U)GH 3,5-F 0 A-//93 H H H H H H0C 2 H3 H Z-UG(=U)GH 3, A-//94 H H H H D CH=N0H 2CH 3 H 2-UC(=U)0H 3 ,b-M e 0 A-//95 H H H H iff CH=N0H2CH 3 H 2-UC(=U)0H 3,6-M e 0 A-//96 H H H H D CH=N0H 2CH 3 H 2-US(=0) 2 CH 3 ,b-F 0 A-//9/ H H H H i i0H=NH2CHI3 H 2-U S=U) 2CH3,6-F 0 A-i/98 H H H H D CH=N0H 2CH 3 H 2-OS(=U) 2CH 3,b-M e 0 A-//99 H H H H H HNOCH 2CH 3 H 2-US(=U) 2CH 3,6-M e 0 A-/800 H H H H Hi0 2H=NHH 3 H Z-GH 2 H 3,b-H 0 A-/801 H H H H 0 CH=N0H 2CH 3 H 2-CH 2 SCH 3 ,6-F 0 A-/802 H H H H H CH=N0H 2CH 3 H 2-CH 2SCH 3,b-M e 0 A-/803 H H H H H 0 HNffOCH 2CH 3 H 2-CH 2SCH 3,6-M e 0 A-/804 H H H H 0 CH=NUH 20H 3 H 2-NM e 2 ,b-F 0
[0263]
[Table 138]
com pound R' R2 R R A R R' (R)m p A-/80b H H H H D0 if 0 H=NCH2CH3 H 2-NMe2,6-F 0 A-7806 H H H H 0 CH=NCH 2 CH 3 H 2-NMe 2 ,b-Me 0 A-/80/ H H H H H CH=NCH2CH3 H 2-NMe2,6-Me 0 A-/808 H H H H f0 CH=NOH 2OH 3 H 2-CN,4-F 0 A-/809 H H H H D CH= NCH 2CH 3 H 2-CN,b-F 0 A-7810 H H H H D0f NCH 0H= 2CH 3 H 2-CN,6-F 0 A-7811 H H H H D CH=NCH 2CH 3 H 2-CN,6-M e 0 A-7812 H H H H D CH=NCH 2CH 3 H 2-GN5-0 Me 0 A-7813 H H H H H 0 CH=NCH 2CH 3 H 2-CN,6-0Me 0 A-7814 H H H H D 0 H=NOOH H 3-ON,6-Me 0 A-/815 H H H H i 0 CH= NOH 2OH 3 H 3-CN,6-UMe 0 A-/816 H H H H D 0 H=NOOH H 4-CN,2-M e 0 A-/817 H H H H H H 4-CN,2-OMe 0 A-/818 H H H H iff CH=NCH2CH3 H 2-N02,4-F 0 A-/819 H H H H D CH=NCH 2CH 3 H 2-N0 2 ,b-F 0 A-/820 H H H H H0 i 0=NH2OH3 H 2-N0 2,6-F 0 A-/821 H H H H f0 OH=3NH H -NU 2,4-Me A-/822 H H H H D CH=NCH 2CH 3 H 2-N0 2,b-MAe 0 A-/823 H H H H OH0NOO 2 OH 3 H 2-NU 2,6-MAe 0 A-/824 H H H H 0 CH=NCH 2CH 3 H 2-Me,4,b-F 2 0 A-82b H H H H 0 CH=NCH 2CH 3 H 2-Me,6-Et 0 A-/826 H H H H H CH=NCH 2CH 3 H 2-cyclopropyl,6-OMe 0 A-82/ H H H H 0 CH=NCH 2CH 3 H 2-Me,b-Et 0 A-/828 H H H H H0 CH=NCH 2CH 3 H 2,6-Et2 0 A-/829 H H H H H H=NOH 2OH 3 H 2-Et,6-F 0 A-/830 H H H H Hi0 O NO 2 OH 3 H 2-GH 20H 3,6-CI 0 A-/831 H H H H H H0O 2O 3 H Z-GH 2UGH 20H 3 ,6- 0
A-/832 H H H H i 0 CH=NCH 2CH 3 H 2-CH 2 NMe 2 0 A-/833 H H H H 0 =UHN (H 3) 2 H 0 A-/834 H H H H D0 =GHN (H 3) 2 2-F 0 A-/835 H H H H Df =GHN (GH 3) 2 2-Cl 0 A-/836 H H H H 0 =GHN (H 3) 2 2-Br 0 A-83/ H H H H f0 =GHN (H 3) 2 2-OH 0 A-/838 H H H H =N (CH 3) 2 2-M e 0 A-/839 H H H H 0 =OHN (H 3) 2 2-Et 0 A-/840 H H H H D =N (CH 3) 2 2-Pr 0 A-/841 H H H H Hf =CHN (CH3) 2 2-CF 3 0
A-/842 H H H H f Di =CHN (CH 3) 2 2-UHF 2 0
A-/843 H H H H 0 =OHN (H 3) 2 2-CH 2 0
A-/844 H H H H Di =NN(HCH3)2 2-GF20I 0 A-/845 H H H H 0 =OHN (H 3) 2 2-cycbpropyl 0 A-/846 H H H H D =N (CH 3) 2 2-cycobbutyl 0 A-/84/ H H H H =N ((H3) 2 2-cycbpentyl 0 A-/848 H H H H =N ((H3) 2 2-ethenyl1 A-/849 H H H H 0 =CHN (CH 3) 2 2-a lyl1 A-/850 H H H H =ifN (CH 3) 2 2-(prop-1-en-1-yD A-851 H H H H DI =IN (CH 3) 2 2-(trifLloroethenyl) 0 A-/852 H H H H 0 =GHN (H 3) 2 2-0Me 0 A-/853 H H H H D=N (H 3) 2 2-OEt 0 A-/854 H H H H 0 =HN (OH 3) 2 2-UPr 0 A-/8bb H H H H 0 =HN (OH 3) 2 2-0 (/-Pr) 0 A-/856 H H H H H0 =GHN (H 3) 2 2-0GF 3 0
A-/85/ H H H H Hi0 =CHN (CH 3) 2 2-UGHF 2 A-/8b8 H H H H 0 =CHN(CH 3) 2 2-(cycbpropybxy) 0 A-/859 H H H H f0 =CHN (CH 3) 2 2-(cycobbutybxy) 0 A-/860 IfH H H H 0 =GNN (CH 3) 2 2-(cycbpentybxy) 0 A-/861 ifi Hi f =GHN (OH 3) 2 2-((2,2-dichbrocycbpropyDoxy) 0
[0264]
[Table 139]
com pound R' R2 RR A R R' (R)m p A-7862 H H H H 0 =GHN (GH32 2-(oxiran-2-y D0 A-7863 H H H H H =GHN (H 3) 2 2-SMe 0 A-7864 H H H H 0 =CHN (H 3) 2 3-SMe 0 A-7865 H H H H i 0 =CHN (H 3) 2 2-S =O)Me 0 A-7866 H H H H D =GHN (H 3) 2 3-S(=O)Me 0 A-7867 H H H H 0 =GHN (H 3) 2 2-S(= D)Me 0 A-7868 H H H H 0 =GHN (H 3) 2 3-S(= D)Me 0 A-7869 'H H H H D 0 =GHN(H 3)2 2-SCF3 0 A-78/0 H H H H Ei 0 =GHN(H 3) 2 3-SCF 3 0 A-7871 H H H H EHi = CHN(H 3) 2 3-S (=0)CF 3 0 A-7872 H H H HWif =CHN (CH 3) 2 3-SCF(0F 3) 2 0 A-78/3 H H H H D i =CHN (CH 3)2 2-(cycbpropy bb) 0 A-7874 H H H H HH =N (CH 3)2 2-(cycbpropylsu fny) 0 A-/8/b H H H H Df = CHN (CH 3) 2 2-(cycbpropy bu Tony D 0 A-7876 H H H H - =GHN(OH 3) 2 2-O(=0)Me 0 A-/8// H H H H E =UHN (CH 3) 2 2-GH 2 0(= )GH 3 0 A-i8/8 H H H H E =CHN (CH 3) 2 2-GH 2G(= U)G 3 0 A-/8/9 H H H H 0 =GHN (H 3) 2 2-GH 2 UH 0 A-/880 H H H H Hf =CHN (CH 3) 2 2-0H 20H 3 0
A-/881 H H H H 0Di =GHN (H 3) 2 2-0H 20H 2CH 3 0
A-/882 H H H H H0 =CHN (CH 3) 2 2-OH 2SCH 3 0 A-/883 H H H H Hf =CHN (CH 3) 2 2-GH 2S = )CH 3 0 A-/884 H H H H Df =CHN (CH 3) 2 2-GH 2S(= U) 2 H 3 0
A-/88b H H H H i if =CHN(CH3)2 2-(benzybxy) 0 A-/886 H H H H if 0 =CHN(CH 3) 2 2-NH 2 A-/88/ H H H H f =GHN (H 3) 2 2-NHMe 0 A-/888 H H H H f =CHN (CH 3) 2 2 M e) 2 0 A-/889 H H H H i 0 =GHN (H 3) 2 2-(13-dioxo n-2-yD 0 A-/890 H H H H f Di =CHN (CH 3) 2 2-(1,3-d bxan-2-y D A-/891 H H H H DIi =GHN (H 3) 2 2-(1#-i idazoE2-yD 0 A-/892 H H H H D =GHN (H 3) 2 2-(thiazo -2-y) 0 A-/893 H H H H 0 =HN (H 3) 2 2-(oxazok2-y D A-/894 H H H H Hi0 =GHN (H 3) 2 2-GH= NUH 0 A-/895 H H H H f =CHN(CH 3) 2 2-OH=NUMe 0 A-/896 H H H H 0 =GHN (H 3) 2 2-(4,b-dihydro-3-isoxazoyD 0 A-/89/ H H H H E =CHN (CH 3) 2 2-N 0 A-/898 H H H H EH =CHN(CH 3 2 2-NO 2 0
A-/899 H H H H D0 =CHN (CH 3) 2 2-F,6-I1 0 A-/900 H H H H 0 =HN (H 3) 2 2-F,6-i e 0 A-/901 H H H H D i =N (CHH3)2 3-F,6-i e 0 A-/902 H H H H 0 =HN(OH 3) 2 4-F,2-i e 0 A-/903 H H H H Df =iN (CH 3) 2 2-F,6-0Me 0 A-/904 H H H H F =CHN (CH 3) 2 3-F,6-UMe 0 A-90b H H H H F =CHN(H 3) 2 2,6-C W A-/906 H H H H D =CHN (CH 3) 2 2- 1,6-M e 0 A-/90/ H H H H f =CHN(CH 3) 2 3-1,6-M e 0 A-/908 H H H H D =CHN (CH 3) 2 4- 1,2-M e 0 A-/909 H H H H 0 =GHN (H 3) 2 2-b1,5-F 3 0 A-/910 H H H H D =CN( H 3) 2 2-C1,6-0F 3 0 A-/911 H H H H 0 = HN (OH 3) 2 2- 1,6-0Me 0 A-/912 H H H H 0 = HN (H 3) 2 3- 1,6-0Me 0 A-/913 H H H f0 H =HN (H 3) 2 4-l,2-0Me 0 A-/914 H H H H 0CHN (CH E 3) 2 2,4-M e2 0
A-/91b H H H EH H =CHN(CH 3) 2 2,5-M e 2 0 A-/916 H H H fH =CHN(CH 3) 2 2,6-M e 2 0 A-/91/ H IHH H =UHN (CH E 3) 2 2- e,4-GF 3 0 A-/918 ifHHfHi =GHN (OH 3) 2 2-M e,b-GF 3
[0265]
[Table 140]
com pound R' R2 RR A R R' (R)m p A-/919 H H H H 0 =GHN (H3)2 2-Me,6-C 3 0 A-7920 H H H H F =OHN (H 3) 2 2-Me,4-UMe F A-7921 H H H H DH =N(OH3)2 2-Me,b-0Me A-7922 H H H H if =0N (GCH 3) 2 2-Me,6-OMe 0 A-7923 H H H H DH=N(OH3)2 3-Me,6-OMe 0 A-7924 H H H H 0 =OHN (H 3) 2 4-Me,2-0Me 0 A-7925 H H H H 0 =GHN (H 3) 2 2,b-UMe 2 0 A-7926 H H H H 0 =OHN (H 3) 2 2,6-UMe 2 0 A-/92/ H H H H 0 =OHN (H 3) 2 2-OMe,6-F 3 0 A-7928 H H H H D0 =GHN (CH 3)2 2-OH F2,5-F A-7929 H H HWif H =GHN (CH 3) 2 2-OHF 2,6-F 0 A-7930 H H H H 0 =GHN (CH 3) 2 2-OH F 2,- e 0 A-7931 H H H C=GHN (CH3)2 H 2-OHF2,6-M e 0 A-7932 H H H H DIi =CHN (CH 3) 2 2-cycbpropyl,b-F 0 A-7933 H H H H 0 =OHN (H 3) 2 2-cycbpropyl,6-F 0 A-7934 H H H H HH =N (CH 3)2 2-cycbopropylb-Me 0 A-7935 H H H H =N (CHH 3) 2 2-cycbpropyl,6-Me 0 A-7936 H H H H 0 =GHN (OH 3) 2 2-ethenyl,6-F 0 A-/93/ H H H H =NN (CH 3) 2 2-ethenyl,6-Me 0 A-7938 H H H H 0 =OHN (H 3) 2 2-OEt,b-F 0 A-7939 H H H H H0 =CHN (CH 3) 2 2-Et,6-F 0 A-7940 H H H H fH =CHN (CH 3) 2 2-UEtb-CI 0 A-7941 H H H H 0Di =CHN(CH 3) 2 2-OEt6-CI 0 A-7942 H H H H fN =i (CH3) 2 2-OEt,b-Me 0 A-7943 H H H H fN =i (CH3) 2 2-OEt,6-Me 0 A-7944 H H H H H0 =OHN (H 3) 2 2-UGHF 2,b-H 0 A-7945 H H H H 0 =CHN (CH 3) 2 2-UGHF 2,6-F 0 A-7946 H H H H i 0 =GHN (OH 3) 2 2-CHF 2 ,b-MAe 0 A-7947 H H H H f Di =CHN(CH 3) 2 2-CHF 2 ,6-MAe 0 A-7948 H H H H 0 =GHN (OH 3) 2 2-(cycbpropybxy),b-F 0 A-7949 H H H H 0 =GHN (OH 3) 2 2-(cycbpropybxy),6-F 0 A-7950 H H H H 0 =GHN (OH 3) 2 2-(cyclopropybxy),b-Me 0 A-7951 H H H H f0 =GHN (OH 3) 2 2-(cyclopropybxy),6-M e 0 A-7952 H H H H H=NN (CH3)2 2-SMe,b-F 0 A-7953 H H H H 0 =HN (OH 3) 2 2-SMe,6-F 0 A-7954 H H H H DH=N(CH3)2 2-SMe,b-Me 0 A-7955 H H H H fN =i (CH 3) 2 2-SMe,6-M e 0 A-7956 H H H H D =NN(CH 3) 2 2-S(=O)Me,b-F 0 A-/9b/ H H H H 0 =HN (OH 3) 2 2-S(=O)Me,6-F 0 A-958 H H H H DI =INN(CH 3) 2 2-S(=0)Me,b-M e 0 A-79b9 H H H H 0 =HN (OH 3) 2 2-S(=0)Me,6-M e 0 A-7960 H H H H 0Di =CHN(CH 3) 2 2-S(=U) 2 Me,b-F 0 A-7961 H H H H fN =i (CH 3) 2 2-S(=U) 2 Me,6-H 0 A-7962 H H H H H =NN (CH 3) 2 2-S(=U) 2 Me,b-M e 0 A-7963 H H H H 0Di =CHN (CH 3) 2 2-S t=U) 2 M e,6-6 e 0 A-7964 H H H H Hf =CHN (CH 3) 2 2-SCF 3 ,b-F A-796b H H H H DIi =UNN (CH 3) 2 2-SCF 3 ,6-F 0 A-7966 H H H H 0 =HN (OH 3) 2 2-SGF 3 ,b-Me 0 A-7967 H H H H DIi =CHN(CH 3) 2 2-SGF 3 ,6-Me 0 A-7968 H H H H 0 =GHN (H 3) 2 2-S=O)GF 3 ,b-H 0
A-7969 H H H H 0 =GHN (H 3) 2 2-S(=O)0F 3 ,6-F 0 A-9/0 H H H H 0 =GHN (H 3) 2 2-S=O)GF 3,b-me 0 A-/9/1 H H H H f0 =UHN (CH 3) 2 2-S =O)GF 3,6-M e A-7972 H H H H 0Di =CHN(CH 3) 2 2-S(=U) 20F 3 ,b-F 0 A-9/3 H H H H 0 =CHN (CH 3) 2 2-S(=U) 20F 3 ,6-F 0 A-7974 H H H H HDi =UHN (CH3)2 2-S=U) 2 CF 3 ,b-M e 0 A-797b H H FH H 0 =HN (OH 3) 2 2-S(=U) 2CF 3 ,6-M e 0
[0266]
[Table 141]
com pound R' R2 RR A R R' (R)m p A-7976 H H H H 0 =GHN (H32 2-(cyclopropylthb),b-F 0 A-/9// H H H H =OHN (H 3) 2 2-(cyclopropylthb),6-F 0 A-/9/8 H H H H D =CHN(H3) 2 2-(cycbpropythio),b-Me 0 A-/979 H H H i 0 H =CHN (CH3) 2 2-(cycbpropythb),6-M e 0 A-7980 H H H H D =NCHN(CH3) 2 2-G(=0)Me,b-F 0 A-7981 H H H H 0 =OHN (OH 3) 2 2-G(=0)Me,6-F 0 A-7982 H H H f H =OHN (OH 3) 2 2-G(=0)Me,b-Me 0 A-7983 H H H H 0 =OHN (OH 3) 2 2-0(=0)Me,6-Me 0 A-7984 H H H H 0 =OHN (H 3) 2 2-0H 2 0Hb-F 0 A-7985 H H H f H Di =CHN (CH 3) 2 2-CH 2UH,6-F A-7986 H H H H H=NN (CH3)2 2-H20H,b-Me 0 A-/98/ H H H f H Di =CHN(CH 3) 2 2-H 2 0H,6-M e 0 A-/988 H H H H 0 =CHN (CH 3) 2 2-H 2 0GH 3 ,4-F 0 A-7989 H H H H DIi =CHN (CH 3) 2 2-0H 20H 3 ,b-F 0 A-7990 H H H H 0 =GHN (H 3) 2 2-0H 20H 3 ,6-F 0 A-7991 H H H fHH =UHN ((H3) 2 2-CH 20H 3 ,4-M e 0 A-7992 H H H H =NN (CH3)2 H 2-CH20H3,b-M e 0 A-7993 H H H H 0 =HN (OH 3) 2 2-0H 20H 3,6-MAe 0 A-7994 H H H H 0 =CHN (CH 3) 2 2-0(=U)0H 3,b-H 0 A-7995 H H H H 0 =GHN (H 3) 2 2-0(=U)0H 3 ,6-F 0 A-7996 H H H H =N (CH 3) 2 2-0(=U)CH 3 ,b-M e 0 A-/997 H H H H =HN (0H3) 2 2-0 (=U)0H 3 ,6-M e 0 A-/998 H H H f H Di =CHN(H 3) 2 2-OS(=U) 0H 2 3 ,b- 0 A-/999 H H H H =CHN (H 3) 2 2-OS(=U) 2 CH 3 ,6-F 0 A-8000 H H H H =f0N ((H3) 2 2-US(=0) 0H 2 3,b-Me 0 A-8001 H H H H 0 =GHN (H 3) 2 2-US(=0) 0H 2 3,6-Me 0 A-8002 H H H f0H =CHN (CH 3) 2 2-CH 2SCH 3 ,b-H 0 A-8003 H H H H i 0 =GHN (H 3) 2 2-GH 2 SOH 3 ,6-F 0 A-8004 H H H H f Di =CHN (CH 3) 2 2-OH 2S0H 3,b-Me 0 A-800 H H H H 0 =HN (OH 3) 2 2-OH 2S0H 3,6-Me 0 A-8006 H H H H 0 =HN (OH 3) 2 2-NM e 2 ,b-F A-800/ H H H H 0 =HN (OH 3) 2 2-NM e 2 ,6-F 0 A-8008 H H fH H 0 =HN(OH3)2 2-NMe2,b-M e 0 A-8009 H H H H =fN (CH 3) 2 2-NM e 2 ,6-M e 0 A-8010 H H H H =GHN (H 3) 2 0 2-0N,4-F F A-8011 H H =N ((H3) 2 H H 2-0N,b-F 0 A-8012 H H H H H=CN (H 3) 2 2-0N,6-F 0 A-8013 H H H H D =N (CH 3) 2 2-ON,6-Me 0 A-8014 H H H H 0 =HN (OH 3) 2 2-0N,b-0Me 0 A-801b H H H H Di =NN(HCH3)2 2-0N,6-0Me 0 A-8016 H H H H 0 =HN (OH 3) 2 3-GN,6-M e 0 A-801/ H H H H Df =iN (CH 3) 2 3-0N,6-0Me 0 A-801 8 H HH H =N (CH 3) 2 4-ON,2-Me 0 A-8019 H H H H H =UNN (CH 3) 2 4-0N,2-UMe 0 A-8020 H HH H 0Di =CHN (CH 3) 2 2-N0 2 14-F 0 A-8021 H H H Hf H =CHN (CH 3) 2 2-N0 2,b-F A-8022 H HH H DIi =CHN (CH 3) 2 2-N0 2 ,6-F 0 A-8023 H HH 0 H =GHN (OH 3) 2 2-N0 2,4-MAe 0 A-8024 H HH H DIi =CHN (CH 3) 2 2-N0 2,b-Me 0 A-8025 H HH 0 H =GHN (H 3) 2 2-N0 2,6-MAe 0 A-8026 H HH 0 H =HN (OH 3) 2 2-Me,4,b-F 2 0 A-802] H HH H =GHN (OH 3) 2 2-Me,6-Et 0 A-8028 H HH H =CHN (CH 3) 2 2-cyclopropyl,6-OMe 0 A-8029 H H H H D =N (CH 3) 2 2-Me,b-Et 0 A-8030 H H H H Hi0 =CHN (CH 3) 2 2,6-Et2 0 A-8031 fN H H H H H0 =i (C H3)2 2-Et,6-F 0 A-8032 H H H H =GHN (OH 3) 2 2-GH 20H 3 ,6-G1 0
[0267]
[Table 142]
com pound R' R2 RR A R R' (R)m p A-8033 Hi- H H H 0 =GHN (GH3)2 2-0H 20H 2CH 3 ,6-CI 0 A-8034 H H H H H=HN (GH3)2 2-CH2NMe2 0 A-8035 H H H H 0 OH 3 OH 3 H F A-8036 H H H H OGH3 T73 2-F 0 A-803/ H H H H D OH 3 OH 3 2-C 0 A-8038 H H H H D OH 3 OH 3 2-Br 0 A-8039 H H H H D OH 3 OH 3 2-OH 0 A-8040 H H H H D OH 3 OH 3 2-M e 0 A-8041 H H H H H 0 OH 3 OH 3 2-Et 0 A-8042 H H H H O GH3 TW3 2-Pr 0 A-8043 H H H H O GH3 TW3 2-03 0 A-8044 H H H H O GH3 T3 2-UHF2 F A-8045 H H H H OH 3 T3 2-H 2F 0 A-8046 H H H H 0 OH 3 OH 3 2-F2G1 0 A-804/ H H H H 0 OH 3 OH 3 2-cycbpropyl 0 A-8048 H H H H 0 H3 C3 2-cycobbutyl 0 A-8049 H H H H O GH3 CH3 2-cycbpentyl 0 A-80b0 H H H H 0 OH 3 OH 3 2-ethenyl1 A-80b1 H H H H 0 H3 C3 2-ally I A-8052 HfH f HH O H3 OH3 2-(prop-1-en-1-y) 0 A-8053 H H H H O0H3 OH3 2-(trffbioroethenyD 0 A-8054 H H H H O 0H3 OH3 2-UMe 0 A-80bb H H H H 0 OH 3 OH 3 2-OEt A-8056 H H H H O 0H3 OH3 2-UPr 0 A-805/ H H H H F OH 3 CH3 2-0 (/-Pr) 0 A-8058 H H H H H GH 3 TW3 2-0G 3 F A-8059 H H H H Hi OH3 MT3 2-GHF2 0
A-8060 H H H H i 0 OH 3 OH 3 2-(cycbpropybxy) 0 A-8061 H H H H 0 OH 3 OH 3 2-(cycobbutyloxy) 0 A-8062 H H H H 0 OH 3 OH 3 2-(cycbpentybxy) 0 A-8063 H H H H 0H 3 OH3 2-((2,2-dichbrocycbpropyI)oxy) 0 A-8064 H H H H H 0 OH 3 OH 3 2-(oxiran-2-y) 0 A-8065 H H H H 0 OH 3 OH 3 2-SMe 0 A-8066 H H H H O GH 3 CH3 3-SMe 0 A-806/ H H H H 0 OH 3 OH 3 2-S(=0)Me 0 A-8068 H H H H D GH 3 TW3 3-S(=0)Me 0 A-8069 H H H H O GH 3 RT3 2-S(=U) 2Me 0 A-8070 H H H H 0 OH 3 OH 3 3-S(=0) 2Me 0 A-8071 H H H H 0 OH 3 OH 3 2-SCF 3 0
A-80/2 H H H H 0 OH 3 OH 3 3-SF 3 0
A-80/3 H H H H 0 OH 3 OH 3 3-S(=0)F 3 0
A-80/4 H H H H 0 OH 3 OH 3 3-SCF(CF 3) 2 0
A-80b H H H H 0 OH 3 C3 2-(cycobpropylthlo) A-806 H H H H H GH3 0M 3 2-(cycbpropylsufinyD A-80] H H H H 0 OH 3 CR3 2-(cycbpropylsufonyD 0 A-808 H H H H 0 OH 3 C3 2-C(=0)Me 0 A-80/9 H H H H 0 OH 3 OH 3 2-GH 2C(=U)0H 3 0 A-8080 H H H H D0iH 3 OH 3 2-GH 20(= 0)GF 3 A-8081 H H H H 0 OH 3 OH 3 2-CH 2 UH 0 A-8082 H H H H O GH3 7H 3 2-H 2 0GH 3 0
A-8083 H H H H 0 OH 3 OH 3 2-0H 20H 2 CH 3 A-8084 H H H H O GH3 7- 3 2-OH 2SCH 3 A-808b H H H H H GiHi3 3 2-OH 2 S(=U)GH 3 0
A-8086 H H H H 0 OH 3 OH 3 2-CH 2 S(=0) 2 CH3 0
A-808/ H H H H f0 OH 3 OH 3 2-(benzybxy) 0 A-8088 H H H H H GH 3 T3 2-NH 2 A-8089 H H H H f0 OH 3 OH 3 2-NHMe 0
[0268]
[Table 143]
com pound R' R2 R R A R R' (R)m p A-8090 H H H H 0 OH 3 OH 3 2-N (Me)2 0 A-8091 H H H H 0 OH 3 OH 3 2-(1,3-dloxolan-2-yD 0 A-8092 H H H H 0 OH 3 OH 3 2-(1,3-dioxan-2-yD A-8093 H H H H OH 3 C73 2-(lH- idazol-2-y) A-8094 H H H H O0H 3 OH3 2-(thiazol-2-yl) 0 A-8095 H H H H D OH 3 OH 3 2-(oxazol-2-yD 0 A-8096 H H H H D OH 3 OH 3 2-GH=N0H 0 A-8097 H H H H D OH 3 OH 3 2-OH=NOMe 0 A-8098 H H H H H 0H3 H3 2-(4,b-dihydro-3-isoxazolyD 0 A-8099 H H HOGH3 TW3 H 2-N 0 A-8100 H H H i 0 H OH 3 7T3 2-NU 2 0
A-8101 H H H H OGH3 T3 2-F,6-I1 0 A-8102 H H H H H OH 3 TW3 2-F,6-Me 0 A-8103 H H H H 0 OH 3 OH 3 3-F,6-M e 0 A-8104 H H H H 0 OH 3 OH 3 4-F,2-M e 0 A-810b H H H H 0 OH 3 CH3 2-F,6-UMe 0 A-8106 H H H H 0 OH 3 T3 3-F,6-UMe A-810/ H H H H 0 OH 3 OH 3 2,6-C 2 A-8108 H H H H H GH 3 T3 2-CI,6-Me 0 A-8109 H H H H 0 OH 3 OH 3 3-GI,6-M e 0 A-81 10 H H H H 0H 3 OH 3 4-GI,2-M e 0 A-8111 H H H H 0 OH 3 OH 3 2-CIb-CF 3 0 A-8112 H H H H 0 OH 3 OH 3 2-CI,6-CF 3 0 A-8113 H H H H O 0H3 OH3 2-CI,6-UMe 0 A-8114 H H H H HDi GH 3 CH3 3-CI,6-UMe 0 A-811b H H H H HHGH3 CH3 4-G1,2-UMe 0 A-8116 H H H H V GH 3 TW3 2,4-Me 2 A-811 H H H H i 0 OH 3 OH 3 2,b-M e 2 0 A-8118 H H H H 0 OH 3 OH 3 2,6-M e 2 0 A-8119 H H H H 0 OH 3 OH 3 2-M e,4-CF 3 0 A-8120 H H H H O 0H3 OH3 2-Me,b-C3F 0 A-8121 H H H H 0 OH 3 OH 3 2-Me,6-CF 3 0 A-8122 H H H H H 0 OH 3 OH 3 2-MAe,4-UMe C) A-8123 H H H H O GH 3 T3 2-Me,b-UMe 0 A-8124 H H H H O0H3 OH3 2-Me,6-0Me 0 A-812b H H H H D OH 3 T3 3-Me,6-0Me 0 A-8126 H H H H O GH 3 CH3 4-Me,2-UMe F A-8127 H H H H 0 OH 3 OH 3 2,b-UMe 2 0 A-8128 H H H H 0 OH 3 OH 3 2,6-UMe 2 0
A-8129 H H H H H 0 OH 3 OH 3 2-OMe,6-F 3 0 A-8130 H H H H 0 OH 3 OH 3 2-CH' 2,b-F 0 A-8131 H H H H D 0iH 3 OH 3 2-CHF2,6-F 0 A-8132 H H H H O GH3 CH 3 2-CHF 2,b-M e 0 A-8133 FH H H H O H3 *MT3 2-CHF 2,6-M e 0 A-8134 H H H H GH3 O MT 3 2-cycbpropylb-F 0 A-813b H H H H 0 OH 3 RT3 2-cycbpropyl,6-F 0 A-8136 H H H H 0 OH 3 OH 3 2-cyclopropylb-Me 0 A-8137 H H H H 0 OH 3 OH 3 2-cyclopropyl,6-Me 0 A-8138 H H H H 0 OH 3 OH 3 2-ethenyl,6-F 0 A-8139 H H H H GH 3 O C3 2-ethenyl,6-Me 0 A-8140 H H H H 0 OH 3 OH 3 2-OEt,b-F A-8141 H H H H O GH3 -7 3 2-Et,6-F 0 A-8142 H H H H H GH 3 T3 2-UEt,b-CI 0 A-8143 H H H H 0 OH 3 OH 3 2-OEt,6-CI 0 A-8144 H H H H O0H3 OH3 2-UEt,b-Me 0 A-814b H H H H f0 OH 3 3 2-UEt,6-Me 0 A-8146 IfH H H I OHH 3 OH 3 2-UGH2,b- 0
[0269]
[Table 144]
com pound R' R-2 R A R R' (R)m p A-814/ i 27 HHHH 0 OH3OH3 2-CHF2,6-F 0 A-8148 H H H H 0 OH 3 OH 3 2-OCHF 2 ,b-Me 0 A-8149 H H H H 0 OH 3 OH 3 2-UGHF 2 ,6 -M e 0 A-8150 H H H H ifH 0ifO3 2-(cycbpropyloxy),b-F 0 A-81b1 H H H H 0 OH 3 OH 3 2-(cycbpropyloxy),6-F 0 A-8152 H H H H D OH 3 OH 3 2-(cyclopropybxy),b-Me 0 A-8153 H H H H D OH 3 OH 3 2-(cyclopropyoxy),6-Me 0 A-8154 H H H H D OH 3 OH 3 2-SMe,b-F 0 A-81bb H H H H H 0 OH 3 OH 3 2-SMe,6-F 0 A-8156 H H H H D GH 3 CR3 2-SMe,b-Me 0 A-815/ H H H H i 0 OH 3 RT3 2-SMe,6-M e 0 A-81b8 H H H H 0 OH 3 CR3 2-S(=0)Me,b-F 0 A-8159 H H H H O GH3 RT3 2-S(=0)Me,6-F 0 A-8160 H H H H 0 OH 3 OH 3 2-S(=0)Me,b-M e 0 A-8161 H H H H 0 OH 3 OH 3 2-S(=0)Me,6-M e 0 A-8162 H H H H O GH3 CH3 2-S(=0) 2Me,b-H 0 A-8163 H H H H O GH 3 RT3 2-S(=0) 2Me,6-F A-8164 H H H H O 0H3 OH3 2-S(=0) 2Me,b-M e 0 A-8165 H H H H 0 GH 3 RT3 2-S(=0) 2 Me,6-M e 0 A-8166 H H I fH H 0H3 OH3 2-SCF3,b-F 0 A-816/ H H H H f0 OH 3 OH 3 2-SCF 3 ,6-F 0 A-8168 H H H H 0 OH 3 OH 3 2-SGF 3 ,b-M e 0 A-8169 H H H H O 0H3 OH3 2-SGF3,6-M e 0 A-81/0 H H H H f0 OH 3 OH 3 2-S(=U)0F 3 ,b-F 0 A-81/l1 H H H H f OH 3 CH3 2-S=U)GF 3,6-F 0 A-81/2 H H H H f0 OH 3 CH3 2-S=U)GF 3,b-M e 0 A-81/3 H H H H f OH 3 MT3 2-S(=U)GF 3 ,6-M e F A-81/4 H H H H i 0 OH 3 OH 3 2-S(=U) 20F 3 ,b-F 0 A-81/b H H H H 0 OH 3 OH 3 2-S(=0) 2CF 3 ,6-F 0 A-81/6 H H H H 0 OH 3 OH 3 2-S(=0) 20F 3 ,b-Me 0 A-81] H H H H 0 OH 3 OH 3 2-S(=0) 20F 3 ,6-M e 0 A-81/8 H H H H 0 OH 3 OH 3 2-(cycobpropylthb),b-F 0 A-81i9 H H H fHO0H3 OH3 2-(cycobpropylthlo),6-F 0 A-8180 H H H H f0 OH 3 RT3 2-(cycbpropylthio),b-M e 0 A-8181 H H H H 0 OH 3 OH 3 2-(cycbpropylthio),6-M e 0 A-8182 H H H H O GH3 RT3 2-C(=0)Me,b-F 0 A-8183 H H H H O GH3 CH3 2-C(=0)Me,6-F 0 A-8184 H H H H O 0H3 OH3 2-C(=0)Me,b-M e 0 A-818b H H H H 0 OH 3 OH 3 2-C(=0)Me,6-M e 0 A-8186 H H H H H 0 OH 3 OH 3 2-CH 2UH,b-F 0 A-818/ H H H H 0 OH 3 OH 3 2-CH 2UH,6-F 0 A-8188 H H H H 0 OH 3 OH 3 2-OH 2UH,b-M e 0 A-8189 H H H H f0 OH 3 C3 2-H 2 0H,6-M e 0 A -8190 H H H H O GH3 7R 3 2-0H 20 GH 3,4-F 0 A-8191 H H Hi H3 2-H20GH3,b-FD Gi3 0 A-8192 H H H H O GH3 0M3 2-H20GH3,6-F 0 A-8193 H H H H 0 OH 3 OH 3 2-CH 20H 3 ,4-M e 0 A-8194 H H H H 0 OH 3 OH 3 2-0H 20CH 3,b-M e 0 A-8195 H H H H 0 OH 3 OH 3 2-CH 20H 3 ,6-Me 0 A-8196 H H H H O GH3 2-O (=U)GH3,b-F A-81i9 H H H H 0 OH 3 OH 3 2-O(=U)0H 3 ,6-F 0 A-8198 H H H H f0 OH 3 RM3 2-0(=0)GH 3,b-M e 0 A-8199 H H H H f0 OH 3 CR3 2-0G0(=U)GH 3,6-M e 0 A-8200 H H H H 0 OH 3 OH 3 2-US(=0) 2 CH 3 ,b-F 0 A-8201 H H H H Hi0 OH 3 OH 3 2-US(=0) 2 CH 3 ,6-F 0 A-8202 H H H H f0 OH 3 RT3 2-US(=U) 2OH 3,b-M e F A-8203 H H FH F F OH 3 OH 3 2-US(=0) 2CH 3,6-M e 0
[0270]
[Table 145]
com pound R' R2 R R A R R' (R)m p A-8204 H H H H H 0 OH3 OH3 2-CH 2SH3,b-F 0 A-8205 H H H H f0 OH 3 OH 3 2-CH 2 SOH 3 ,6-F 0 A-8206 H H H H 0 OH 3 OH 3 2-CH 2SOH 3,b-M e 0 A-8207 H H H H i 0 OH 3 *-C3 2-H 2 SC0H 3,6-M e A-8208 H H H H O 0H3 OH3 2-NMe2,b-FW A-8209 H H H H D OH 3 OH 3 2-NMe 2 ,6-F 0 A-8210 H H H H D OH 3 OH 3 2-NMe 2 ,b-M e 0 A-8211 H H H H D OH 3 OH 3 2-NMe 2 ,6-M e 0 A-8212 H H H H H 0 OH 3 OH 3 2-CN,4-F 0 A-8213 H H H H O GH3 -T3 2-CN,b-F 0 A-8214 H H H H O GH3 T3 2-CN,6-F 0 A-8215 iH H H H 0 OH3 T3 2-CN,6-Me 0 A-8216 H H H H i 0 OH 3 T3 2-CN,b-OMe 0 A-8217 H H H H 0 OH 3 OH 3 2-CN,6-OMe 0 A-8218 H H H H 0 OH 3 OH 3 3-CN,6-M e 0 A-8219 H H H H 0 3 T3 3-CN,6-OMe 0 A-8220 H H H H f0 OH 3 CH3 4-CN,2-Me 0 A-8221 H H H H O 0H3 OH3 4-CN,2-OMe 0 A-8222 H H H H OH 3 T3 2-NU 2 ,4-F 0 A-8223 H H H H 0 OH 3 OH 3 2-N0 2 ,b-F 0 A-8224 H H H H Hi0 OH 3 OH 3 2-N0 2 ,6-F 0 A-8225 H H H H f0 OH 3 OH 3 2-N0 2,4-MvAe 0 A-8226 H H H H O 0H3 OH3 2-N20,b-M e 0 A-8227 H H H H f0 OH 3 OH 3 2-N0 2,6-M e 0 A-8228 H H H H iF OH 3 CH3 2-M e,4,b-F 2 0 A-8229 HfHCHHHif OH 3 CR3 2-M e,6-Et F A-8230 H H H H f OH 3 MT3 2-cyclopropyl,6-OMe 0 A-8231 H H H H i 0 OH 3 OH 3 2-M e,b-Et 0 A-8232 H H H H 0 OH 3 OH 3 2,6-Et2 0 A-8233 H H H H 0 OH 3 OH 3 2-Et,6-F 0 A-8234 H H H H 0 OH 3 OH 3 2-0H 20H 3 ,6-CI 0 A-8235 H H H H 0 OH 3 OH 3 2-0H 20H 2CH 3,6-CI 0 A-8236 H H H H H 0 OH 3 OH 3 2-CH 2 NMe 2 0 A-8237 H H H H HFf GH 2 GN GH2CN H 0 A-8238 H H H H 0 OH 2ON CH 2ON 2 -F A-8239 H H H H D GH 2 GN T72GN 2-C 1 0 A-8240 H H H H H GH 2 GN GH27 2-Br 0 A-8241 H H H H 0 OH 2ON CH 2ON 2-OH 0 A-8242 H H H H 0 OH 2ON CH 2ON 2-M e 0 A-8243 H H H H H 0 OH 2ON CH 2ON 2-Et 0 A-8244 H H H H 0 OH 2ON CH 2ON 2-Pr 0 A-8245 H H H H 0 OH 2ON CH 2ON 2-CF 3 0
A-8246 H H H H GH 2 GN T2CN 2-GHF 2 0
A-8247 H H H H 0 H2 GN G2GN 2-GH 2F 0 A-8248 H H H H f D0if GH 2 GN GH2G 2-GF 2GI1 A-8249 H H H H f0 GH 2 GN GH27G 2-cycbpropyl 0 A-8250 H H H H 0 OH 2ON CH 2ON 2-cyclobutyl 0 A-8251 H H H H 0 OH 2ON CH 2ON 2-cycbpentyl 0 A-8252 H H H H 0 OH 2ON CH 2ON 2-ethenyl1 A-8253 H H H H GH 2 GN 72CN 2-allyl A-8254 H H H H D 0H 2ON CH2ON 2-(prop-1-en-1-y) 0 A-8255 H H H H if0 f GH 2GN GH2G 2-(trffboroethenyD A-8256 H H H H f0 GH 2 GN GH27G 2-UMe F A-8257 H H H H 0 OH 2ON CH 2ON 2-OEt A-8258 IfH H H H H0 H 2ON CH 2ON 2-UPr 0 A-8259 H H H H f0 GH 2 GN GH2GN 2-0(/-Pr) 0 A-8260 H H H HF 7 H 2ON CH 2ON 2-0F 3 0
[0271]
[Table 146]
com pound R' R2 R R A R R' (R)m p A-8261 H H H H 0 OH 2ON CH 2ON 2-0)H F2 A-8262 H H H H 0 H 2ON CH 2ON 2-(cycbpropybxy) 0 A-8263 H H H H 0 H 20N OH 20N 2-(cycobbuty bxy) 0 A-8264 H H H H H GH 2 GN G2GN 2-(cycbpentybxy) 0 A-8265 H H H H 0 OH 2ON CH 2ON 2-((2,2-d ch brocycbpropy Doxy) 0 A-8266 H H H H D 0H 2ON 2-(oxiran-2-y D0 CH2ON A-8267 H H H H D 0H2ON CH2ON 2-SMe 0 A-8268 H H H H D 0H2ON CH2ON 3-SMe 0 A-8269 H H H H H 0 OH 2ON CH 2ON 2-S (=0)M e 0 A-8270 H H H H D CH 2CN T2GUN 3-S (= 0)M e 0 A-82/ 1 H H H H if 0 CH 2CN GH27N 2-S= U) 2Me 0 A-8272 H H H H D CH 2CN T2GUN 3-S (=) 2M e A-8273 H H H H CH 2CN T2GUN 2-S CGH A-8274 H H H H 0 OH 2ON CH 2ON 3-SG,3 A-82/b H H H H 0 H 2ON CH 2ON 3-S (= 0)CF A-8276 H H H H I GH 2CN G72GN 3-SCF (F 3 ) 2 A-8277 H H H H H CH 2CN GH27G 2-(cycobpropytho) 0 A-8278 H H H H D 0H 2ON CH2ON 2-(cycbpropy Isu finy D 0 A-8279 H H H H G2GR 2-(cycobpropy u fony D A-8280 H H H H 0 OH 2ON CH 2ON 2-G (= 0)M e 0 A-8281 H H H H Hi0 OH 2ON CH 2ON 2-GH 2 0(= )H 3 0 A-8282 H H H H Hi0 OH 2ON CH 2ON 2-GH 2 0(=U)CF 3 0 A-8283 H H H H 0 OH 2ON CH 2ON 2-GH 2 UH 0 A-8284 H H H H f0 OH 2ON CH 2ON 2-GH 20H 3 0 A-8285 H H H H GH 2CN GHR2CN 2-GH 20H 2 CH 3 0
A-8286 H H H H H0 f GH2GN G72G 2-CH 2SCH3 0 A-8287 H H H Hi GH 2CN GH27N 2-CH 2S (= )H 3 0
A-8288 H H H H i 0 OH 2ON CH 2ON 2-GH 2S(= 0) 2 CH 3 0 A-8289 H H H H D 0H2ON CH2ON 2-(benzy bxy) 0 A-8290 H H H H 0 OH 2ON CH 2ON 2-NH 2 A-8291 H H H H D 0H2ON CH2ON 2-NH M e A-8292 H H H H 0 OH 2ON CH 2ON 2-N (e) 2 0 A-8293 H H H H f0 OH 2ON CH 2ON 2-0,3-d bxoan-2-yD 0 A-8294 H H H H ii f CH2CN G72GN 2-(1,3-d bxan-2-y D A-8295 H H H H 0 H 2ON CH 2ON 2-(1H- idazoE2-yD A-8296 H H H H D CH 2CN GH2CN 2-(thiazo -2-y) 0 A-8297 H H H H iif CH2CN GH27N 2-(oxazol-2-y D A-8298 H H H H 0 OH 2ON CH 2ON 2-GH= N0H 0 A-8299 H H H H 0 OH 2ON CH 2ON 2-OH= NOM e 0 A-8300 H H H H H 0 OH 2ON CH 2ON 2-(4,b-dihydro-3-oxazo D 0 A-8301 H H H H 0 OH 2ON CH 2ON 2-N 0 A-8302 H H H H 0 OH 2ON CH 2ON 2-NO 2 0
A-8303 H H H H cH 2 GN T2CN 2-F,6-GI 0 A-8304 H H H H E 0 CH 2CN G2GN 2-F,6- e 0 A-8305 H H H H ifD GH2GN GH27 3-F,6-M e 0 A-8306 H H H H GH 2 GN GH27 4-F,2-M e A-8307 H H H H 0 OH 2ON CH 2ON 2-F,6-M e 0 A-8308 H H H H D 0H2ON CH2ON 3-F,6-M e 0 A-8309 H H H H 0 OH 2ON OH 2ON 2,6-O' 0 A-8310 H H H H i if CH2CN TH2CN 2- 1,6-M e 0 A-8311 H H H H 0 OH 2ON CH 2ON 3- 1,6-M e 0 A-8312 H H HHii f CH2CN T2GUN 4-01,2-M e 0 A-8313 H H H H HD0 CH 2CN GH27GN 2-C Ib-CF 3 0 A-8314 H H H H 0 OH 2ON CH 2ON 2- I,6-F 3 0 A-8315 H H H H f0 OH 2ON CH 2ON 2-G 1,6-0M e 0 A-8316 H H H H i if CH2GN GH2GN 3-G 1,6-0M e 0 A-8317 H H H H f0 OH 2 GN GH 2GN 4-G 1,2-UM e 0
[0272]
[Table 147]
com pound R' R2 R R A R R' (R)m p A-8318 H H H H 0 CH 2CN CH 2CN 2,4-M e 2 0 A-8319 H H H H 0 CH 2CN CH 2CN 2,b-M e 2 0 A-8320 H H H H 0 CH 2CN CH 2CN 2,6-Me 2 0 A-8321 H H H H i 0 CH 2CN G2GN 2-M e,4-H3 0 A-8322 H H H H D CH 2CN CH 2CN 2-Me,b-F 3 0 A-8323 H H H H f Di CH 2CN CH 2CN 2-Me,6-F 3 0 A-8324 H H H H 0Di CH 2CN CH 2CN 2-Me,4-0Me A-8325 H H H H 0Di CH 2CN CH 2CN 2-Me,b-0Me 0 A-8326 H H H H H 0 CH 2CN CH 2CN 2-Me,6-0Me 0 A-832/ i H H H H 0 CH2CN T2GUN 3-M e,6-0Me 0 A-832 Hf8 H H H i 0 CH 2CN G72GN 4-M e,2-UMe 0 A-8329 H H H H D CH 2CN T2GUN 2,b-UMe 2 0
A-8330 H H H H CH 2CN T2GUN 2,6-UMe 2 0 A-8331 H H H H 0Di CH 2CN CH 2CN 2-UMe,6-F 3 0 A-8332 H H H H 0Di CH 2CN CH 2CN 2-CH F 2,b-F 0 A-8333 H H H H I GH 2CN G72GN 2-CHF 2,6-F 0 A-8334 H H H H H CH 2CN GH27G 2-CH 2,b-A e 0 A-8335 H H H H 0 CH 2CN CH 2CN 2-CH1 2,6-M e 0 A-8336 H H H H I GH 2CN G72N 2-cycobpropylb-F 0 A-8337 H H H H DIi CH 2CN CH 2CN 2-cycbpropyl,6-F 0 A-8338 H H H H H CH 2CN CH 2CN 2-cyclopropylb-M e 0 A-8339 H H H H H CH 2CN CH 2CN 2-cyclopropyl,6-M e 0 A-8340 H H H H D CH 2CN CH 2CN 2-ethenyl,6-F 0 A-8341 H H H H H CH 2CN CH 2CN 2-ethenyl,6-M e 0 A-8342 H H H H GH 2CN GHR2CN 2-UEt,b-F A-8343 H H H H H0 f GH2GN G72G 2-UEt,6-F 0 A-8344 H H H H H 0 CH 2CN G72GN 2-UEt,b-CI 0 A-8345 H H H H i 0 CH 2CN CH 2CN 2-UEt,6-CI 0 A-8346 H H H H D CH 2CN CH 2CN 2-OEt,b-Me 0 A-8347 H H H H 0Di CH 2CN CH 2CN 2-OEt,6-Me 0 A-8348 H H H H 0Di CH 2CN CH 2CN 2-CHF 2,b-F 0 A-8349 H H H H 0Di CH 2CN CH 2CN 2-CH' 2,6-F 0 A-8350 H H H H H 0 CH 2CN CH 2CN 2-OCHF 2 ,b-Me 0 A-8351 H H H H iif CH2CN T2GUN 2-CHF 2,6-MAe A-8352 H H H H D CH 2CN CH 2CN 2-(cycbpropyloxy),b-F 0 A-8353 H H H H D GH2GN GH2CN 2-(cycbpropyloxy),6-F 0 A-8354 H H H H f CH 2CN H2GUN 2-(cyclopropyloxy),b-M e 0 A-8355 H H H H D CH 2CN CH 2CN 2-(cyclopropybxy),6-Me 0 A-8356 H H H H 0Di CH 2CN CH 2CN 2-SMe,b-F 0 A-8357 H H H H H 0 CH 2CN CH 2CN 2-SMe,6-F 0 A-8358 H H H H 0 CH 2CN CH 2CN 2-SMe,b-Me 0 A-8359 H H H H D CH 2CN CH 2CN 2-SMe,6-Me 0 A-8360 H H H H I GH 2CN G72GN 2-S(=0)Me,b-F 0 A-8361 H H H H CH 2CN T2G7N 2-S(=0)Me,6-F 0 A-8362 H H H H CH2 N G72GN 2-S(=0)Me,b-M e 0 A-8363 H H H H CH2 N G72GN 2-S(=0)Me,6-M e 0 A-8364 H H H H 0 CH 2CN CH 2CN 2-S(=0) 2Me,b-F 0 A-8365 H H H H 0 CH 2CN CH 2CN 2-S(=U) 2Me,6-F 0 A-8366 H H H H 0 CH 2CN CH 2CN 2-S(=0) 2 Me,b-Me 0 A-8367 H H H H GH 2CN GH2CN 2-S(=U) 2 Me,6-M e 0 A-8368 H H H H 0 CH 2CN CH 2CN 2-SC3,b-F 0 A-8369 H H H H HDi CH 2CN G72GN 2-SCF 3 ,6-F 0 A-8370 H H H H iif CH2CN GH27G 2-SCF3,b-M e 0 A-8371 H H H H D CH 2CN CH 2CN 2-SCF 3 ,6-Me 0 A-8372 H H H H Hi0 CH 2CN CH 2CN 2-S(=0)C3,b-F 0 A-8373 H H H H i GH 2 GN GHR2GN 2-S(=U)GF 3 ,6- 0 A-8374 H H H H f0 CH 2 GN H 2GN 2-S(=U)G 3 ,b-M e 0
[0273]
[Table 148]
com pound R' R2 R R A R R' (R)m p A-8375 H H H H 0 CH 2CN CH 2CN 2-S(=U)CF 3 ,6-M e 0 A-8376 H H H H f0 CH 2CN CH 2CN 2-S(=U) 20F 3 ,b-F 0 A-8377 H H H H 0 CH 2CN CH 2CN 2-S(=U) 20F 3 ,6-F A-8378 H H H H i 0 GH 2 GN TH2C 2-S(=0) 0F 3 ,b-M e 2 0 A-8379 H H H H D CH 2CN CH 2CN 2-S(=U) 2CF 3 ,6-M e 0 A-8380 H H H H f Di CH 2CN CH 2CN 2-(cycbpropylthb),b-F 0 A-8381 H H H H f Di CH 2CN CH 2CN 2-(cycbpropylthb),6-F 0 A-8382 H H H H f Di CH 2CN CH 2CN 2-(cycbpropylthio),b-Me 0 A-8383 H H H H H 0 CH 2CN CH 2CN 2-(cycbpropylthio),6-Me 0 A-8384 H H H H D GH 2 GN TH2GN 2-G(=0)Me,b-F 0 A-8385 H H H H i 0 GH 2 GN G72GN 2-0(=U)Me,6-F 0 A-8386 H H H H D GH 2 GN TH2GN 2-G(=0)Me,b-M e 0 A-8387 H H H H GH 2 GN TH2GN 2-G(=U)Me,6-Me A-8388 H H H H DI CH 2CN CH 2CN 2-GH 2UH,b-F 0 A-8389 H H H H DI CH 2CN CH 2CN 2-GH 2UH,6-F 0 A-8390 H H H H 7 GH 2 GN GH27GN 2-GH 20H,b-M e 0 A-8391 H H H H H GH 2 GN GH27G 2-GH 20,6-M e 0 A-8392 H H H H 0 CH 2CN CH 2CN 2-GH 20H 3 ,4-F 0 A-8393 H H H H f GH 2 GN G72GN 2-GH 20H 3,b-F A-8394 H H H H DI CH 2CN CH 2CN 2-GH 20H 3 ,6-F 0 A-8395 H H H H i i f CH2CN CH2CN 2-OH 20CH3,4-Me 0 A-8396 H H H H i i f CH2CN CH2CN 2-OH 20CH3,b-Me 0 A-8397 H H H H D0 CH 2CN CH 2CN 2-OH 20CH 3 ,6-Me 0 A-8398 H H H H H 0 CH 2CN CH 2CN 2-UC(=0)CH 3 ,b 0 A-8399 H H H H H GH 2 GN GHR2CN 2-0(=0)GH 3,6-F 0 A-8400 H H H H iif CH2CN GHR2CN 2-0(=0)CH 3,b-M e F A-8401 H H H H iF CH 2CN TH2GN 2-0G0(=U)GH 3 ,6-M e 0 A-8402 H H H H i 0 CH 2CN CH 2CN 2-OS(=0) 2CH 3 ,b- 0 A-8403 H H H H 0Di CH 2CN CH 2CN 2-OS(=0) 2CH 3 ,6-F 0 A-8404 H H H H 0Di CH 2CN CH 2CN 2-OS(=0) 2CH 3,b-Me 0 A-8405 H H H H f Di CH 2CN CH 2CN 2-OS(=0) 2CH 3,6-M e 0 A-8406 H H H H 0Di CH 2CN CH 2CN 2-OH 2 S0H 3,b-F 0 A-8407 H H H H HD0 CH 2CN CH 2CN 2-OH 2 S0H 3 ,6-F 0 A-8408 H H H H f GH 2 GN GH27GN 2-CH 2S0H 3,b-MAe 0 A-8409 H H H H 0 CH 2CN CH 2CN 2-OH 2SCH 3,6-Me 0 A-8410 H H H H GH 2 N H27GN 2-NM e 2 ,b-F A-8411 H H H H GH 2 N GH27GN 2-NM e 2 ,6-F 0 A-8412 H H H H D CH 2CN CH 2CN 2-NMe 2 ,b-Me 0 A-8413 H H H H 0 CH 2CN CH 2CN 2-NMe 2 ,6-MAe 0 A-8414 H H H H H 0 CH 2CN CH 2CN 2-ON,4-F 0 A-8415 H H H H 0 CH 2CN CH 2CN 2-ONb-F 0 A-8416 H H H H 0 CH 2CN CH 2CN 2-N,6-F 0 A-8417 H H H H GH 2 GN GHR2CN 2-GN,6-M e 0 A-8418 H H H H GH 2 GN T2G7N 2-ONS5-UMe 0 A-8419 H H H H D GH 2 GN TH2GN 2-GN,6-0Me 0 A-8420 H H H H GH 2 GN TH2GN 3-GN,6-M e 0 A-8421 H H H H 0 CH 2CN CH 2CN 3-GN,6-0Me 0 A-8422 H H H H DI CH 2CN CH 2CN 4-ON,2-Me 0 A-8423 H H H H 0 CH 2CN CH 2CN 4-GN,2-0Me 0 A-8424 H H H H H GH 2 GN GHR2CN 2-N0 2 ,4-F 0 A-8425 H H H H 0 CH 2CN CH 2CN 2-N0 2 ,b-F 0
A-8426 H H H H H GH 2 GN G72GN 2-N0 2,6-F 0 A-8427 H H H H GH 2 GN TH2GN 2-N0 2,4-MAe 0 A-8428 H H H H 0 CH 2CN CH 2CN 2-N0 2,b-Me 0 A-8429 H H H H f0 CH 2CN CH 2CN 2-N0 2,6-MAe 0 A-8430 H H H H GH 2 GN GHR2GN 2-Me,4,b- 2 0
A-8431 H f FIFH 0 CH 2 GN CH 2CN 2-M e,6-Et 0
[0274]
[Table 149]
com pound R' R2 R R A R R' (R)m p A-8432 H H H H 0 CH 2CN CH 2CN 2-cyclopropyl,6-OMe 0 A-8433 H H H H 0 CH 2CN CH 2CN 2-Me,b-Et A-8434 H H H H 0 CH 2CN CH 2CN 2,6-Et2 A-8435 H H H H i 0 CH 2CN G2GN 2-Et,6-F 0 A-8436 H H H H f Di CH 2CN CH 2CN 2-0H 20H 3 ,6-CI 0 A-8437 H H H H f Di CH 2CN CH 2CN 2-0H 20H 2 CH 3 ,6-CI 0 A-8438 H H H H 0Di CH 2CN CH 2CN 2-CH 2 NMe 2 0 A-8439 H H H H F Di -H 20 2-U-GH 2G2- H 0 A-8440 H H H H 0 -GH 20H 2-U-GH 2 0H 2 - 2-F 0 A-8441 H H H H 0 -OH 2 CH 2-0- H2CH 2- 2-Cl 0 A-8442 H H H H i 0 -H 2 CH 2-U-OH 2CH 2- 2-Br A-8443 H H H H 0 -H 2 CH 2-0-OH 2CH 2- 2-OH 0 A-8444 H H H H H-0H 2 CH 2-U-OH 2CH 2- 2-M e 0 A-8445 H H H H D -H 2 CH 2-0-CH 2CH 2- 2-Et 0 A-8446 H H H H 0Di -GH 2 CH 2-U-GH 2CH 2- 2-Pr 0 A-8447 H H H H 0H D-C 2H2-U-C 2U2- 2-UF3 0 A-8448 H H H H -H 2 CH 2-U-CH 2CH 2- 2-H F2 0
A-8449 H H H H D -GH 2 CH 2-U-GH 2CH 2- 2-CH 2F 0
A-8450 H H H H -H 2 CH 2-U-CH 2CH 2- 2-OF 2CI 0 A-8451 H H H H D -GH 2 CH 2-U-GH 2CH 2- 2-cycbpropyl 0 A-8452 H H H H f0 -OH 2 CH 2-U-OH 2CH 2- 2-cycobbutyl 0 A-8453 H H H H -H2 CH 2-U-OH 2CH 2- 2-cycobpentyl 0 A-8454 H H H H D -H 2 CH 2-0-OH 2CH 2- 2-ethenyl1 A-8455 H H H H -H 2 CH 2-U-OH 2CH 2- 2-allyl A-8456 H H H H -H 2 CH 2-U-OH 2CH 2- 2-(prop-1-en-1-yD A-8457 H H H H -OH 2 0H2-OH2 02- 2-(trfftLoroethenyl) 0 A-8458 H H H H f0 -OH 2 CH 2-U-OH 2CH 2- 2-UMe F A-8459 H H H H i 0 -GH 20H 2-U-GH 20H 2- 2-UEt A-8460 H H H H F -OH 2 CH 2-0- H 2CH 2- 2-OPr 0 A-8461 H H H H 0 Di -GH 2 CH 2-U-GH 2CH 2- 2-0 (/-Pr) 0 A-8462 H H H H f Df -GH 2 CH 2-U-GH 2CH 2- 2-0G3 0 A-8463 H H H H DIIi -GH 2 C 2-U-GH 2CH 2- 2-CHF 2 0
A-8464 H H HHi i f -OH 202--GH2CH2- 2-(cycbpropybxy) 0 A-8465 H H H H f -H 2 CH2--H 2CH2- 2-(cycobbutybxy) 0 A-8466 H H H H 0 -GH 2 CH 2-U-GH 2CH 2- 2-(cycobpentybxy) 0 A-8467 H H H H ifD f -OH 22-0-H2CH2- 2-((2,2-dichbrocycbpropyDoxy) 0 A-8468 H H H H iF -OH 2 CH2--GH 2CH2- 2-(oxiran-2-yD A-8469 H H H H D -OH 2 CH 2-0- H2CH 2- 2-SMe 0 A-8470 H H H H D -GH 2 CH 2-U-GH 2CH 2- 3-SMe 0 A-84/1 H H H H D -OH 2 CH 2-0- H 2CH 2- 2-S(=0)Me 0 A-8472 H H H H DIIi -GH 2 H2-U-GH 2CH 2- 3-S(=0)Me 0 A-8473 H H H H D -H 2 CH 2-0-OH 2CH 2- 2-S(=U) 2Me 0 A-8474 H H HHi i f -OH2CH2-U-OH2CH2- 3-S(=U) 2Me 0 A-8475 H H H H 0 -OH 2 CH 2-U-OH 2CH 2- 2-SC, A-8476 H H H H D -H 2 CH2-0-OH 2CH 2- 3-SC3 A-8477 H H H H HD0 -OH 2 CH2-U-OH 2CH 2- 3-S(=U)GF 3 A-8478 H H HI H DI -OH 2 CH 2-0-OH 2CH 2- 3-S CF(CF3 2 0 A-8479 H H H H 0 -GH 2 CH 2-U-GH 2CH 2- 2-(cycobpropyfthio) 0 A-8480 H H H H 0DiI -H 2 C 2-0- H 2CH 2- 2-(cycbpropylsufinyl) 0 A-8481 H H H HF -OH 2 02--GH 2CH 2- 2-(cycobpropylulonyD 0 A-8482 H H H H D -GH 2 CH2-U-GH 2CH 2- 2-C(=0)Me 0 A-8483 H H H H i -GH 2 CH 2-U-GH 2CH 2- 2- H 2 C(=U)0H 3 0
A-8484 H H H H Hi0 -OH 2 CH 2-U-OH 2CH 2- 2- H2 C(=U)0GF 3 A-8485 H H H H DFFW -H 2 C 2-0- H2CH 2- 2-CH 2 UH F A-8486 H H H H Hi0 -OH 2 CH 2-U-OH 2CH 2- 2-0H 20H 3 0 A-8487 H H H H C-H 2-0 H2CH2- 2-- 2-H200H 2CH3 0 A-8488 H H H Hf -GH 2 CH 2-U-GH 2CH 2- 2-CH 2SCH 3 0
[0275]
[Table 150]
com pound R' R2 R R A R R' (R)m P A-8489 HH H H H -GH 2-U-GH22- 2-GH 2S(=)CH 3 0 A-8490 H H H H i 0 -GH 20H 2-U-GH 20H 2- 2-GH 2S(=U) 2 CH 3 0 A-8491 H H H H Df -CH 2CH 2-0-CH 2CH 2- 2-(benzybxy) A-8492 H H H H 0 -CH 2CH 2-U-CH 2CH 2- 2-NH 2 A-8493 H H H H D -CH 2CH 2-0-CH 2CH 2- 2-NHMe 0 A-8494 H H H H Di0-GH 20H2-U-GH 20H2- 2-N (e)2 A-8495 H H H H D -GH 2CH2--GH 2CH2- 2-(1,3-dioxolan-2-yD A-8496 H H H H D -OH 2 0H2--GH 2CH 2- 2-0,3-dioxan-2-yD A-8497 H H H H 0 -GH 2CH 2-U-GH 2CH 2- 2-(l1-m idazol-2-yD A-8498 H H H H 0 -OH 2 CH2-0-H 2C H2- 2-(thiazol-2-y) 0 A-8499 H H H H 1 H2H20-U-H2CH 2- 2-(oxazol-2-yD A-8b00 H H H H 0 -H 2 H02 -U-OH 2CH 2- 2-GH=N0H 0 A-8501 H H H H -OH 2CH 2-U-OH 2CH 2- 2-GH=NUMe 0 A-8502 H H H H - Dii -OH 2CH 2-0-H 2CH 2- 2-(4,b-dihydro-3-isoxazolyD 0 A-8503 H H H H 0 -GH 2CH 2-U-GH 2CH 2- 2-N 0 A-8504 H H H HIF D -2C 2UH 2-0-CH 2CH 2- 2-NO 2 0 A-8505 H H H H F -if -H 2CH 2-U-OH 2CH 2- 2-F,6-I1 0 A-8506 H H H H D -GH 2 CH2-U-GH 2CH 2- 2-F,6-Me 0 A-8507 H H H H -H 2CH 2-U-OH 2CH 2- 3-F,6-Me 0 A-8b08 H H H H D -GH 2CH 2-U-GH 2CH 2- 4-F,2-Me 0 A-8509 H H H H -OH 2CH 2-U-OH 2CH 2- 2-F,6-UMe 0 A-8b1O H H H H FV - 2 -HH2CH 2- 2-U-H 3-F,6-UMe 0 A-8b11 H H H H -OH 2CH 2-0-OH 2CH 2- 2,6-C12 0 A-8512 H H H H -OH 2CH 2-U-OH 2CH 2- 2-GI,6-M e 0 A-8513 H H H H DF-OH 2CH 2-U-OH 2CH 2- 3-GI,6-M e 0 A-8514 H H H H -GH 2 CH2-U-GH 2CH 2- 4-GI,2-M e 0 A-8b15 H H H H HDi -OH 2CH 2-U-OH 2CH 2- 2-0,b-F 3 F A-8516 H H H H i 0 -GH 2CH 2-U-GH 2CH 2- 2-I,6-GF 3 0 A-8b/17 H H H H D -OH 2CH 2-0- H 2CH 2- 2-GI,6-0Me 0 A-8b18 H H H H D -GH 2 CH2-U-GH 2CH 2- 3-GI,6-0Me 0 A-8519 H H H H DFf0 -GH 2 H 2-U-GH 2CH 2- 4-GI,2-0Me 0 A-8520 H H H H iF 0 -GH 2 CH2-U-GH 2CH 2- 2,4-Me 2 0
A-8521 H H H H F -GH 2CH 2-U-GH 2CH 2- 2,b-Me 2 0 A-8522 H H H H -OH 2CH 2-U-OH 2CH 2- 2,6-M e 2 0 A-8523 H H H H 0 -GH 2CH 2-U-GH 2CH 2- 2-Me,4-GF 3 0 A-8524 H H H H 0Di -OH 2CH 2-0- H2CH 2- 2-M e,b-F 3 0 A-8525 H H H H f -H 2CH 2-U-OH 2CH 2- 2-M e,6-GF 3 0 A-8526 H H H H D -H 2CH 2-0-OH 2CH 2- 2-Me,4-0Me A-8527 H H H H D -GH 2CH 2-U-GH 2CH 2- 2-Me,b-0Me 0 A-8528 H H H H 0 -H 2CH 2-0-OH 2CH 2- 2-Me,6-OMe 0 A-8529 H H H H 0 -GH 2CH 2-U-GH 2CH 2- 3-Me,6-0Me 0 A-8530 H H H H f Di -OH 2 CH2 -U-OH 2CH 2- 4-Me,2-0Me A-8531 H H HH -OH 2CH 2-U-OH 2CH 2- 2,5-UMe 2 0 A-8532 H H H i 0 H -OH 2CH 2-U-OH 2CH 2- 2,6-UMe 2 0 A-8533 H H HH D -H 2CH 2-0-OH 2CH 2- 2-OM e,6-GF 3 0 A-8534 H H HH -H 2CH 2-U-OH 2CH 2- 2- HF 2,b-F A-8535 iH H HH 0 -OH 2 H-0-OH 2CH 2- 2-OHF 2,6-F 0 A-8536 H H HH D -GH 2CH 2-U-GH 2CH 2- 2-GHF 2,b-MAe 0 A-8537 H H H f H Di -OH 2CH 2-0- H2CH 2- 2-GHF 2,6-Me 0 A-8538 H H H f0 H -OH 2 02--H 2CH 2- 2-cycbpropy1,5-4 0 A-8539 H H H H 0Df -GH 2 H 2-U-GH 2CH 2- 2-cycbpropyl,64 0 A-8540 H H H H 7-OH 20-0-H 20H 2- 2-cyclopropyl,5-Me 0 A-8541 H H H HF -H 2CH 2-U-OH 2CH 2- 2-cyclopropyl,6-M e 0 A-8542 H H H H D -OH 2 CH2-0-H 2C H2 2-ethenyl,64 0 A-8543 H H HHi i f -OH2 0--H2CH 2- 2-ethenyl,6-Me 0 A-8544 H H H H HDi -CH 2 H 2-0-GH 2UH 2- 2-Et,b-F 0 A-8545 HIHII H H 0 -GH 20H 2-U-GH 20H 2- 2-UEt,6-F
[0276]
[Table 151]
com pound R' R2 R R A R R' (R)m P A-8546 H H H HH D0 -GH2H2-U-GH2H2- 2-OEtb-CI 0 A-854/ H H H H HiF -GH 20H 2-U-GH 20H 2- 2-UOEt6-CI 1 A-8548 H H H H -OH 2CH 2-0-CH 2CH 2- 2-OEt,b-Me 0 A-8549 H H H Hf -H 2CH 2-U-CH 2CH 2- 2-OEt,6-Me 0 A-8bb0 H H H H D -OH 2CH 2-0-CH 2CH 2- 2-CHF 2,b-F 0 A-8bb1 H H H H Df -GH 20H 2-U-GH 20H 2- 2-CHF 2,6-F 0 A-8552 H H H H f Df -GH 2 H 2-U-GH 20H 2- 2-OCHF 2 ,b-Me 0 A-8553 H H H HD -GH 20H 2-U-GH 20H 2- 2-CHF 2 ,6-MAe 0 A-8554 H H H H D -GH 2 0H2--GH 20H 2- 2-(cycbpropybxy),b-F 0 A-8bbb i H H H H Di0 -OH 2CH2-0-H 2CH 2- 2-(cycbpropybxy),6-F 0 A-8556 H H H H -OH 2 CH2-U-H 2CH 2- 2-(cyclopropyloxy),b-M e 0 A-8bb/ H H H H 0 -OH 2 CH2-0-H 2C H2- 2-(cyclopropybxy),6-Me 0 A-8bb8 H H H H -OH 2CH 2-U-OH 2CH 2- 2-SMe,b-F 0 A-8559 H H H H Di0 -OH 2CH2-0- H 2CH2- 2-SMe,6-F 0 A-8560 H H H H 0 -GH 20H 2-U-GH 20H 2- 2-SMe,b-Me 0 A-8561 H H H HD -CH 2UH 2-0-GH 2UH 2- 2-SMe,6-Me 0 A-8562 H H H H 0 -OH 2CH 2-U-OH 2CH 2- 2-S(=0)Me,b-F 0 A-8563 H H H H D -GH 20H 2-U-GH 20H 2- 2-S(=0)Me,6-F 0 A-8564 H H H H f -OH 2 H 2-U-CH 2CH 2- 2-S(=0)Me,b-Me 0 A-8565 H H H HD -GH 20H 2-U-GH 20H 2- 2-S(=0)Me,6-Me 0 A-8566 H H H H 0 -OH 2CH 2-U-OH 2CH 2- 2-S(0=) 2Me,b-F A-856/ H H H H 0 -OH 2CH 2-U-OH 2CH 2- 2-S(=U20) 2 M e,6-F 0 A-8568 H H H H f Di -OH 2CH 2-0- H2CH 2- 2-S(=0) 2 Me,b-Me 0 A-8569 H H H H H-0H 2CH 2-U-CH 2CH 2- 2-S(=0) 2 Me,6-Me 0 A-85/0 H H H H -H 2CH 2-U-CH 2CH 2- 2-SC3,b-F A-85/1 H H H H -GH 20H 2-U-GH 20H 2- 2-SCF 3 ,6-F 0 A-85/2 i H fH H H f -OH 2 H20-UH 2CH 2- 2-SCF 3 ,b-M e 0 A-85/3 H H H H i 0 -GH 2 0H2-U-GH 2CH 2- 2-SCF 3 ,6-Me 0 A-8b/4 H H H H f Di -OH 2 CH2-0-H 2CH 2- 2-S(=U)C3,b-F 0 A-8b/b H H H H D-f -GH 2 0H2-U-GH 2CH 2- 2-S(=U)0F 3 ,6-F 0 A-8b/6 H H H H DFf -GH 2CH 2-U-GH 2CH 2- 2-S(=U)GF 3 ,b-Me 0 A-8b]] H H H H ifiD0 -GH2H 2-U-GH 2H 2- 2-S(=U)F 3,6-Me 0 A-85/8 H H H HF -GH 2 0H2-U-GH 2CH 2- 2-S(=0) 20%3,b-F 0 A-85/9 H H H H H0 -OH 2 CH2-U-H 2CH 2- 2-S(=U) 20F 3 ,6-F 0 A-8b80 H H H H 0 -GH 2CH 2-U-GH 2CH 2- 2-S(=0) 2CF 3 ,b-M e 0 A-8b81 H H H H D -H 2CH 2-0- H2CH 2- 2-S(=U) 2CF 3 ,6-Me F A-8582 H H H Hf -OH 2 CH2-U-H 2CH 2- 2-(cyclopropylthlo),b-F 0 A-8583 H H H H D -OH 2 CH2-0-H 2C H2- 2-(cycobpropylthio),6-F 0 A-8584 H H HHifiDi f -GH 202-GH2H2- 2-(cycbpropylthio),b-Me 0 A-8b8b H H H H f Dii -OH 2 C2-0-H 2C H 2- 2-(cycbpropylthio),6-Me 0 A-8586 H H H H D -GH 2 H 2-U-GH 2CH 2- 2-C(=0)Me,b-F 0 A-8b]8 H H H H 0 -OH 2CH 2-0- H 2CH 2- 2-C(=0)Me,6-F 0 A-8588 H H H H -OH 2CH 2-U-OH 2CH 2- 2-C(=0)Me,b-Me 0 A-8589 H H H H H if 0 -H 2H 2-U-OH 2CH2- 2-C(=0)Me,6-Me 0 A-85b90 H H H H Di -OH 2CH 2-0- H2CH 2- 2- H2 H,b-H 0 A-8591 H H H H -OH 2CH 2-U-OH 2CH 2- 2- H2 H,6-F A-85b92 H H H H D -OH 2CH 2-0- H2CH 2- 2-CH 2UH,b-M e 0 A-85b93 H H H H D -GH 2CH 2-U-GH 2CH 2- 2-CH 2UH,6-M e 0 A-85b94 H H H H D - 2CH H 2-0- H2CH 2- 2-CH 20H 3 ,4-F 0 A-8595 H H H H -GH 2CH 2-U-GH 2CH 2- 2- H20H 3 ,b-H 0 A-85b96 H H H H D -GH 2CH 2-U-GH 2CH 2- 2-CH 20H 3 ,6-F 0 A-859/ H H H H -GH 2CH 2-U-GH 2CH 2- 2-OH 2UCH 3 ,4-M e 0 A-8598 H H H H -OH 2CH 2-U-OH 2CH 2- 2-OH 2UCH 3 ,b-M e 0 A-85b99 H H H H D -H 2CH 2-0- H2CH 2- 2-CH 20CH 3 ,6-MAe F A-8600 H H H H f0 -OH 2CH 2-U-OH 2CH 2- 2-0(=U)0H 3 ,b-F 0 A-8601 H H H H -CH 2 H 2-0-CH 2CH 2- 2-C(=U)0H 3 ,6- 0 A-8602 H H H Hf -GH 2CH 2-U-GH 2CH 2- 2-0(=0)CH 3 ,b-M e 0
[0277]
[Table 152]
com pound R' R2 R R A R R' (R)m P A-8603 H H H H if -G H 2H2-U-GH2H2- 2-0(=0)CH 3 ,6-M e 0 A-8604 H H H HHi -GH 20H2-U-GH 20H2- 2-US(=U) 2CH3,b4 0 A-8605 H H H Hi Df -CH 2CH 2-0-CH 2CH 2- 2-OS(=U) 2 CH 3 ,6-F 0 A-8606 H H H H i 0 -CH 2CH 2-U-CH 2CH 2- 2-US(=U) 2CH 3,b-M e 0 A-8607 H H H H D -CH 2CH 2-0-CH 2CH 2- 2-OS(=U) 2CH 3,6-M e 0 A-8608 H H H H D -GH 20H2-0-GH 20H 2- 2-OH 2 S0H 3 ,b-F 0 A-8609 H H H H D -OH 20H2-0-GH 20H 2- 2-OH 2 S0H 3 ,6-F 0 A-8610 H H H H D -GH 20H 2-U-GH 20H 2- 2-OH 2SCH 3,b-MAe 0 A-8611 H H H H 0 -GH 20H 2-U-GH 20H 2- 2-OH 2SCH 3,6-MAe 0 A-8612 H H H H 0 -CH 2CH 2-0-CH 2CH 2- 2-NMe 2 ,b-F A-8613 H H H H i 0 -H 2CH 2-U-CH 2CH 2- 2-NMe 2 ,6-F 0 A-8614 H H H H D -H 2CH 2-0-CH 2CH 2- 2-NMe 2 ,b-MAe 0 A-8615 H H Hf0 H -CH 2CH 2-U-CH 2CH 2- 2-NMe 2 ,6-M e 0 A-8616 H H H H 0 -CH 2CH 2-0-CH 2CH 2- 2-ON,4-F 0 A-8617 H H HIH DI -GH 20H 2-U-GH 20H 2- 2-ON,b-F 0 A-8618 H H H H 7i -2C 2 H2-0-CH 2CH 2- 2-ON,6-F 0 A-8619 H H H H -CH 2CH 2-U-CH 2CH 2- 2-ON,6-M e 0 A-8620 H H H H D -GH 20H 2-U-GH 2 0H 2- 2-CN,b-0Me 0 A-8621 H H H H -H 2CH 2-U-CH 2CH 2- 2-CN,6-UMe 0 A-8622 H H H H D -GH 20H 2-U-GH 20H 2- 3-ON,6-Me 0 A-8623 H H HHi i f -CH 2CH2-U-CH 2CH2- 3-CN,6-UMe 0 A-8624 H H HHii f -CH 2CH2-U-CH 2CH2- 4-ON,2-Me 0 A-8625 H H H H D -CH 2CH 2-0-CH 2CH 2- 4-CN,2-0Me 0 A-8626 H H H H i -CH 2CH 2-U-CH 2CH 2- 2-N0 2,4-F A-8627 H H H H H -CH 2CH 2-U-CH 2CH 2- 2-N0 2,b-F A-8628 H H H H H -GH 20H 2-U-GH 20H 2- 2-N0 2,6-F 0 A-8629 H H H H -CH 2CH 2-U-CH 2CH 2- 2-NU 2,4-MAe 0 A-8630 H H H H i -GH 20H 2-U-GH 2 0H 2- 2-NU 2,b-Me 0 A-8631 H H H H f Di -CH 2 H02-U-CH 2CH 2 - 2-NU 2,6-Me 0 A-8632 H H H H D -OH 202 -GH 20H 2- 2-Me,4,b-F 2 0 A-8633 H H H H D -GH 20H 2-U-GH 20H 2- 2-Me,6-Et 0 A-8634 22-GH20H2- H H H H FC -H 2-cyclopropyl,6-OMe 0 A-8635 H H H HF -GH 20H 2-U-GH 20H 2- 2-Me,b-Et 0 A-8636 H H H H HD0 -CH 2CH 2-U-CH 2CH 2- 2,6-Et2 0 A-8637 H H H H f Di -GH 20H 2-U-GH 20H 2- 2-Et,6-F 0 A-8638 H H H H 0Di -CH 2CH 2-0-CH 2CH 2- 2-H 20GH 3 ,6-I1W A-8639 H H H H HD -CH 2CH 2-U-CH 2CH 2- 2-H 20GH 20H 3 ,6-C 1F A-8640 H H H H Dif -CH 2CH 2-0-CH 2CH 2- 2-OH 2 NMe 2 0 A-8641 H H fH H H S H H H 0 A-8642 H H H H H S H H 2-F 0 A-8643 H H fH H H S H H 2-Cl 0 A-8644 H H fH H H S H H 2-Br 0 A-8645 HH H H H S H H 2-OH 0 A-8646 H H H H S H H 2-Me 0 A-8647 H H H H S H H 2-Et 0 A-8648 H H fH H H S H H 2-Pr 0 A-8649 H H fH H H S H H 2-OF 3 0 A-8650 H H fH H H S H H 2-UHF 2 0 A-8651 H H fH H H S H H 2-OH 2F 0 A-8652 H S H HiH H H H 2-GF 201 0 A-8653 H H H H S H H 2-cyclopropyl 0 A-8654 H H fH H H S H H 2-cyclobutyl 0 A-8655 i H H H H S H H 2-cyclopentyl 0 A-8656 H H H H S H H 2-ethenyl1 A-8657 H H H H S H H 2-alyl 0 A-8658 H H H fH S H H 2-(prop-1-en-1-yD 0 A-8659 H H H H S H H 2-(trit loroethenyl) 0
[0278]
[Table 153]
com pound RI R2 R R R A R R' (R)m P A-8660 H H H H H S H H 2-0Me 0 A-8661 H H H H H S H H 2-0Et 0 A-8662 H H H H H S H H 2-0Pr 0 A-8663 H H H H H S H H 2-0(/-Pr) 0 A-8664 H H H H H S H H 2-0CF, 0 A-8665 H H H H H S H H 2-0CHF 2 0 A-8666 H H H H H S H H 2-(cycbpropy bxy) 0 A-8667 H H H H H S H H 2-(cycobbutybxy) 0 A-8668 H H H H H S H H 2-(cycbpentybxy) 0 A-8669 H H H H H S H H 2-((2,2-dichbrocycbpropyDoxy) 0 A-8670 H H H H H S H H 2-(oxiran-2-yD 0 A-8671 H H H H H S H H 2-SMe 0 A-8672 H H H H H S H H 3-SMe 0 A-8673 H H H H H S H H 2-S(=0)Me 0 A-8674 H H H H H S H H 3-S(=0)Me 0 A-8675 H H H H H S H H 2-S(=0) 2Me 0 A-8676 H H H H H S H H 3-S(=0) 2Me 0 A-8677 H H H H H S H H 2-SCF 0 A-8678 H H H H H S H H 3-SCF, 0 A-8679 H H H H H S H H 3-S(=0)CF 0 A-8680 H H H H H S H H 3-SCF(CF3) 2 0 A-8681 H H H H H S H H 2-(cycbpropyfthio) 0 A-8682 H H H H H S H H 2-(cycbpropylsulfhyl) 0 A-8683 H H H H H S H H 2-(cycbpropysulfonyD 0 A-8684 H H H H H S H H 2-C(=0)Me 0 A-8685 H H H H H S H H 2-CH 20(=0)0H 3 0 A-8686 H H H H H S H H 2-CH2C(=0 )0C 0 A-8687 H H H H H S H H 2-CH20H 0 A-8688 H H H H H S H H 2-CH 2 0CH 3 0 A-8689 H H H H H S H H 2-CH 2 0CH 2CH 3 0 A-8690 H H H H H S H H 2-CH 2SCH 3 0 A-8691 H H H H H S H H 2-CH 2S (=0)CH 3 0 A-8692 H H H H H S H H 2-CH 2S(=0) 2 CH3 0 A-8693 H H H H H S H H 2-(benzybxy) 0 A-8694 H H H H H S H H 2-NH 2 0 A-8695 H H H H H S H H 2-NHMe 0 A-8696 H H H H H S H H 2-NMe) 2 0 A-8697 H H H H H S H H 2-(1,3-dioxolan-2-yD 0 A-8698 H H H H H S H H 2-(1,3-dioxan-2-yD 0 A-8699 H H H H H S H H 2-(l1H-in idazol-2-yD 0 A-8700 H H H H H S H H 2-(thiazol-2-yl) 0 A-8701 H H H H H S H H 2-(oxazol-2-yD 0 A-8702 H H H H H S H H 2-CH=N0H 0 A-8703 H H H H H S H H 2-CH=NOMe 0 A-8704 H H H H H S H H 2-(4,5-dihydro-3-soxazolyD 0 A-8705 H H H H H S H H 2-CN 0 A-8706 H H H H H S H H 2-N02 0 A-870 7 H H H H H S H H 2-F,6-CI 0 A-8708 H H H H H S H H 2-F,6-Me 0 A-8709 H H H H H S H H 3-F,6-Me 0 A-8710 H H H H H S H H 4-F,2-Me 0 A-8711 H H H H H S H H 2-F,6-0Me 0 A-8712 H H H H H S H H 3-F,6-0Me 0 A-8713 H H H H H S H H 2,6-Cl2 0 A-8714 H H H H H S H H 2-CI,6-Me 0 A-8715 H H H H H S H H 3-CI,6-Me 0 A-8716 Hf FiHHFHS H H 4-CI,2-Me 0
[0279]
[Table 154]
com pound RI R2 R R R A R R' (R)m P A-8717 H H H H H S H H 2-C1,5-CF, 0 A-8718 H H H H H S H H 2-C1,6-CF, 0 A-8719 H H H H H S H H 2-C1,6-0Me 0 A-8720 H H H H H S H H 3-C1,6-0Me 0 A-8721 H H H H H S H H 4-C1,2-0Me 0 A-8722 H H H H H S H H 2,4-Me2 0 A-8723 H H H H H S H H 2,5-Me 2 0 A-8724 H H H H H S H H 2,6-Me 2 0 A-8725 H H H H H S H H 2-M e,4-CF 3 0 A-8726 H H H H H S H H 2-Me,b-CF 3 0 A-8727 H H H H H S H H 2-Me,6-CF3 0 A-8728 H H H H H S H H 2-Me,4-0Me 0 A-8729 H H H H H S H H 2-Me,5-0Me 0 A-8730 H H H H H S H H 2-Me,6-OMe 0 A-8731 H H H H H S H H 3-Me,6-OMe 0 A-8732 H H H H H S H H 4-Me,2-0Me 0 A-8733 H H H H H S H H 2,b-0Me 2 0 A-8734 H H H H H S H H 2,6-0Me 2 0 A-8735 H H H H H S H H 2-OMe,6-G 3 0 A-8736 H H H H H S H H 2-CHF 2,5-F 0 A-8737 H H H H H S H H 2-CHF 2,6-F 0 A-8738 H H H H H S H H 2-CHF 2,5-M e 0 A-8739 H H H H H S H H 2-CHF 2,6-M e 0 A-8740 H H H H H S H H 2-cycbpropyl,5-F 0 A-8741 H H H H H S H H 2-cycbpropyl,6-F 0 A-8742 H H H H H S H H 2-cycbpropyl,5-Me 0 A-8743 H H H H H S H H 2-cycbpropyl,6-M e 0 A-8744 H H H H H S H H 2-ethenyl,6-F 0 A-8745 H H H H H S H H 2-ethenyl,6-Me 0 A-8746 H H H H H S H H 2-0Et,5-F 0 A-8747 H H H H H S H H 2-0Et,6-F 0 A-8748 H H H H H S H H 2-0Et5-C1 0 A-8749 H H H H H S H H 2-0Et6-C1 0 A-8750 H H H H H S H H 2-OEt,5-Me 0 A-8751 H H H H H S H H 2-0Et,6-Me 0 A-8752 H H H H H S H H 2-0CHF 2,b-F 0 A-8753 H H H H H S H H 2-0CHF 2,6-F 0 A-8754 H H H H H S H H 2-0CHF 2 ,5 -M e 0 A-8755 H H H H H S H H 2-0CHF 2,6-M e 0 A-8756 H H H H H S H H 2-(cycbpropybxy),5-F 0 A-8757 H H H H H S H H 2-(cycbpropybxy),6-F 0 A-8758 H H H H H S H H 2-(cyclopropybxy),5-Me 0 A-8759 H H H H H S H H 2-(cyclopropybxy),6-M e 0 A-8760 H H H H H S H H 2-SMe,5-F 0 A-8761 H H H H H S H H 2-SMe,6-F 0 A-8762 H H H H H S H H 2-SMe,5-M e 0 A-8763 H H H H H S H H 2-SMe,6-Me 0 A-8764 H H H H H S H H 2-S(=O)Me,5-F 0 A-8765 H H H H H S H H 2-S(=O)Me,6-F 0 A-8766 H H H H H S H H 2-S(=0)Me,5-M e 0 A-8767 H H H H H S H H 2-S(=0)Me,6-M e 0 A-8768 H H H H H S H H 2-S(=0) 2Me,b-F 0 A-8769 H H H H H S H H 2-S(=0) 2Me,6-F 0 A-8770 H H H H H S H H 2-S(=0) 2 Me,5-M e 0 A-8771 H H H H H S H H 2-S(=0) 2 Me,6--M e 0 A-8772 H H H H H S H H 2-SCF 3 ,b-F 0 A-8773 HH H7 H H S H H 2-SCF 3 ,6-F 0
[0280]
[Table 155]
com pound RI R2 R R R A R R' (R)m P A-8774 H H H H H S H H 2-SCF 3 ,5-M e 0 A-8775 H H H H H S H H 2-SCF 3 ,6-Me 0 A-8776 H H H H H S H H 2-S (=O)CF,5-F 0 A-8777 H H H H H S H H 2-S (=O)F 3 ,6-F 0 A-8778 H H H H H S H H 2-S(=O)CF 3 ,5-Me 0 A-8779 H H H H H S H H 2-S(=O)CF 3 ,6-Me 0 A-8780 H H H H H S H H 2-S(=0) 2CF,5-F 0 A-8781 H H H H H S H H 2-S(=0) 2CF3 ,6-F 0 A-8782 H H H H H S H H 2-S(=0) 2 CF3 ,5-Me 0 A-8783 H H H H H S H H 2-S(=0) 2CF 3 ,6-M e 0 A-8784 H H H H H S H H 2-(cycobpropylthb),5-F 0 A-8785 H H H H H S H H 2-(cycobpropylthb),6-F 0 A-8786 H H H H H S H H 2-(cycbpropylthb),5-M e 0 A-8787 H H H H H S H H 2-(cycbpropylthb),6-Me 0 A-8788 H H H H H S H H 2-C(=0)Me,5-F 0 A-8789 H H H H H S H H 2-C(=0)Me,6-F 0 A-8790 H H H H H S H H 2-C(=0)Me,5-Me 0 A-8791 H H H H H S H H 2-C(=0)Me,6 -M e 0 A-8792 H H H H H S H H 2-CH 20H,b-F 0 A-8793 H H H H H S H H 2-CH 20H,6-F 0 A-8794 H H H H H S H H 2-CH 20H, 5-M e 0 A-8795 H H H H H S H H 2-CH 20H,6-M e 0 A-8796 H H H H H S H H 2-CH 20CH 3 ,4-F 0 A-8797 H H H H H S H H 2-CH 20CH 3 ,5-F 0 A-8798 H H H H H S H H 2-CH 200H 3 ,6-F 0 A-8799 H H H H H S H H 2-CH 20CH 3 .4-M e 0 A-8800 H H H H H S H H 2-CH 20CH 3 ,b-M e 0 A-8801 H H H H H S H H 2-CH 20CH 3 ,6-MAe 0 A-8802 H H H H H S H H 2-0C(=0)CH 3 ,5-F 0 A-8803 H H H H H S H H 2-0C(=0)CH 3 ,6-F 0 A-8804 H H H H H S H H 2-0C(=0)CH 3 ,5-M e 0 A-8805 H H H H H S H H 2-0C(=0)CH 3 ,6-Me 0 A-8806 H H H H H S H H 2-OS(=0) 2CH 3 ,5-F 0 A-8807 H H H H H S H H 2-OS(=O) 20H 3 ,6-F 0 A-8808 H H H H H S H H 2-OS(=0) 2CH 3 ,5-M e 0 A-8809 H H H H H S H H 2-OS(=0) 2CH 3 ,6-M e 0 A-8810 H H H H H S H H 2-CH 2 SCH 3 ,b-F 0 A-8811 H H H H H S H H 2-CH 2 SCH 3 ,6-F 0 A-8812 H H H H H S H H 2-CH 2SCH 3 ,35-Me 0 A-8813 H H H H H S H H 2-CH 2SCH 3 ,6-M e 0 A-8814 H H H H H S H H 2-NM e 2 ,5-F 0 A-8815 H H H H H S H H 2-NMe 2 ,6-F 0 A-8816 H H H H H S H H 2-NMe 2 ,5-MAe 0 A-8817 H H H H H S H H 2-NMe 2 ,6-M e 0 A-8818 H H H H H S H H 2-CNA-F 0 A-8819 H H H H H S H H 2-CN,5-F 0 A-8820 H H H H H S H H 2-CN,6-F 0 A-8821 H H H H H S H H 2-CN,6-Me 0 A-8822 H H H H H S H H 2-CN,5-0Me 0 A-8823 H H H H H S H H 2-CN,6-0Me 0 A-8824 H H H H H S H H 3-CN,6-Me 0 A-8825 H H H H H S H H 3-CN,6-0Me 0 A-8826 H H H H H S H H 4-CN,2-Me 0 A-8827 H H H H H S H H 4-CN,2-0Me 0 A-8828 H H H H H S H H 2-N0 2,4-F 0 A-8829 H H H H H S H H 2-N0 2 ,5-F 0 A-8830 IH IH IH H H S H H 2-N0 2 ,6-F 0
[0281]
[Table 156]
com pound RI R2 R R R A R R' (R)m P A-8831 H H H H H S H H 2-N0 2,4-MAe 0 A-8832 H H H H H S H H 2-N0 2,5-Me 0 A-8833 H H H H H S H H 2-N0 2,6-Me 0 A-8834 H H H H H S H H 2-M e,4,b- 2 0 A-8835 H H H H H S H H 2-M e,6-Et 0 A-8836 H H H H H S H H 2-cyclopropyl,6-OMe 0 A-8837 H H H H H S H H 2-M e,5-Et 0 A-8838 H H H H H S H H 2,6-Et2 0 A-8839 H H H H H S H H 2-Et,6-F 0 A-8840 H H H H H S H H 2-CH 200H 3,6-CI 0 A-8841 H H H H H S H H 2-CH 200H 20H 3 ,6-CI 0 A-8842 H H H H H S H H 2-CH 2 NMe 2 0 A-8843 H H H H H 0 H H H 1 A-8844 H H H H H 0 H H 2-F 1 A-8845 H H H H H 0 H H 3-F 1 A-8846 H H H H H 0 H H 4-F 1 A-8847 H H H H H 0 H H 2-Cl 1 A-8848 H H H H H 0 H H 3-Cl 1 A-8849 H H H H H 0 H H 4-Cl 1 A-8850 H H H H H 0 H H 2-Br 1 A-8851 H H H H H 0 H H 3-Br 1 A-8852 H H H H H 0 H H 4-Br 1 A-8853 H H H H H 0 H H 2-1 1 A-8854 H H H H H 0 H H 3-1 1 A-8855 H H H H H 0 H H 4-1 1 A-8856 H H H H H 0 H H 2-OH 1 A-8857 H H H H H 0 H H 3-OH 1 A-8858 H H H H H 0 H H 4-OH 1 A-8859 H H H H H 0 H H 2-SH 1 A-8860 H H H H H 0 H H 3-SH 1 A-8861 H H H H H 0 H H 4-SH 1 A-8862 H H H H H 0 H H 2-Me 1 A-8863 H H H H H 0 H H 3-Me 1 A-8864 H H H H H 0 H H 4-Me 1 A-8865 H H H H H 0 H H 2-Et 1 A-8866 H H H H H 0 H H 3-Et 1 A-8867 H H H H H 0 H H 4-Et 1 A-8868 H H H H H 0 H H 2-Pr 1 A-8869 H H H H H 0 H H 3-Pr 1 A-8870 H H H H H 0 H H 4-Pr 1 A-8871 H H H H H 0 H H 2-/-Pr 1 A-8872 H H H H H 0 H H 3-/-Pr 1 A-8873 H H H H H 0 H H 4-/-Pr 1 A-8874 H H H H H 0 H H 2-Bu 1 A-8875 H H H H H 0 H H 3-Bu 1 A-8876 H H H H H 0 H H 4-Bu 1 A-8877 H H H H H 0 H H 2-s-Bu 1 A-8878 H H H H H 0 H H 3-s-Bu 1 A -8879 H H H H H 0 H H 4-s-Bu 1 A-8880 H H H H H 0 H H 2-/-Bu 1 A-8881 H H H H H 0 H H 3-/-Bu 1 A-8882 H H H H H 0 H H 4-/-Bu 1 A-8883 H H H H H 0 H H 2-t-Bu 1 A-8884 H H H H H 0 H H 3-t-Bu 1 A -8885 H H H H H 0 H H 4-t-Bu 1 A-8886 H H H H H 0 H H 2-%3 1 A-888 H H H H 0 H H 3-CF3 1
[0282]
[Table 157]
com pound RI R2 R R R A R R' (R)m P A-8888 H H H H H 0 H H 4-CF, 1 A-8889 H H H H H 0 H H 2-CHF 2 1 A-8890 H H H H H 0 H H 3-CHF 2 1 A-8891 H H H H H 0 H H 4-CHF 2 1 A-8892 H H H H H 0 H H 2-CH 2F 1 A-8893 H H H H H 0 H H 3-CH 2F 1 A-8894 H H H H H 0 H H 4-CH 2F 1 A-8895 H H H H H 0 H H 2-CF 2C1 1 A-8896 H H H H H 0 H H 3-CF 2C1 1 A-8897 H H H H H 0 H H 4-0F 201 T A-8898 H H H H H 0 H H 2-UF(CF,) 2 T A-8899 H H H H H 0 H H 3-UF(CF 3 ) 2 T A-8900 H H H H H 0 H H 4-GF(CF 3 ) 2 T A-8901 H H H H H 0 H H 2-cycobpropyl 1 A-8902 H H H H H 0 H H 3-cycobpropyl 1 A-8903 H H H H H 0 H H 4-cycobpropyl 1 A-8904 H H H H H 0 H H 2-cycobutyl 1 A-8905 H H H H H 0 H H 3-cycobbutyl 1 A-8906 H H H H H 0 H H 4-cycobbutyl 1 A-8907 H H H H H 0 H H 2-cycobpentyl 1 A-8908 H H H H H 0 H H 3-cycobpentyl 1 A-8909 H H H H H 0 H H 4-cycobpentyl 1 A-8910 H H H H H 0 H H 2-(cycbpropyh ethyl) 1 A-8911 H H H H H 0 H H 3-(cycbpropyh ethyl) 1 A-8912 H H H H H 0 H H 4-(cycbpropyh ethyl) 1 A-8913 H H H H H 0 H H 2-(cycobbutyhiethyl 1 A-8914 H H H H H 0 H H 3-(cycobbutyhiethyD 1 A-8915 H H H H H 0 H H 4-(cycobbutyhiethyD 1 A-8916 H H H H H 0 H H 2-(cycbpentyhiethyl) 1 A-8917 H H H H H 0 H H 3-(cycbpentyhiethyl) 1 A-8918 H H H H H 0 H H 4-(cycbpentyhiethyD 1 A-8919 H H H H H 0 H H 2-(cycobpropylethyD 1 A-8920 H H H H H 0 H H 3-(cycobpropylethyD 1 A-8921 H H H H H 0 H H 4-(cycobpropylethyD 1 A-8922 H H H H H 0 H H 2-(2,2-difluorocyclopropyD 1 A-8923 H H H H H 0 H H 3-(2,2-diflorocyclopropyD 1 A-8924 H H H H H 0 H H 4-(2,2-difluorocyclopropyl) 1 A-8925 H H H H H 0 H H 2-(2,2-dichbrocycbpropyD 1 A-8926 H H H H H 0 H H 3-(2,2-dichbrocycbpropyD 1 A-8927 H H H H H 0 H H 4-(2,2-dichbrocycbpropyD 1 A-8928 H H H H H 0 H H 2-ethenyl 1 A-8929 H H H H H 0 H H 3-ethenyl 1 A-8930 H H H H H 0 H H 4-ethenyl 1 A-8931 H H H H H 0 H H 2-aIlyl 1 A-8932 H H H H H 0 H H 3-aIlyl 1 A-8933 H H H H H 0 H H 4-aIlyl 1 A-8934 H H H H H 0 H H 2-(prop-1-en-1-y) 1 A-8935 H H H H H 0 H H 3-(prop-1-en-1-y) 1 A-8936 H H H H H 0 H H 4-(prop-1-en-1-y) 1 A-8937 H H H H H 0 H H 2-(trifboroethenyl) 1 A-8938 H H H H H 0 H H 3-(trifboroethenyl) 1 A-8939 H H H H H 0 H H 4-(trifLoroethenyl) 1 A-8940 H H H H H 0 H H 2-(2,2-dichbroethenyD 1 A-8941 H H H H H 0 H H 3-(2,2-dichbroethenyD 1 A-8942 H H H H H 0 H H 4-(2,2-dich broethenyD 1 A-8943 H H H H H 0 H H 2-ethynyl 1 A-8944 FH H H H 0 H H 3-ethyny| T
[0283]
[Table 158]
com pound RI R2 R R R A R R' (R)m P A-8945 Hif5- H H H H 0 H H 4-ethynyl 1 A-8946 H H H H H 0 H H 2-(1-propyn-1-yD 1 A-8947 H H H H H 0 H H 3-(1-propyn-1-y) 1 A-8948 H H H H H 0 H H 4-(1-propyn-1-yD 1 A-8949 H H H H H 0 H H 2-(2-propyn-1-y) 1 A-8950 H H H H H 0 H H 3-(2-propyn-1-y) 1 A-8951 H H H H H 0 H H 4-(2-propyn-1-y) 1 A-8952 H H H H H 0 H H 2-(2-cyclopropylethynyD 1 A-8953 H H H H H 0 H H 3-(2-cyclopropylethynyD 1 A-8954 H H H H H 0 H H 4-(2-cyclopropylethynyD 1 A-8955 H H H H H 0 H H 2-(2-chbroethynyD 1 A-8956 H H H H H 0 H H 3-(2-chbroethynyD 1 A-8957 H H H H H 0 H H 4-(2-chbroethynyD 1 A-8958 H H H H H 0 H H 2-(2-brom oethynyl) 1 A-8959 H H H H H 0 H H 3-(2-brom oethynyl) 1 A-8960 H H H H H 0 H H 4-(2-brom oethynyD 1 A-8961 H H H H H 0 H H 2-0Me 1 A-8962 H H H H H 0 H H 3-0Me 1 A-8963 H H H H H 0 H H 4-0Me 1 A-8964 H H H H H 0 H H 2-0Et 1 A-8965 H H H H H 0 H H 3-0Et 1 A-8966 H H H H H 0 H H 4-0Et 1 A-8967 H H H H H 0 H H 2-0Pr 1 A-8968 H H H H H 0 H H 3-0Pr 1 A-8969 H H H H H 0 H H 4-0Pr 1 A-8970 H H H H H 0 H H 2-0(/-Pr) 1 A-8971 H H H H H 0 H H 3-0(/-Pr) 1 A-8972 H H H H H 0 H H 4-0(/-Pr) 1 A-8973 H H H H H 0 H H 2-0Bu 1 A-8974 H H H H H 0 H H 3-0Bu 1 A-8975 H H H H H 0 H H 4-0Bu 1 A-8976 H H H H H 0 H H 2-0 (s-Bu) 1 A-8977 H H H H H 0 H H 3-0 (s-Bu) 1 A-8978 H H H H H 0 H H 4-0 (s-Bu) 1 A-8979 H H H H H 0 H H 2-0(/-Bu) 1 A-8980 H H H H H 0 H H 3-0(/-Bu) 1 A-8981 H H H H H 0 H H 4-0(/-Bu) 1 A-8982 H H H H H 0 H H 2-0 (t-Bu) 1 A -8983 H H H H H 0 H H 3-0 (t-Bu) 1 A-8984 H H H H H 0 H H 4-0 (t-Bu) 1 A-8985 H H H H H 0 H H 2-0CF3 1 A-8986 H H H H H 0 H H 3-0CF3 1 A-8987 H H H H H 0 H H 4-00F 1 A-8988 H H H H H 0 H H 2-0CHF 2 1 A-8989 H H H H H 0 H H 3-OCHF 2 1 A-8990 H H H H H 0 H H 4-0CHF 2 1 A-8991 H H H H H 0 H H 2-0CH 2 CF3 1 A-8992 H H H H H 0 H H 3-0CH 2 CF3 1 A-8993 H H H H H 0 H H 4-0CH 2 CF3 1 A-8994 H H H H H 0 H H 2-(cycbpropy bxy) 1 A-8995 H H H H H 0 H H 3-(cycbpropy bxy) 1 A-8996 H H H H H 0 H H 4-(cycbpropy bxy) 1 A-8997 H H H H H 0 H H 2-(cycobbutybxy) 1 A-8998 H H H H H 0 H H 3-(cycobbutybxy) 1 A-8999 H H H H H 0 H H 4-(cycobbutybxy) 1 A-9000 H H H H H 0 H H 2-(cycbpenty bxy) 1 A-9001 HHfH H0 H H 3-(cycobpentybxy) 1
[0284]
[Table 159]
com pound RI R2 R R R A R R' (R)m P A-9002 H H H H H 0 H H 4-(cycbpentybxy) 1 A-9003 H H H H H 0 H H 2-((2,2-d bh brocycbpropy Doxy) 1 A-9004 H H H H H 0 H H 3-((2,2-d bh brocycbpropy Doxy) 1 A-9005 H H H H H 0 H H 4-((2,2-dichbrocycbpropyDoxy) 1 A-9006 H H H H H 0 H H 2-(cycbpropyh ethoxy) 1 A-9007 H H H H H 0 H H 3-(cycbpropyh ethoxy) 1 A-9008 H H H H H 0 H H 4-(cycbpropyh ethoxy) 1 A-9009 H H H H H 0 H H 2-((2,2-difluorocycobpropyDm ethoxy) 1 A-9010 H H H H H 0 H H 3-((2,2-difluorocycobpropyDm ethoxy) 1 A-9011 H H H H H 0 H H 4-((2,2-difluorocycobpropyDm ethoxy) 1 A-9012 H H H H H 0 H H 2-(oxiran-2-yD 1 A-9013 H H H H H 0 H H 3-(oxiran-2-y) 1 A-9014 H H H H H 0 H H 4-(oxiran-2-yD 1 A-9015 H H H H H 0 H H 2-(oxiran-2-yh ethyD 1 A-9016 H H H H H 0 H H 3-(oxiran-2-yh ethyD 1 A-9017 H H H H H 0 H H 4-(oxiran-2-yh ethyD 1 A-9018 H H H H H 0 H H 2-SM e 1 A-9019 H H H H H 0 H H 3-SM e 1 A-9020 H H H H H 0 H H 4-SM e 1 A-9021 H H H H H 0 H H 2-SEt 1 A-9022 H H H H H 0 H H 3-SEt 1 A-9023 H H H H H 0 H H 4-SEt 1 A-9024 H H H H H 0 H H 2-S(=0)Me 1 A-9025 H H H H H 0 H H 3-S(=0)Me 1 A-9026 H H H H H 0 H H 4-S(=0)Me 1 A-9027 H H H H H 0 H H 2-S(=0) 2Me 1 A-9028 H H H H H 0 H H 3-S(=0) 2Me 1 A-9029 H H H H H 0 H H 4-S (=0)2M e 1 A-9030 H H H H H 0 H H 2-SCF, 1 A-9031 H H H H H 0 H H 3-SCF, 1 A-9032 H H H H H 0 H H 4-SCF, 1 A-9033 H H H H H 0 H H 2-S(=0)CF3 1 A-9034 H H H H H 0 H H 3-S(=0)CF3 1 A-9035 H H H H H 0 H H 4-S(=0)CF3 1 A-9036 H H H H H 0 H H 2-S (=0) 2CF3 1 A-9037 H H H H H 0 H H 3-S (=0) 2CF 3 1 A-9038 H H H H H 0 H H 4-S (=0) 2CF 3 1 A-9039 H H H H H 0 H H 2-SCF(CF3) 2 1 A-9040 H H H H H 0 H H 3-SCF(CF3) 2 1 A-9041 H H H H H 0 H H 4-SCF(CF 3) 2 1 A-9042 H H H H H 0 H H 2-(cycobpropy fth b) 1 A-9043 H H H H H 0 H H 3-(cycobpropy th b) 1 A-9044 H H H H H 0 H H 4-(cycobpropy th b) 1 A-9045 H H H H H 0 H H 2-(cycbpropylsulfhy) 1 A-9046 H H H H H 0 H H 3-(cycbpropylsulfhy) 1 A-9047 H H H H H 0 H H 4-(cycbpropylsulfhy) 1 A-9048 H H H H H 0 H H 2-(cycobpropysufonyD 1 A-9049 H H H H H 0 H H 3-(cycbpropysulfonyl) 1 A-9050 H H H H H 0 H H 4-(cycbpropysulfonyl) 1 A-9051 H H H H H 0 H H 2-((cycobpropyhiethyDthio) 1 A-9052 H H H H H 0 H H 3-((cycobpropyhiethyDthio) 1 A-9053 H H H H H 0 H H 4-((cycobpropyhiethyDthio) 1 A-9054 H H H H H 0 H H 2-((cycbpropy I ethy Dsu finy D 1 A-9055 H H H H H 0 H H 3-((cycbpropy I ethy Dsu finy D 1 A-9056 H H H H H 0 H H 4-((cycbpropy I ethy Dsu finy D 1 A-9057 H H H H H 0 H H 2-((cyclopropyhiethyDsulfonyD 1 A-9058 H HffH H 0 H H 3-((cyclopropyhiethyDsufonyl) 1
[0285]
[Table 160]
com pound R' R2 R R A R R' (R)m p A-9059 H H H H 0 H H 4-((cyclopropyh ethy Dsu fonyD 1 A-9060 H H H H i 0 H H 2-(((2,2-d ifuorocycbpropy Dm ethyDtho) A-9061 H H H H 0 H H 3-(((2,2-d ifuorocycbpropy Dm ethyDthb) 1 A-9062 H H H H i 0 H H 4-(((2,2-d ifuorocycbpropy Dm ethy Dtho) A-9063 H H H H 0 H H 2-(((2,2-d fluorocycbpropy Dm ethy Dsu finy D 1 A-9064 H H H H 0 H H 3-(((2,2-d fluorocycbpropy Dm ethy Dsu finy D 1 A-9065 H H H H 0 H H 4-(((2,2-d fluorocycbpropy Dm ethy Dsu finy D 1 A-9066 H H H H 0 H H 2-(((2,2-d fuorocycbpropy Dm ethy Dsu many D 1 A-9067 H H H H 0 H H 3-(((2,2-d fuorocycbpropy Dm ethy Dsu many D 1 A-9068 H H H H 0 H H 4-(((2,2-d fuorocycbpropy Dm ethy Dsu many D 1 A-9069 H H H H 0 H H 2- (= )M e A-90/0 H H H H f Di H H 3- (=0)M e 1 A-901 H H H H 0 H H 4- (= )M e A-9072 H H H H 0Di H H 2- (= 0)Et 1 A-90/3 H H H H 0Di H H 3- (= 0)Et 1 A-9074 H H H H HD0 H H 4-C 0Et T A-9075 H H H H f0 H H 2-C(= 0)G 3 A-9076 H H H H 0 H H 3-C(= 0)C 3 A-9077 H H H H f0 H H 4-C(= 0)G 3 A-9078 H H H H 0 H H 2-C(= 0)0M e 1 A-90/79 H H H H 0 H H 3-C(= 0)0M e A-9080 H H H H f0 H H 4-C(= 0)0M e A-9081 H H H H 0 H H 2-C (=0 )0Et 1 A-9082 H H H H f0 H H 3-C (=0 )0Et A-9083 H H H H HD0 H H 4- 0(= )0Et A-9084 H H H H f0 H H 2-C = U)NH 2 A-9085 H H H H f0 H H 3-C = U)NH 2 A-9086 H H H H i 0 H H 4-C = U)NH 2 A-9087 H H H H 0 H H 2-C (= 0)NHM e 1 A-9088 H H H H 0 H H 3-C (= 0)NHM e 1 A-9089 H H H H 0 H H 4-C (= 0)NHM e 1 A-9090 H H H H 0 H H 2-C (=0 )NM e2 T A-9091 H H H H HD0 H H 3-C (=0 )NM e 2 T A-9092 H H H H f0 H H 4-C (=0 )NM e 2 T A-9093 H H H H 0 H H 2-CH 2C =0 )H 3 T A-9094 H H H H 0 H H 3-CH 2 C= 0)GH 3 A-9095 H H H H f0 H H 4-CH 2 C(= 0)H 3 A-9096 H H H H 0 H H 2-CH 2 C(=0 )C 3 A-9097 H H H H 0 H H 3-CH 2 C(=0 )0 3 A-9098 H H H H 0Di H H 4-CH 2 (=0)CF U 3 A-9099 H H IHH 0 H H 2-CH 2C =0 )0H 3 A-9100 H H H H 0 H H 3-CH 2C (=0 )0H 3 A-9101 H H H H f0 H H 4-CH 2C (=0 )0H 3 A-9102 H H H H 0 H H 2-CH 20H A-9103 H H H H 0 H H 3-CH 20H A-9104 H H H H f0 H H 4-CH 20H A-9105 H H H H 0Di H H 2-CH 20H 3 1
A-9106 H H H H 0 H H 3-CH 20H 3 1
A-9107 H H H H 0 H H 4-CH 20H 3 1
A-9108 H H H H f0 H H 2-CH 20H 2CH 3 T A-9109 H H H H 0 H H 3-CH 20H 2CH 3 T A-9110 H H H H f0 H H 4-CH 20H 2CH 3 T A-9111 H H H H f0 H H 2-GH (GH 3 )0H 3 T A-9112 H H H H 0 H H 3-GH (CH 3 )0H 3 T A-9113 H H H H f0 H H 4-GH(H 3 )0H 3 T A-9114 H H H H f0 H H 2-CH 2 CH 2UGH 3 T A-911b H H H H 0 H H 3-CH 20H 2UGH 3 T
[0286]
[Table 161]
com pound R' R2 R R A R R' (R)m p A-9116 H H H H 0 H H 4-0H 20H 20H 3 1 A-9117 H H H H f0 H H 2-0H 20F 3 T A-9118 H H H H 0 H H 3-0H 20F 3 T A-9119 H H H H i 0 H H 4-GH 20F 3 T A-9120 H H H H 0 H H 2-0F 20H 3 T A-9121 H H H H 0 H H 3-0F 20H 3 1 A-9122 H H H H 0 H H 4-0F 20H 3 1 A-9123 H H H H 0 H H 2-CFGF 2 2 0F 3 1 A-9124 H H H H H 0 H H 3-CFGF 2 2 0F 1 A-9125 H H H H 0 H H 4-GF 2 F 2 0G 3 T A-9126 H H H H i 0 H H 2-C(=U)GH 3 T A-9127 H H H H 0 H H 3-C(=U)GH 3 T A-9128 H H H H H0 H H 4-C(=U)GH 3 T A-9129 H H H H 0 H H 2-0C(= U)F 3 1 A-9130 H H H H 0 H H 3-UC(=U)F 3 1 A-9131 H H H H H0 H H 4-C(=U)GH 3 T A-9132 H H H H HD0 H H 2-UC(=U)NH 2 T A-9133 H H H H E 0 H H 3-0(= 0)NH 2 A-9134 H H H H H0 H H 4-UC(=U)NH 2 T A-9135 H H H H 0 H H 2-O(=U)NHOH 3 1 A-9136 H H H H H0 H H 3-O(=U)NHGH 3 T A-9137 H H H H H0 H H 4-O(=U)NHGH 3 T A-9138 H H H H 0 H H 2-UC(=0)N(CH3) 2 A-9139 H H H H Hi0 H H 3-UC(=0)N(H 3) 2 T A-9140 H H H H HD0 H H 4-UC(=U)N(GH 3) 2 T A-9141 H H H H H0 H H 2-GH 20(=O)NH 2 T A-9142 H H H H H0 H H 3-GH 20(=O)NH 2 T A-9143 H H H H i 0 H H 4-GH 2 0C(=U)NH 2 A-9144 H H H H 0 H H 2-GH 20C(=U)NHGH 3 T A-9145 H H H H 0 H H 3-0H 20(=U)NHGH 3 1 A-9146 H H H H 0 H H 4-GH 20(=U)NHGH 3 T A-9147 H H H H 0 H H 2-GH 20(= )N (H 3) 2 A-9148 H H H H H0 H H 3-GH 20C(=U)N (H 3) 2 A-9149 H H H H H0 H H 4-GH 20(=O)N (GH 3) 2 A-9150 H H H H 0 H H 2-UO(=U)OH 3 T A-9151 H H H H 0 H H 3-OC(=O)UGH 3 T A-9152 H H H H H0 H H 4-OC(=O)UGH 3 A-9153 H H H H 0 H H 2-GH 20C(=U)OH 3 A-9154 H H H H 0 H H 3-0H 20(=U)UGH 3 1 A-9155 H H H H 0Di H H 4-GH 20C(=U)OH 3 1 A-9156 H H H H 0 H H 2-0H 20(=U)GH 3 1 A-9157 H H H H 0 H H 3-GH 20C(=U)H 3 T A-9158 H H H H H0 H H 4-GH 20(=O)GH 3 T A-9159 H H H H 0 H H 2-U S=U) 2 CH 3 A-9160 H H H H 0 H H 3-USt=U) 20H 3 A-9161 H H H H H0 H H 4-U S=U) 20H 3 A-9162 H H H H 0Di H H 2-CH 2SOH 3 T A-9163 H H H H 0 H H 3-CH 2SOH 3 T A-9164 H H H H 0 H H 4-CH 2SOH 3 T A-9165 H H H H H0 H H 2-CH 2S(=U)GH 3 T A-9166 H H H H 0 H H 3-CH 2S(=0)CH 3 T A-9167 H H H H 0 H H 4-CH 2S(=U)GH 3 T A-9168 H H H H 0 H H 2-CH 2S(=U) 20H 3 T A-9169 H H H H 0 H H 3-CH 2S (=0) 2 H 3 T A-9170 H H H H 0 H H 4-CH 2S(=0) 2 CH 3 T A-9171 IH H H H 0 H H 2-CH 2SCF 3 T A-9172 Hfi HfH i H H 3-CH2SGF 3
[0287]
[Table 162]
com pound RI R2 R R R A R R' (R)m P A-9173 i H H H H H 0 H H 4-C2HSCF 1 A-9174 H H H H H 0 H H 2-CH 2S(=O)CF 1 A-9175 H H H H H 0 H H 3-CH 2S(=O)CF 1 A-9176 H H H H H 0 H H 4-CH 2S(=O0)CI 3 1 A-9177 H H H H H 0 H H 2-CH 2S(=0) 2CF T A-9178 H H H H H 0 H H 3-CH 2S(=0) 2CF 1 A-9179 H H H H H 0 H H 4-CH 2S(=0) 2CF 1 A-9180 H H H H H 0 H H 2-phenyl 1 A-9181 H H H H H 0 H H 3-phenyl 1 A-9182 H H H H H 0 H H 4-phenyl 1 A-9183 H H H H H 0 H H 2-(phenyloxy) 1 A-9184 H H H H H 0 H H 3-(pheny loxy) 1 A-9185 H H H H H 0 H H 4-(phenyloxy) 1 A-9186 H H H H H 0 H H 2-benzyl 1 A-9187 H H H H H 0 H H 3-benzyl 1 A-9188 H H H H H 0 H H 4-benzyl 1 A-9189 H H H H H 0 H H 2-(benzy bxy) 1 A-9190 H H H H H 0 H H 3-(benzy bxy) 1 A-9191 H H H H H 0 H H 4-(benzy bxy) 1 A-9192 H H H H H 0 H H 2-((2-fborobenzy Doxy) 1 A-9193 H H H H H 0 H H 3-((2-fborobenzy Doxy) 1 A-9194 H H H H H 0 H H 4-((2-fLorobenzy Doxy) 1 A-9195 H H H H H 0 H H 2-((3-fLorobenzy Doxy) 1 A-9196 H H H H H 0 H H 3-((3-fborobenzy Doxy) 1 A-9197 H H H H H 0 H H 4-((3-fLorobenzy Doxy) 1 A-9198 H H H H H 0 H H 2-((4-fLorobenzyDoxy) 1 A-9199 H H H H H 0 H H 3-((4-fLorobenzyDoxy) 1 A-9200 H H H H H 0 H H 4-((4-fLorobenzyDoxy) 1 A-9201 H H H H H 0 H H 2-((2-ch brobenzyDoxy) 1 A-9202 H H H H H 0 H H 3-((2-ch brobenzyDoxy) 1 A-9203 H H H H H 0 H H 4-((2-chbrobenzyDoxy) 1 A-9204 H H H H H 0 H H 2-((3-ch brobenzyDoxy) 1 A-9205 H H H H H 0 H H 3-((3-ch brobenzyDoxy) 1 A-9206 H H H H H 0 H H 4-((3-ch brobenzyDoxy) 1 A-9207 H H H H H 0 H H 2-((4-ch brobenzyDoxy) 1 A-9208 H H H H H 0 H H 3-((4-ch brobenzyDoxy) 1 A-9209 H H H H H 0 H H 4-((4-ch brobenzyDoxy) 1 A-9210 H H H H H 0 H H 2-((2-m ethylbenzyDoxy) 1 A-9211 H H H H H 0 H H 3-((2-m ethylbenzyDoxy) 1 A-9212 H H H H H 0 H H 4-((2-m ethylbenzyDoxy) 1 A-9213 H H H H H 0 H H 2-((3-m ethylbenzyDoxy) 1 A-9214 H H H H H 0 H H 3-((3-m ethylbenzyDoxy) 1 A-9215 H H H H H 0 H H 4-((3-m ethylbenzyDoxy) 1 A-9216 H H H H H 0 H H 2-((4-m ethylbenzyDoxy) 1 A-9217 H H H H H 0 H H 3-((4-m ethylbenzyDoxy) 1 A-9218 H H H H H 0 H H 4-((4-m ethylbenzyDoxy) 1 A-9219 H H H H H 0 H H 2-((2-(trifforom ethyDbenzyDoxy) 1 A-9220 H H H H H 0 H H 3-((2-(trfborom ethyDbenzyDoxy) 1 A-9221 H H H H H 0 H H 4-((2-(trfborom ethyDbenzyDoxy) 1 A-9222 H H H H H 0 H H 2-((3-(trfborom ethyDbenzyDoxy) 1 A-9223 H H H H H 0 H H 3-((3-(trfborom ethyDbenzyDoxy) 1 A-9224 H H H H H 0 H H 4-((3-(trifborom ethyDbenzyDoxy) 1 A-9225 H H H H H 0 H H 2-((4-(trfborom ethyDbenzyDoxy) 1 A-9226 H H H H H 0 H H 3-((4-(trfborom ethyDbenzyDoxy) 1 A-9227 H H H H H 0 H H 4-((4-(trifborom ethyDbenzyDoxy) 1 A-9228 H H H H H 0 H H 2-((2-m ethoxybenzyDoxy) 1 A-9229 H Hf H H 0 H H 3-((2-m ethoxybenzyDoxy) 1
[0288]
[Table 163]
com pound RI R2 R R R A R R' (R)m P A-9230 H H H H H 0 H H 4-((2-m ethoxybenzyDoxy) 1 A-9231 H H H H H 0 H H 2-((3-m ethoxybenzyDoxy) T A-9232 H H H H H 0 H H 3-((3-m ethoxybenzyDoxy) T A-9233 H H H H H 0 H H 4-((3-m ethoxybenzyDoxy) T A-9234 H H H H H 0 H H 2-((4-m ethoxybenzyDoxy) T A-9235 H H H H H 0 H H 3-((4-m ethoxybenzyDoxy) 1 A-9236 H H H H H 0 H H 4-((4-m ethoxybenzyDoxy) 1 A-9237 H H H H H 0 H H 2-((2-(trifluorom ethoxy)benzyDoxy) 1 A-9238 H H H H H 0 H H 3-((2-(trifluorom ethoxy)benzyDoxy) 1 A-9239 H H H H H 0 H H 4-((2-(trifluorom ethoxy)benzyDoxy) 1 A-9240 H H H H H 0 H H 2-((3-(trifluorom ethoxy)benzyDoxy) 1 A-9241 H H H H H 0 H H 3-((3-(trifluorom ethoxy)benzyDoxy) 1 A-9242 H H H H H 0 H H 4-((3-(trifluorom ethoxy)benzyDoxy) 1 A-9243 H H H H H 0 H H 2-((4-(trifluorom ethoxy)benzyDoxy) 1 A-9244 H H H H H 0 H H 3-((4-(trifluorom ethoxy)benzyDoxy) 1 A-9245 H H H H H 0 H H 4-((4-(trifluorom ethoxy)benzyDoxy) 1 A-9246 H H H H H 0 H H 2-((2-(m ethylthio)benzyl)oxy) 1 A-9247 H H H H H 0 H H 3-((2-(m ethylthio)benzyDoxy) 1 A-9248 H H H H H 0 H H 4-((2-(m ethylthio)benzyl)oxy) 1 A-9249 H H H H H 0 H H 2-((3-(m ethylthio)benzyDoxy) 1 A-9250 H H H H H 0 H H 3-((3-(m ethylthio)benzyl)oxy) 1 A-9251 H H H H H 0 H H 4-((3-(m ethylthio)benzyl)oxy) 1 A-9252 H H H H H 0 H H 2-((4-(m ethylthio)benzyDoxy) 1 A-9253 H H H H H 0 H H 3-((4-(m ethylthio)benzyl)oxy) 1 A-9254 H H H H H 0 H H 4-((4-(m ethylthio)benzyl)oxy) 1 A-9255 H H H H H 0 H H 2-((2-(m ethylsulhyDbenzyDoxy) 1 A-9256 H H H H H 0 H H 3-((2-(m ethylsulhyDbenzyDoxy) 1 A-9257 H H H H H 0 H H 4-((2-(m ethylsulhyDbenzyDoxy) 1 A-9258 H H H H H 0 H H 2-((3-(m ethylsulhyDbenzyDoxy) 1 A-9259 H H H H H 0 H H 3-((3-(m ethylsulhyDbenzyDoxy) 1 A-9260 H H H H H 0 H H 4-((3-(m ethylsulhyDbenzyDoxy) 1 A-9261 H H H H H 0 H H 2-((4-(m ethylsulhyDbenzyDoxy) 1 A-9262 H H H H H 0 H H 3-((4-(m ethylsulhyDbenzyDoxy) 1 A-9263 H H H H H 0 H H 4-((4-(m ethylsulhyDbenzyDoxy) 1 A-9264 H H H H H 0 H H 2-((2-(m ethyIsulfonyDbenzyDoxy) 1 A-9265 H H H H H 0 H H 3-((2-(m ethyIsulfonyDbenzyDoxy) 1 A-9266 H H H H H 0 H H 4-((2-(m ethyIsulfonyDbenzyDoxy) 1 A-9267 H H H H H 0 H H 2-((3-(m ethyIsulfonyDbenzyDoxy) 1 A-9268 H H H H H 0 H H 3-((3-(m ethyIsulfonyDbenzyDoxy) 1 A-9269 H H H H H 0 H H 4-((3-(m ethyIsulfonyDbenzyDoxy) 1 A-9270 H H H H H 0 H H 2-((4-(m ethyIsulfonyDbenzyDoxy) 1 A-9271 H H H H H 0 H H 3-((4-(m ethyIsulfonyDbenzyDoxy) 1 A-9272 H H H H H 0 H H 4-((4-(m ethyIsulfonyDbenzyDoxy) 1 A-9273 H H H H H 0 H H 2-((2-(trifluorom ethylthio)benzyDoxy) 1 A-9274 H H H H H 0 H H 3-((2-(trifluorom ethy lth io)benzy Doxy) 1 A-9275 H H H H H 0 H H 4-((2-(trifluorom ethylthio)benzyDoxy) 1 A-9276 H H H H H 0 H H 2-((3-(trifluorom ethylthio)benzyDoxy) 1 A-9277 H H H H H 0 H H 3-((3-(trifluorom ethylthio)benzyDoxy) 1 A-9278 H H H H H 0 H H 4-((3-(trifluorom ethylthio)benzyDoxy) 1 A-9279 H H H H H 0 H H 2-((4-(trifluorom ethylthio)benzyDoxy) 1 A-9280 H H H H H 0 H H 3-((4-(trifluorom ethylthio)benzyDoxy) 1 A-9281 H H H H H 0 H H 4-((4-(trifluorom ethylthio)benzyDoxy) 1 A-9282 H H H H H 0 H H 2-((2-(trifluorom ethyIsulfinyDbenzyDoxy) 1 A-9283 H H H H H 0 H H 3-((2-(trifluorom ethyIsulfinyDbenzyDoxy) 1 A-9284 H H H H H 0 H H 4-((2-(trifluorom ethyIsulfinyDbenzyDoxy) 1 A-9285 H H H H H 0 H H 2-((3-(trifluorom ethyIsulfinyDbenzyDoxy) 1 A-9286 H H H H H0 H H 3-((3-(trfluorom ethyIsufinyl)benzyl)oxy) 1
[0289]
[Table 164]
com pound RI R2 R R R A R R' (R)m P A-9287 H H H H H 0 H H 4-((3-(trifluorom ethyIsulfinyDbenzyDoxy) 1 A-9288 H H H H H 0 H H 2-((4-(trifluorom ethyIsulfinyDbenzyDoxy) 1 A-9289 H H H H H 0 H H 3-((4-(trifluorom ethyIsulfinyDbenzyDoxy) 1 A-9290 H H H H H 0 H H 4-((4-(trifluorom ethyIsulfinyDbenzyDoxy) 1 A-9291 H H H H H 0 H H 2-((2-(trifluorom ethylsulfony)benzyDoxy) 1 A-9292 H H H H H 0 H H 3-((2-(trifluorom ethylsulfonyI)benzyDoxy) 1 A-9293 H H H H H 0 H H 4-((2-(trifluorom ethylsulfonyI)benzyDoxy) 1 A-9294 H H H H H 0 H H 2-((3-(trifluorom ethylsulfonyI)benzyDoxy) 1 A-9295 H H H H H 0 H H 3-((3-(trifluorom ethylsulfonyI)benzyDoxy) 1 A-9296 H H H H H 0 H H 4-((3-(trifluorom ethylsulfonyI)benzyDoxy) 1 A-9297 H H H H H 0 H H 2-((4-(trifluorom ethylsulfonyI)benzyDoxy) 1 A-9298 H H H H H 0 H H 3-((4-(trifluorom ethylsulfonyI)benzyDoxy) 1 A-9299 H H H H H 0 H H 4-((4-(trifluorom ethylsulfonyI)benzyDoxy) 1 A-9300 H H H H H 0 H H 2-((2-am inobenzyDoxy) 1 A-9301 H H H H H 0 H H 3-((2-am inobenzyDoxy) 1 A-9302 H H H H H 0 H H 4-((2-am inobenzyDoxy) 1 A-9303 H H H H H 0 H H 2-((3-am inobenzyDoxy) 1 A-9304 H H H H H 0 H H 3-((3-am inobenzyDoxy) 1 A-9305 H H H H H 0 H H 4-((3-am inobenzyDoxy) 1 A-9306 H H H H H 0 H H 2-((4-am inobenzyDoxy) 1 A-9307 H H H H H 0 H H 3-((4-am inobenzyDoxy) 1 A-9308 H H H H H 0 H H 4-((4-am inobenzyDoxy) 1 A-9309 H H H H H 0 H H 2-((2-(m ethybm ho)benzyDoxy) 1 A-9310 H H H H H 0 H H 3-((2-(m ethy bm ho)benzy Doxy) 1 A-9311 H H H H H 0 H H 4-((2-(m ethy bm ho)benzy Doxy) 1 A-9312 H H H H H 0 H H 2-((3-(m ethy bm ho)benzy Doxy) 1 A-9313 H H H H H 0 H H 3-((3-(m ethy bm ho)benzy Doxy) 1 A-9314 H H H H H 0 H H 4-((3-(m ethy bm ho)benzy Doxy) 1 A-9315 H H H H H 0 H H 2-((4-(m ethy bm ho)benzy Doxy) 1 A-9316 H H H H H 0 H H 3-((4-(m ethy bm ho)benzy Doxy) 1 A-9317 H H H H H 0 H H 4-((4-(m ethy bm ho)benzy Doxy) 1 A-9318 H H H H H 0 H H 2-((2-(d iethylam ino)benzyDoxy) 1 A-9319 H H H H H 0 H H 3-((2-(d iethylam ino)benzyDoxy) 1 A-9320 H H H H H 0 H H 4-((2-(d iethylam ino)benzyDoxy) 1 A-9321 H H H H H 0 H H 2-((3-(d iethylam ino)benzyDoxy) 1 A-9322 H H H H H 0 H H 3-((3-(d iethylam ino)benzyDoxy) 1 A-9323 H H H H H 0 H H 4-((3-(d iethylam ino)benzyDoxy) 1 A-9324 H H H H H 0 H H 2-((4-(d iethylam ino)benzyDoxy) 1 A-9325 H H H H H 0 H H 3-((4-(d iethylam ino)benzyDoxy) 1 A-9326 H H H H H 0 H H 4-((4-(d iethylam ino)benzyDoxy) 1 A-9327 H H H H H 0 H H 2-((2-cyanobenzy Doxy) 1 A-9328 H H H H H 0 H H 3-((2-cyanobenzy Doxy) 1 A-9329 H H H H H 0 H H 4-((2-cyanobenzy Doxy) 1 A-9330 H H H H H 0 H H 2-((3-cyanobenzy Doxy) 1 A-9331 H H H H H 0 H H 3-((3-cyanobenzy Doxy) 1 A-9332 H H H H H 0 H H 4-((3-cyanobenzy Doxy) 1 A-9333 H H H H H 0 H H 2-((4-cyanobenzyDoxy) 1 A-9334 H H H H H 0 H H 3-((4-cyanobenzyDoxy) 1 A-9335 H H H H H 0 H H 4-((4-cyanobenzyDoxy) 1 A-9336 H H H H H 0 H H 2-((2-nitrobenzyDoxy) 1 A-9337 H H H H H 0 H H 3-((2-nitrobenzyDoxy) 1 A-9338 H H H H H 0 H H 4-((2-nitrobenzyDoxy) 1 A-9339 H H H H H 0 H H 2-((3-nitrobenzyDoxy) 1 A-9340 H H H H H 0 H H 3-((3-nitrobenzyDoxy) 1 A-9341 H H H H H 0 H H 4-((3-nitrobenzyDoxy) 1 A-9342 H H HIH H 0 H H 2-((4-nitrobenzyDoxy) 1 A-9343 i f Hi H 0 H H 3-((4-nitrobenzyDoxy) T
[0290]
[Table 165]
com pound RI R2 R R R A R R' (R)m P A-9344 H H H H H 0 H H 4-((4-nitrobenzyDoxy) 1 A-9345 H H H H H 0 H H 2-NH 2 A-9346 H H H H H 0 H H 3-NH 2 A-9347 H H H H H 0 H H 4-NH 2 A-9348 H H H H H 0 H H 2-N HM e 1 A-9349 H H H H H 0 H H 3-N HM e 1 A-9350 H H H H H 0 H H 4-N HM e 1 A-9351 H H H H H 0 H H 2-NH Et 1 A-9352 H H H H H 0 H H 3-NH Et 1 A-9353 H H H H H 0 H H 4-NH Et 1 A-9354 H H H H H 0 H H 2-N (e) 2 A-9355 H H H H H 0 H H 3-N (e) 2 A-9356 H H H H H 0 H H 4-N (e) 2 A-9357 H H H H H 0 H H 2-N (Et) 2 A-9358 H H H H H 0 H H 3-N (Et) 2 A-9359 H H H H H 0 H H 4-N(Et) 2 A-9360 H H H H H 0 H H 2-CHO 1 A-9361 H H H H H 0 H H 3-CHO 1 A-9362 H H H H H 0 H H 4-CHO 1 A-9363 H H H H H 0 H H 2-C (= )0H 1 A-9364 H H H H H 0 H H 3-C (= )0H 1 A-9365 H H H H H 0 H H 4-C (= )0H 1 A-9366 H H H H H 0 H H 2-(1,3-dioxolan-2-yD 1 A-9367 H H H H H 0 H H 3-(1,3-dioxolan-2-yD 1 A-9368 H H H H H 0 H H 4-(1,3-dioxolan-2-yD 1 A-9369 H H H H H 0 H H 2-(1,3-dioxan-2-yD 1 A-9370 H H H H H 0 H H 3-(1,3-dioxan-2-yD 1 A-9371 H H H H H 0 H H 4-(1,3-dioxan-2-yD 1 A-9372 H H H H H 0 H H 2-(1H-in idazol-2-yD 1 A-9373 H H H H H 0 H H 3-(1H-in idazol-2-yD 1 A-9374 H H H H H 0 H H 4-(1H-in idazol-2-yD 1 A-9375 H H H H H 0 H H 2-(thiazol-2-yl) 1 A-9376 H H H H H 0 H H 3-(thiazol-2-yl) 1 A-9377 H H H H H 0 H H 4-(thiazol-2-yl) 1 A-9378 H H H H H 0 H H 2-(oxazol-2-yD 1 A-9379 H H H H H 0 H H 3-(oxazol-2-yD 1 A-9380 H H H H H 0 H H 4-(oxazol-2-yD 1 A-9381 H H H H H 0 H H 2-CH= NOH 1 A-9382 H H H H H 0 H H 3-CH= NOH 1 A-9383 H H H H H 0 H H 4-CH= NOH 1 A-9384 H H H H H 0 H H 2-CH= NOM e 1 A-9385 H H H H H 0 H H 3-CH= NOM e 1 A-9386 H H H H H 0 H H 4-CH= NOM e 1 A-9387 H H H H H 0 H H 2-(4,5-dihydro-3-soxazolyD 1 A-9388 H H H H H 0 H H 3-(4,5-d ihydro-3-isoxazo l D 1 A-9389 H H H H H 0 H H 4-(4,5-dihydro-3-soxazolyD 1 A-9390 H H H H H 0 H H 2-CN 1 A-9391 H H H H H 0 H H 3-CN 1 A-9392 H H H H H 0 H H 4-CN 1 A-9393 H H H H H 0 H H 2-N0 2 T A-9394 H H H H H 0 H H 3-N0 2 T A-9395 H H H H H 0 H H 4-N0 2 T A-9396 H H H H H 0 H H 2,3--2 A-9397 H H H H H 0 H H 2,4-F 2 T A-9398 H H H H H 0 H H 2,5-F 2 A-9399 H H H H H 0 H H 2,6--2 A-9400 IH H HIH H 0 H H 3,4-F 2
[0291]
[Table 166]
com pound RI R2 R R R A R R' (R)m P A-9401 H H H H H 0 H H 3,5-F2 1 A-9402 H H H H H 0 H H 2-F,3-OI 1 A-9403 H H H H H 0 H H 2-F,4-0| 1 A-9404 H H H H H 0 H H 2-F,5-C| 1 A-9405 H H H H H 0 H H 2-F,6-C| 1 A-9406 H H H H H 0 H H 3-F,2-0| 1 A-9407 H H H H H 0 H H 3-F,4-0| 1 A-9408 H H H H H 0 H H 3-F,5-C| 1 A-9409 H H H H H 0 H H 3-F,6-C| 1 A-9410 H H H H H 0 H H 4-F,2-C| 1 A-9411 H H H H H 0 H H 4-F,3-C| 1 A-9412 H H H H H 0 H H 2-F,3-Me 1 A-9413 H H H H H 0 H H 2-F,4--M e 1 A-9414 H H H H H 0 H H 2-F,5-Me 1 A-9415 H H H H H 0 H H 2-F,6-Me 1 A-9416 H H H H H 0 H H 3-F,2-Me 1 A-9417 H H H H H 0 H H 3-F,4--M e 1 A-9418 H H H H H 0 H H 3-F,5-Me 1 A-9419 H H H H H 0 H H 3-F,6-Me 1 A-9420 H H H H H 0 H H 4-F,2-Me 1 A-9421 H H H H H 0 H H 4-F,3-Me 1 A-9422 H H H H H 0 H H 2-F,3-CF, 1 A-9423 H H H H H 0 H H 2-F,4-CF, 1 A-9424 H H H H H 0 H H 2-F,5 -CF 1 A-9425 H H H H H 0 H H 2-F,6-F 3 1 A-9426 H H H H H 0 H H 3-F,2-F 3 1 A-9427 H H H H H 0 H H 3-F,4-O% 1 A-9428 H H H H H 0 H H 3-F,5-CF3 1 A-9429 H H H H H 0 H H 3-F6-CF 3 1 A-9430 H H H H H 0 H H 4-F,2-CF3 1 A-9431 H H H H H 0 H H 4-F,3-CF3 1 A-9432 H H H H H 0 H H 2-F,3-0Me 1 A-9433 H H H H H 0 H H 2-F,4-0Me 1 A-9434 H H H H H 0 H H 2-F,5-0Me 1 A-9435 H H H H H 0 H H 2-F,6-0Me 1 A-9436 H H H H H 0 H H 3-F,2-0Me 1 A-9437 H H H H H 0 H H 3-F,4-0Me 1 A-9438 H H H H H 0 H H 3-F,5-0Me 1 A-9439 H H H H H 0 H H 3-F,6-0Me 1 A-9440 H H H H H 0 H H 4-F,2-0Me 1 A-9441 H H H H H 0 H H 4-F,3-0Me 1 A-9442 H H H H H 0 H H 2,3-C 1 A-9443 H H H H H 0 H H 2,4-X 1 A-9444 H H H H H 0 H H 2,b-0 1 A-9445 H H H H H 0 H H 2,6-O 1 A-9446 H H H H H 0 H H 3,4- 1 A-9447 H H H H H 0 H H 3,5-C 1 A-9448 H H H H H 0 H H 2-CI,3-Me 1 A-9449 H H H H H 0 H H 2-CI,4-Me 1 A-9450 H H H H H 0 H H 2-CI,5-Me 1 A-9451 H H H H H 0 H H 2-CI,6-Me 1 A-9452 H H H H H 0 H H 3-CI,2-Me 1 A-9453 H H H H H 0 H H 3-CI,4-Me 1 A-9454 H H H H H 0 H H 3-CI,5-Me 1 A-9455 H H H H H 0 H H 3-C,6-Me 1 A-9456 H H H H H 0 H H 4-C,2-Me 1 A-9457 HF FH IH 0 H H 4-C,3-Me T
[0292]
[Table 167]
com pound RI R2 R R R A R R' (R)m P A-9458 H H H H H 0 H H 2-C 1,3-CF, 1 A-9459 H H H H H 0 H H 2-C I,4-CF 1 A-9460 H H H H H 0 H H 2-C 1,5-CF 1 A-9461 H H H H H 0 H H 2-01 ,6-GF, 1 A-9462 H H H H H 0 H H 3-C 1,2-CF, 1 A-9463 H H H H H 0 H H 3-C I,4-CF 1 A-9464 H H H H H 0 H H 3-C 1,5-CF 1 A-9465 H H H H H 0 H H 3-C 1,6-CF 1 A-9466 H H H H H 0 H H 4-C I,2-CF, 1 A-9467 H H H H H 0 H H 4-01 ,3-F 3 1 A-9468 H H H H H 0 H H 2-C 1,3-D M e 1 A-9469 H H H H H 0 H H 2-C 4- M e 1 A-9470 H H H H H 0 H H 2-C 1,5-D M e 1 A-9471 H H H H H 0 H H 2-C 1,6-0M e 1 A-9472 H H H H H 0 H H 3-C 1,2-0 M e 1 A-9473 H H H H H 0 H H 3-C 4- M e 1 A-9474 H H H H H 0 H H 3-C 1,5-D M e 1 A-9475 H H H H H 0 H H 3-C 1,6-0M e 1 A-9476 H H H H H 0 H H 4-C 1,2-0 M e 1 A-9477 H H H H H 0 H H 4-C 1,3-D M e 1 A-9478 H H H H H 0 H H 2,3-M e 2 T A-9479 H H H H H 0 H H 2,4-M e2 A-9480 H H H H H 0 H H 2,5-M e 2 T A-9481 H H H H H 0 H H 2,6-M e 2 T A-9482 H H H H H 0 H H 3,4-M e2 T A-9483 H H H0 H H H H 3,5-M e2 A-9484 H H H0 H H H H 2-M e,3-% T A-9485 H H H0 H H H H 2-Ae,4-C 1 A-9486 H H H0 H H H H 2- e,5-CF T A-9487 H H H0 H H H H 2-M e,6-C 1 A-9488 H H H0 H H H H 3-M e,2-C T A-9489 H H H0 H H H H 3-M e,4-C% 1 A-9490 H H H0 H H H H 3-M e,5-CF3 1 A-9491 H H H0 H H H H 3-M e,6-G0 T A-9492 H H H0 H H H H 4-M e,2-C T A-9493 H H H H H 0 H H 4-M e,3-% T A-9494 H H H H H 0 H H 2-M e,3-0 M e A-9495 H H H H H 0 H H 2-M e,4-0 M e 1 A-9496 H H H H H 0 H H 2-M e,5-0 M e 1 A-9497 H H H H H 0 H H 2-M e,6-0 M e 1 A-9498 H H H H H 0 H H 3-M e,2-0 M e 1 A-9499 H H H H H 0 H H 3-M e,4-0 M e 1 A-9500 H H H H H 0 H H 3-M e,5-0 M e 1 A-9501 H H H H H 0 H H 3-M e,6-0M e 1 A-9502 H H H H H 0 H H 4-M e,2-0M e 1 A-9503 H H H H H 0 H H 4-M e,3-0M e 1 A-9504 H H H H H 0 H H 2,3-0M e 2 A-9505 H H H H H 0 H H 2,4-0M e2 A-9506 H H H H H 0 H H 2,5-0M e 2 A-9507 H H H H H 0 H H 2,6-0M e 2 A-9508 H H H H H 0 H H 3,4-0M e 2 A-9509 H H H H H 0 H H 3,5-0M 2 T2 A-9510 H H H H H 0 H H 2-0 Me,3- F 3 1 A-9511 H H H H H 0 H H 2-0 M e,4-CF3 1 A-9512 H H H H H 0 H H 2-0M e,5-CF3 1 A-9513 H H H H H 0 H H 2-OM e,6-F3 1 A-9514 H H H H H0 H H 3-OM e,2-CF3 1
[0293]
[Table 168]
com pound RI R2 R R R A R R' (R)m P A-9515 H H H H H 0 H H 3-0Me,4-CF 3 1 A-9516 H H H H H 0 H H 3-0Me,5-CF 3 1 A-9517 H H H H H 0 H H 3-OMe,6-CF3 1 A-9518 H H H H H 0 H H 4-0Me,2-F 3 1 A-9519 H H H H H 0 H H 4-0Me,3-CF 3 1 A-9520 H H H H H 0 H H 2-CHF 2,3-F 1 A-9521 H H H H H 0 H H 2-CHF 2,4-F 1 A-9522 H H H H H 0 H H 2-CHF 2,5-F 1 A-9523 H H H H H 0 H H 2-CHF 2,6-F 1 A-9524 H H H H H 0 H H 2-CHF 2,3-Ae T A-9525 H H H H H 0 H H 2-CHF 2,4-Me T A-9526 H H H H H 0 H H 2-CHF 2,b-Me T A-9527 H H H H H 0 H H 2-CHF 2,6-Me T A-9528 H H H H H 0 H H 2-cycbpropyl,3-F 1 A-9529 H H H H H 0 H H 2-cycbpropyl,4-F 1 A-9530 H H H H H 0 H H 2-cycbpropyl,5-F 1 A-9531 H H H H H 0 H H 2-cycbpropy1,6-F 1 A-9532 H H H H H 0 H H 2-cycbpropyl,3-Me 1 A-9533 H H H H H 0 H H 2-cycbpropyl,4-Me 1 A-9534 H H H H H 0 H H 2-cycbpropyl,5-Me 1 A-9535 H H H H H 0 H H 2-cycbpropyl,6-Me 1 A-9536 H H H H H 0 H H 2-ethenyl,3-F 1 A-9537 H H H H H 0 H H 2-ethenyl,4-F 1 A-9538 H H H H H 0 H H 2-etheny1,5-F 1 A-9539 H H H H H 0 H H 2-ethenyl,6-F 1 A-9540 H H H H H 0 H H 2-ethenyl,3-Me 1 A-9541 H H H H H 0 H H 2-ethenyl,4-M e 1 A-9542 H H H H H 0 H H 2-ethenyl,5-Me 1 A-9543 H H H H H 0 H H 2-ethenyl,6-Me 1 A-9544 H H H H H 0 H H 2-0Et,3-F 1 A-9545 H H H H H 0 H H 2-0Et,4-F 1 A-9546 H H H H H 0 H H 2-0Et,5-F 1 A-9547 H H H H H 0 H H 2-0Et,6-F 1 A-9548 H H H H H 0 H H 2-0Et3-CI 1 A-9549 H H H H H 0 H H 2-0Et4-CI 1 A-9550 H H H H H 0 H H 2-0Et5-CI 1 A-9551 H H H H H 0 H H 2-0Et6-CI 1 A-9552 H H H H H 0 H H 2-OEt,3-Me 1 A-9553 H H H H H 0 H H 2-0Et,4-Me 1 A-9554 H H H H H 0 H H 2-0Et,5-M e 1 A-9555 H H H H H 0 H H 2-0Et,6-Me 1 A-9556 H H H H H 0 H H 2-0Pr,3-F 1 A-9557 H H H H H 0 H H 2-0Pr,4-F 1 A-9558 H H H H H 0 H H 2-0Pr,5-F 1 A-9559 H H H H H 0 H H 2-0Pr,6-F 1 A-9560 H H H H H 0 H H 2-OPr,3-Me 1 A-9561 H H H H H 0 H H 2-OPr,4-Me 1 A-9562 H H H H H 0 H H 2-OPr,5-Me 1 A-9563 H H H H H 0 H H 2-OPr,6-Me 1 A-9564 H H H H H 0 H H 2-0 (/-Pr),3-F 1 A-9565 H H H H H 0 H H 2-0 (/-Pr),4-F 1 A-9566 H H H H H 0 H H 2-0 (/-Pr),5-F 1 A-9567 H H H H H 0 H H 2-0 (/-Pr),6-F 1 A-9568 H H H H H 0 H H 2-0 (/-Pr),3-M e 1 A-9569 H H H H H 0 H H 2-0 (/-Pr),4-M e 1 A-9570 H H H H H 0 H H 2-0 (/-Pr),5-Me 1 A-9571 H HffH H 0 H H 2-0 (/-Pr),6-Me T
[0294]
[Table 169]
com pound RI R2 R R R A R R' (R)m P A-9572 i H H H H H 0 H H 2-0CF,,3-F 1 A -9573 H H H H H 0 H H 2-0 CF,,4-F T A-9574 H H H H H 0 H H 2-0C F,5-F T A-9575 H H H H H 0 H H 2-00F,64F T A-9576 H H H H H 0 H H 2-0CF3 ,3-Me T A-9577 H H H H H 0 H H 2-0CF3 ,4-Me 1 A-9578 H H H H H 0 H H 2-0CF3 ,5-Me 1 A-9579 H H H H H 0 H H 2-0CF3 ,6-Me 1 A-9580 H H H H H 0 H H 2-0CHF 2,3-F 1 A-9581 H H H H H 0 H H 2-0CHF 2,4-F A-9582 H H H H H 0 H H 2-0CHF 2,b- T A-9583 H H H H H 0 H H 2-0CHF 2,6-4 A-9584 H H H H H 0 H H 2-0CHF 2 ,3-Me T A-9585 H H H H H 0 H H 2-0CHF 2 ,4-Me 1 A-9586 H H H H H 0 H H 2-0CHF 2 ,5-Me 1 A-9587 H H H H H 0 H H 2-0CHF 2 ,6-Me T A-9588 H H H H H 0 H H 2-(cycbpropy bxy),3-F 1 A-9589 H H H H H 0 H H 2-(cycbpropybxy),4-F 1 A-9590 H H H H H 0 H H 2-(cycbpropy bxy),5-F 1 A-9591 H H H H H 0 H H 2-(cycbpropybxy),6-F 1 A-9592 H H H H H 0 H H 2-(cyclopropybxy),3-M e 1 A-9593 H H H H H 0 H H 2-(cyclopropybxy),4-M e 1 A-9594 H H H H H 0 H H 2-(cyclopropybxy),5-Me 1 A-9595 H H H H H 0 H H 2-(cyclopropybxy),6-M e 1 A-9596 H H H H H 0 H H 2-(oxiran-2-yD,3-F 1 A-9597 H H H H H 0 H H 2-(oxiran-2-yD,4-F 1 A-9598 H H H H H 0 H H 2-(oxiran-2-yD,5-F 1 A-9599 H H H H H 0 H H 2-(oxiran-2-yD,6-F 1 A-9600 H H H H H 0 H H 2-(oxiran-2-yD,3-Me 1 A-9601 H H H H H 0 H H 2-(oxiran-2-yD,4-Me 1 A-9602 H H H H H 0 H H 2-(oxiran-2-yD,5-Me 1 A-9603 H H H H H 0 H H 2-(oxiran-2-yD,6-Me 1 A-9604 H H H H H 0 H H 2-(oxiran-2-yh ethyD,3-F 1 A-9605 H H H H H 0 H H 2-(oxiran-2-y hethyD,4-F 1 A-9606 H H H H H 0 H H 2-(oxiran-2-yh ethyD,5-F 1 A-9607 H H H H H 0 H H 2-(oxiran-2-yh ethyD,6-F 1 A-9608 H H H H H 0 H H 2-(oxiran-2-yhiethyl),3-M e 1 A-9609 H H H H H 0 H H 2-(oxiran-2-y hethy),4-Me 1 A-9610 H H H H H 0 H H 2-(oxiran-2-y hethyl),5-Me 1 A-9611 H H H H H 0 H H 2-(oxiran-2-y hethyl),6-Me 1 A-9612 H H H H H 0 H H 2-SM e,3-F 1 A-9613 H H H H H 0 H H 2-SM e,4-F 1 A-9614 H H H H H 0 H H 2-SM e,5-F 1 A-9615 H H H H H 0 H H 2-SM e,6-F 1 A-9616 H H H H H 0 H H 2-SMe,3-M e 1 A-9617 H H H H H 0 H H 2-SMe,4-M e 1 A-9618 H H H H H 0 H H 2-SMe,5-Me 1 A-9619 H H H H H 0 H H 2-SMe,6-M e 1 A-9620 H H H H H 0 H H 2-SEt,3-F 1 A-9621 H H H H H 0 H H 2-SEt,4-F 1 A-9622 H H H H H 0 H H 2-SEt,5-F 1 A-9623 H H H H H 0 H H 2-SEt,6-F 1 A-9624 H H H H H 0 H H 2-SEt,3-M e 1 A-9625 H H H H H 0 H H 2-SEt,4-M e 1 A-9626 H H H H H 0 H H 2-SEt,5-M e 1 A-9627 H H H H H 0 H H 2-SEt,6-M e 1 A-9628 H H H H 0 H H 2-S(=0)Me,3-F 1
[0295]
[Table 170]
com pound RI R2 R R R A R R' (R)m P A-9629 i H H H H H 0 H H 2-S(=0)Me,4-F 1 A-9630 H H H H H 0 H H 2-S(=0)Me,5-F 1 A-9631 H H H H H 0 H H 2-S(=0)Me,6-F 1 A-9632 H H H H H 0 H H 3-S(=0)Me,2-F 1 A-9633 H H H H H 0 H H 3-S(=0)Me,4-F 1 A-9634 H H H H H 0 H H 3-S(=0)Me,5-F 1 A-9635 H H H H H 0 H H 3-S(=0)Me,6-F 1 A-9636 H H H H H 0 H H 2-S(=0)Me,3-M e 1 A-9637 H H H H H 0 H H 2-S(=0)Me,4-M e 1 A-9638 H H H H H 0 H H 2-S(=0)Me,5-M e 1 A-9639 H H H H H 0 H H 2-S(=0)Me,6-M e 1 A-9640 H H H H H 0 H H 3-S(=0)Me,2-M e 1 A-9641 H H H H H 0 H H 3-S(=0)Me,4-M e 1 A-9642 H H H H H 0 H H 3-S(=0)Me,5-M e 1 A-9643 H H H H H 0 H H 3-S(=0)Me,6-M e 1 A-9644 H H H H H 0 H H 2-S(=0) 2Me,3-F 1 A-9645 H H H H H 0 H H 2-S(=0) 2Me,4-F 1 A-9646 H H H H H 0 H H 2-S(=0) 2Me,5-F 1 A-9647 H H H H H 0 H H 2-S(=0) 2Me,6-F 1 A-9648 H H H H H 0 H H 2-S(=0) 2 Me,3-M e 1 A-9649 H H H H H 0 H H 2-S(=0) 2 Me,4-M e 1 A-9650 H H H H H 0 H H 2-S(=0) 2 Me,5-M e 1 A-9651 H H H H H 0 H H 2-S(=0) 2 Me,6--M e 1 A-9652 H H H H H 0 H H 2-SCF,,3-F 1 A-9653 H H H H H 0 H H 2-SCF 3 ,4-F T A-9654 H H H H H 0 H H 2-SCF 3 ,b-F T A-9655 H H H H H 0 H H 2-SCF 3 ,6-F T A-9656 H H H H H 0 H H 2-SCF 3 ,3-M e 1 A-9657 H H H H H 0 H H 2-SCF 3 ,4-M e 1 A-9658 H H H H H 0 H H 2-SCF 3 ,5-M e 1 A-9659 H H H H H 0 H H 2-SCF 3 ,6-M e 1 A-9660 H H H H H 0 H H 2-S (=0)CF 3 ,3-F 1 A-9661 H H H H H 0 H H 2-S (=0)CF 3 ,4-F 1 A-9662 H H H H H 0 H H 2-S (=O)F 3 ,b-F 1 A-9663 H H H H H 0 H H 2-S (=0)CF 3 ,6-F 1 A-9664 H H H H H 0 H H 2-S(=O)CF 3 ,3-M e 1 A-9665 H H H H H 0 H H 2-S(=O)CF 3 ,4-M e 1 A-9666 H H H H H 0 H H 2-S(=O)CF 3 ,5-M e 1 A-9667 H H H H H 0 H H 2-S(=O)CF 3 ,6-Me 1 A-9668 H H H H H 0 H H 2-S(=0) 2CF3 ,3-F 1 A-9669 H H H H H 0 H H 2-S(=0) 2CF3 ,4-F 1 A-9670 H H H H H 0 H H 2-S(=0) 2CF3 ,5-F T A-9671 H H H H H 0 H H 2-S(=0) 20F 3 ,6-F T A-9672 H H H H H 0 H H 2-S(=0) 2CF 3 ,3-M e 1 A-9673 H H H H H 0 H H 2-S (=0) 2CF 3,4-M e 1 A-9674 H H H H H 0 H H 2-S(=0) 2CF 3 ,b-M e 1 A-9675 H H H H H 0 H H 2-S(=0) 2 CF 3 ,6-M e 1 A-9676 H H H H H 0 H H 2-(cycobpropylthb),3-F 1 A-9677 H H H H H 0 H H 2-(cycobpropylthb),4-F 1 A-9678 H H H H H 0 H H 2-(cycobpropylthb),5-F 1 A-9679 H H H H H 0 H H 2-(cycobpropylthb),6-F 1 A-9680 H H H H H 0 H H 2-(cycbpropylthb),3-M e 1 A-9681 H H H H H 0 H H 2-(cycbpropylthb),4-M e 1 A-9682 H H H H H 0 H H 2-(cycbpropylthb),5-Me 1 A-9683 H H H H H 0 H H 2-(cycbpropylthb),6-M e 1 A-9684 H H H H H 0 H H 2-C (=0)M e,3-F 1 A-9685 H H H H 0 H H 2-C (= 0)Me,4-F 1
[0296]
[Table 171]
com pound RI R2 R R R A R R' (R)m P A-9686 H H H H H 0 H H 2-C (=0)M e,5-F 1 A-9687 H H H H H 0 H H 2-C (=0)M e,6-F 1 A-9688 H H H H H 0 H H 2-C(=0)Me,3-M e 1 A-9689 H H H H H 0 H H 2-C(=0)Me,4-M e T A-9690 H H H H H 0 H H 2-C(=0)Me,5-M e T A-9691 H H H H H 0 H H 2-C(=0)Me,6--M e 1 A-9692 H H H H H 0 H H 3-C (=0)M e,2-F 1 A-9693 H H H H H 0 H H 3-C (=0)M e,4-F 1 A-9694 H H H H H 0 H H 3-C (=0)M e,5-F 1 A-9695 H H H H H 0 H H 3-C (=0)M e,6-F 1 A-9696 H H H H H 0 H H 3-C(=0)Me,2-M e 1 A-9697 H H H H H 0 H H 3-C(=0)Me,4-M e 1 A-9698 H H H H H 0 H H 3-C(=0)Me,5-M e 1 A-9699 H H H H H 0 H H 3-C(=0)Me,6--M e 1 A-9700 H H H H H 0 H H 2-C(=0)0Me,3-F 1 A-9701 H H H H H 0 H H 2-C(=0)0Me,4-F 1 A-9702 H H H H H 0 H H 2-C(=0)0Me,5-F 1 A-9703 H H H H H 0 H H 2-C(=0)0Me,6-F 1 A -9704 H H H H H 0 H H 2-C (=0)0 M e,3-M Ae 1 A -9705 H H H H H 0 H H 2-C (=0)0 M e,4-M e 1 A-9706 H H H H H 0 H H 2-C(=0)0Me,5-MvAe T A-9707 H H H H H 0 H H 2-C(=0)0Me,6-MA e 1 A-9708 H H H H H 0 H H 2-C(=0)0Et,3-F 1 A-9709 H H H H H 0 H H 2-C(=0)0Et,4-F 1 A-9710 H H H H H 0 H H 2-C(=0)0Et,5-F 1 A-9711 H H H H H 0 H H 2-C(=0)0Et,6-F 1 A-9712 H H H H H 0 H H 2-C(=0)0Et3-M e 1 A-9713 H H H H H 0 H H 2-C(=0)0Et4-M e 1 A-9714 H H H H H 0 H H 2-C(=0)0Et5-M e 1 A-9715 H H H H H 0 H H 2-C(=0)0Et6-M e 1 A-9716 H H H H H 0 H H 2-C(=0)NH 2,3-F 1 A-9717 H H H H H 0 H H 2-C(=0)NH 2,4-F 1 A-9718 H H H H H 0 H H 2-C(=0)NH 2,5-F 1 A-9719 H H H H H 0 H H 2-C(=0)NH 2,6- 1 A-9720 H H H H H 0 H H 2-C(=0)NH 2 ,3-M e 1 A-9721 H H H H H 0 H H 2-C(=0)NH 2 ,4-M e 1 A-9722 H H H H H 0 H H 2-C(=0)NH 2 ,b-M e 1 A-9723 H H H H H 0 H H 2-C(=0)NH 2 ,6-M e 1 A-9724 H H H H H 0 H H 2-C(=0)NHMe,3-F 1 A-9725 H H H H H 0 H H 2-C(=0)NHMe,4-F 1 A-9726 H H H H H 0 H H 2-C(=0)NHMe,5-F 1 A-9727 H H H H H 0 H H 2-C(=0)NHMe,6-F 1 A-9728 H H H H H 0 H H 2-C(=0)NHMe,3-M e 1 A-9729 H H H H H 0 H H 2-C(=0)NHMe,4-M e 1 A-9730 H H H H H 0 H H 2-C(=0)NHMe,5-M e 1 A-9731 H H H H H 0 H H 2-C(=0)NHMe,6-M e 1 A-9732 H H H H H 0 H H 2-C(=0)NMe 2 ,3-F 1 A-9733 H H H H H 0 H H 2-C(=0)NMe 2 ,4-F 1 A-9734 H H H H H 0 H H 2-C(=0)NMe 2 ,5-F 1 A-9735 H H H H H 0 H H 2-C(=O)NMe 2 ,6- 1 A-9736 H H H H H 0 H H 2-C(=0)NMe 2,3-M e 1 A-9737 H H H H H 0 H H 2-C(=0)NMe 2,4-M e 1 A-9738 H H H H H 0 H H 2-C(=0)NMe 2,b-M e 1 A-9739 H H H H H 0 H H 2-C(=0)NMe 2,6-M e 1 A-9740 H H H H H 0 H H 2-CH 20H,3-F 1 A-9741 H H H H H 0 H H 2-CH 20H,4-F 1 A-9742 IH IH IH H H 0 H H 2-CH 20H,5-F T
[0297]
[Table 172]
com pound R' R2 R R A R R' (R)m p A-9743 i H H H H 0 H H 2-GH2UH,6-FT A-9744 H H H H 0 H H 2-CH 20H,3-- e A-9745 H H H H 0 H H 2-CH 20H,4-v e A-9746 H H H H i 0 H H 2-CH 2UH,b-M e A-9747 H H H H 0 H H 2-0H 20H,6-6- e A-9748 H H H H 0 H H 2-UH 20H 3 ,3-FT A-9749 H H H H 0 H H 2-UH 20H 3 ,4-F A-9750 H H H H 0 H H 2-GH 20H 3 ,b-FT A-9751 H H H H H 0 H H 2-UH 20H 3 ,6-F1 A-9752 H H H H 0 H H 2-CH 2UCH 3 ,3-M e A-9753 H H H H i 0 H H 2-CH 2UCH 3 ,4-M e A-9754 H H H H 0 H H 2-CH 2 CH 3 ,b- e T A-9755 H H H H 0 H H 2-CH 2 CH 3 6- e A-9756 H H H H 0 H H 2-UH 20H 2 CH 3 ,3-FT A-9757 H H H H 0 H H 2-UH 20H 2 CH 3 ,4-F A-9758 H H H H f0 H H 2-GH 20H 2 CH 3 ,b-H A-9759 H H H H HD0 H H 2-GH 20H 2 CH 3 ,- T A-9760 H H H H 0 H H 2-UH 20H 2 CH 3,3-Me A-9761 H H H H f0 H H 2-H 20H 2CH 3,4-Me A-9762 H H H H 0 H H 2-UH 20H 2CH 3 ,b-Me 1 A-9763 H H H H f0 H H 2-GH 20H 2 CH 3 ,6-Me T A-9764 H H H H H0 H H 2-00C= U)CH 3 ,3-F 1 A-9765 H H H H 0 H H 2-0C0(= )CH 3 ,4-F T A-9766 H H H H H0 H H 2-00C=)= H 3 ,b-F A-9767 H H H H EH H H 2- C(= U)GH 3 ,6-FT A-9768 H H H H f0 H H 2-0(=U)CH 3,3-M e A-9769 H H H H f0 H H 2-00(=U)CH 3 ,4-M e A-9770 H H H H i 0 H H 2-00 = U)CH 3 ,b-M e 1 A-9771 H H H H 0 H H 2-00(=0)CH 3 ,6-Me T A-9772 H H H H 0 H H 2-OS =0 ) 2 GH 3 ,3-F T A-9773 H H H H D0 H H 2-OS =0 )2H3,4-F A-9774 H H H H 0 H H 2-OS =0 ) 2 GH 3 ,b-F T A-9775 H H H H HD0 H H 2-OS =0 ) 2 H 3 ,6-F 1 A-9776 H H H H f0 H H 2-OS =O ) 2 CH 3,3-M e A-9777 H H H H 0 H H 2-OS(= 0) 2 H 3,4-MeT A-9778 H H H H 0 H H 2-OS =O ) 2 CH 3,b-M e A-979 H H H H f0 H H 2-OS = ) 2 CH 3,6-MeT A-9780 H H H H 0 H H 2-UH 2 SH,3-FT A-9781 H H H H 0 H H 2-UH 2 SOH 3 ,4-F A-9782 H H H H H 0 H H 2-UH 2 SOH 3 ,b-F A-9783 H H H H 0 H H 2-UH 2 SOH 3 ,6-F A-9784 H H H H 0 H H 2-UH 2S0H 3,3-M e A-9785 H H H H f0 H H 2-CH 2SCH 3,4-e T A-9786 H H H H 0 H H 2-CH 2SCH 3,b-M e A-9/87 H H H H 0 H H 2-CH 2 SCH 3 6-M eT A-9788 H H H H H 0 H H 2-CH 2 SCF 3,3-T A-9789 H H H H 0Di H H 2-OH2SOF 3 ,4-F A-9790 H H H H 0 H H 2-UH 2SOF 3 ,b-F A-9791 H H H H 0 H H 2-UH 2SOF 3 ,6-F A-9792 H H H H f0 H H Z-GH 2SCF 3 ,3-M e A-9793 H H H H 0 H H 2-UH 2S0F 3 ,4-M e A-9794 H H H H f0 H H 2-CH 2SCF 3 ,b-M e A-9795 H H H H f0 H H 2-CH 2SCF 3 ,6-M e A-9796 H H H H 0 H H 2-(benzy bxy),3-F T A-9797 H H H H f0 H H 2-(benzy bxy),4-F T A-9798 H H H H f0 H H 2-(benzy bxy),b-F T A-9799 IH IHII H H 0 H H 2-(benzybxy),6-F T
[0298]
[Table 173]
com pound RI R2 R R R A R R' (R)m P A-9800 H H H H H 0 H H 2-(benzyloxy),3-Me 1 A-9801 H H H H H 0 H H 2-(benzyloxy),4-M e 1 A-9802 H H H H H 0 H H 2-(benzyloxy),5-Me 1 A-9803 H H H H H 0 H H 2-(benzyloxy),6-M e 1 A-9804 H H H H H 0 H H 2-NH 2,3-F T A-9805 H H H H H 0 H H 2-NH 2,4-F 1 A-9806 H H H H H 0 H H 2-NH 2,5-F 1 A-9807 H H H H H 0 H H 2-NH 2,6-F 1 A-9808 H H H H H 0 H H 2-NH 2,3-Me 1 A-9809 H H H H H 0 H H 2-NH 2,4-Me T A-9810 H H H H H 0 H H 2-NH 2,5-Me T A-9811 H H H H H 0 H H 2-NH 2 ,6-Me T A-9812 H H H H H 0 H H 2-NHMe,3-F 1 A-9813 H H H H H 0 H H 2-NHMe,4-F 1 A-9814 H H H H H 0 H H 2-NHMe,5-F 1 A-9815 H H H H H 0 H H 2-NHMe,6-F 1 A-9816 H H H H H 0 H H 2-NHMe,3-M e 1 A-9817 H H H H H 0 H H 2-NHMe,4-M e 1 A-9818 H H H H H 0 H H 2-NHMe,5-M e 1 A-9819 H H H H H 0 H H 2-NHMe,6-MA e 1 A-9820 H H H H H 0 H H 2-NHEt,3-F 1 A-9821 H H H H H 0 H H 2-NHEt,4-F 1 A-9822 H H H H H 0 H H 2-NHEt,5-F 1 A-9823 H H H H H 0 H H 2-NHEt,6-F 1 A-9824 H H H H H 0 H H 2-NHEt,3-M e 1 A-9825 H H H H H 0 H H 2-NHEt,4-Me 1 A-9826 H H H H H 0 H H 2-NHEt,5-M e 1 A-9827 H H H H H 0 H H 2-NHEt,6-M e 1 A-9828 H H H H H 0 H H 2-NMe 2 ,3-F 1 A-9829 H H H H H 0 H H 2-NMe 2 ,4-F 1 A-9830 H H H H H 0 H H 2-NMe 2 ,5-F 1 A-9831 H H H H H 0 H H 2-NMe 2 ,6-F 1 A-9832 H H H H H 0 H H 2-NMe 2 ,3-Me 1 A-9833 H H H H H 0 H H 2-NMe 2 ,4-Me T A-9834 H H H H H 0 H H 2-NMe 2 ,5-Me T A-9835 H H H H H 0 H H 2-NMe 2 ,6-Me T A-9836 H H H H H 0 H H 2-NEt 2,3-F T A-9837 H H H H H 0 H H 2-NE½,4-F 1 A-9838 H H H H H 0 H H 2-NEt2 ,5-F 1 A-9839 H H H H H 0 H H 2-NEt2 ,6-F 1 A-9840 H H H H H 0 H H 2-NEt2,3-Me 1 A-9841 H H H H H 0 H H 2-NEt2,4-Me 1 A-9842 H H H H H 0 H H 2-NEt2,5-Me 1 A-9843 H H H H H 0 H H 2-NEt2,6-Me 1 A-9844 H H H H H 0 H H 2-CHO,3-F 1 A-9845 H H H H H 0 H H 2-CHO,4-F 1 A-9846 H H H H H 0 H H 2-CH0,5-F 1 A-9847 H H H H H 0 H H 2-CHO,6-F 1 A-9848 H H H H H 0 H H 2-CHO,3-M e 1 A-9849 H H H H H 0 H H 2-CHO,4-MAe 1 A-9850 H H H H H 0 H H 2-CHO,5-M e 1 A-9851 H H H H H 0 H H 2-CHO,6-M e 1 A-9852 H H H H H 0 H H 2-C (=0)OH,3-F 1 A-9853 H H H H H 0 H H 2-C (=0)OH,4-F 1 A-9854 H H H H H 0 H H 2-C (=0)OH,5-F 1 A-9855 H H H H H 0 H H 2-C(=0)OH,6-F 1 A-9856 H F FH IH 0 H H 2-C(=0)0H,3-Me T
[0299]
[Table 174]
com pound RI R2 R R R A R R' (R)m P A-9857 i H H H H H 0 H H 2-C(=0)0H,4e-M 1 A-9858 H H H H H 0 H H 2-C(=0)0H,b5-M e 1 A-9859 H H H H H 0 H H 2-C(=0)0H,6-M e 1 A-9860 H H H H H 0 H H 2-(1,3-dioxolan-2-yD,3-F 1 A-9861 H H H H H 0 H H 2-(1,3-dioxolan-2-yD,4-F 1 A-9862 H H H H H 0 H H 2-0,3-dioxolan-2-yD,5-F 1 A-9863 H H H H H 0 H H 2-0,3-dioxolan-2-yD,6-F 1 A-9864 H H H H H 0 H H 2-(1,3-dioxolan-2-yD,3-M e 1 A-9865 H H H H H 0 H H 2-(1,3-dioxolan-2-yD,4-M e 1 A-9866 H H H H H 0 H H 2-(1,3-dioxolan-2-yD,5-M e 1 A-9867 H H H H H 0 H H 2-(1,3-dioxolan-2-yD,6-M e 1 A-9868 H H H H H 0 H H 2-0,3-dioxan-2-yD,3-F 1 A-9869 H H H H H 0 H H 2-0,3-dioxan-2-yD,4-F 1 A-9870 H H H H H 0 H H 2-0,3-dioxan-2-yD,5-F 1 A-9871 H H H H H 0 H H 2-0,3-dioxan-2-yD,6-F 1 A-9872 H H H H H 0 H H 2-(1,3-dioxan-2-yD,3-Me 1 A-9873 H H H H H 0 H H 2-(1,3-dioxan-2-yD,4-M e 1 A-9874 H H H H H 0 H H 2-(1,3-dioxan-2-yD,5-Me 1 A-9875 H H H H H 0 H H 2-(1,3-dioxan-2-yD,6-M e 1 A-9876 H H H H H 0 H H 2-(thiazol-2-y),3-F 1 A-9877 H H H H H 0 H H 2-(thiazol-2-y),4-F 1 A-9878 H H H H H 0 H H 2-(thiazol-2-y1),5-F 1 A-9879 H H H H H 0 H H 2-(thiazol-2-y),6-F 1 A-9880 H H H H H 0 H H 2-(thbzol-2-yD,3-Me 1 A-9881 H H H H H 0 H H 2-(thbzol-2-yD,4-Me 1 A-9882 H H H H H 0 H H 2-(thbzol-2-yD,5-Me 1 A-9883 H H H H H 0 H H 2-(thbzol-2-yD,6-M e 1 A-9884 H H H H H 0 H H 2-(oxazo[-2-yD,3-F 1 A-9885 H H H H H 0 H H 2-(oxazo[-2-yD,4-F 1 A-9886 H H H H H 0 H H 2-(oxazol-2-yD,5-F 1 A-9887 H H H H H 0 H H 2-(oxazol-2-yD,6-F 1 A-9888 H H H H H 0 H H 2-(oxazol-2-yD,3-M e 1 A-9889 H H H H H 0 H H 2-(oxazol-2-yD,4-Me 1 A-9890 H H H H H 0 H H 2-(oxazol-2-yD,5-M e 1 A-9891 H H H H H 0 H H 2-(oxazol-2-yD,6-M e 1 A-9892 H H H H H 0 H H 2-CH= N0H ,3-F 1 A-9893 H H H H H 0 H H 2-CH= N0H ,4-F 1 A-9894 H H H H H 0 H H 2-CH= N0H ,5-F 1 A-9895 H H H H H 0 H H 2-CH= N0H ,6-F 1 A-9896 H H H H H 0 H H 2-CH=N0H,3-M e 1 A-9897 H H H H H 0 H H 2-CH=N0H,4-M e 1 A-9898 H H H H H 0 H H 2-CH=N0H,5-M e 1 A-9899 H H H H H 0 H H 2-CH=N0H,6-M e 1 A-9900 H H H H H 0 H H 2-CH= N0M e,3-F 1 A-9901 H H H H H 0 H H 2-CH= N0M e,4-F 1 A-9902 H H H H H 0 H H 2-CH= N0M e,5-F 1 A-9903 H H H H H 0 H H 2-CH= N0M e,6-F 1 A-9904 H H H H H 0 H H 2-CH=N0Me,3-M e 1 A-9905 H H H H H 0 H H 2-CH=N0Me,4-M e 1 A-9906 H H H H H 0 H H 2-CH=N0Me,5-M e 1 A-9907 H H H H H 0 H H 2-CH=N0Me,6-M e 1 A-9908 H H H H H 0 H H 2-CN,3-F 1 A-9909 H H H H H 0 H H 2-CNA-F 1 A-9910 H H H H H 0 H H 2-CN,5-F 1 A-9911 H H H H H 0 H H 2-CN,6-F 1 A-9912 H H H H H 0 H H 2-CN,3-CI 1 A-9913 HH H H H 0 H H 2-CN,4-CI 1
[0300]
[Table 175]
com pound RI R2 R R R A R R' (R)m P A-9914 H H H H H 0 H H 2-CN,5-C I 1 A-9915 H H H H H 0 H H 2-CN,6-C I 1 A-9916 H H H H H 0 H H 2-CN,3-M e 1 A-9917 H H H H H 0 H H 2-CN A- e 1 A-9918 H H H H H 0 H H 2-CN,5-M e 1 A-9919 H H H H H 0 H H 2-CN,6-M e 1 A-9920 H H H H H 0 H H 2-CN,3-0M e 1 A-9921 H H H H H 0 H H 2-CN,4-0M e 1 A-9922 H H H H H 0 H H 2-CN,5-0M e 1 A-9923 H H H H H 0 H H 2-CN,6-0M e 1 A-9924 H H H H H 0 H H 3-CN,2-F 1 A-9925 H H H H H 0 H H 3-CNA-F 1 A-9926 H H H H H 0 H H 3-CN,5-F 1 A-9927 H H H H H 0 H H 3-CN,6-F 1 A-9928 H H H H H 0 H H 3-CN,2-C I 1 A-9929 H H H H H 0 H H 3-CN 4-CI1 1 A-9930 H H H H H 0 H H 3-CN,5-C I 1 A-9931 H H H H H 0 H H 3-CN,6-C I 1 A-9932 H H H H H 0 H H 3-CN,2-M e 1 A-9933 H H H H H 0 H H 3-CN A- e 1 A-9934 H H H H H 0 H H 3-CN,5-M e 1 A-9935 H H H H H 0 H H 3-CN,6-M e 1 A-9936 H H H H H 0 H H 3-CN,2-0M e 1 A-9937 H H H H H 0 H H 3-CN,4-0M e 1 A-9938 H H H H H 0 H H 3-CN,5-0M e 1 A-9939 H H H H H 0 H H 3-CN,6-0M e 1 A-9940 H H H H H 0 H H 4-CN,2-F 1 A-9941 H H H H H 0 H H 4-CN,3-F 1 A-9942 H H H H H 0 H H 4-CN,2-C I 1 A-9943 H H H H H 0 H H 4-CN,3-C I 1 A-9944 H H H H H 0 H H 4-CN,2-M e 1 A-9945 H H H H H 0 H H 4-CN ,3- e 1 A-9946 H H H H H 0 H H 4-CN,2-0M e 1 A-9947 H H H H H 0 H H 4-CN,3-0M e 1 A-9948 H H H H H 0 H H 2-N0 2 ,3-F 1 A-9949 H H H H H 0 H H 2-N0 2 ,4-F T A-9950 H H H H H 0 H H 2-N0 2 ,5-4 1 A-9951 H H H H H 0 H H 2-N0 2 ,6-F 1 A-9952 H H H H H 0 H H 2-A0 2,3-M e 1 A-9953 H H H H H 0 H H 2-A0 2 ,4-M e 1 A-9954 H H H H H 0 H H 2-A0 2,5-M e 1 A-9955 H H H H H 0 H H 2-N0 2,6-M e 1 A-9956 H H H H H 0 H H 2-M e,3,4- 2 T A-9957 H H H H H 0 H H 2-M e,3,b-F 2 T A-9958 H H H H H 0 H H 2-M e,3,6-F 2 T A-9959 H H H H H 0 H H 2-M e,4,b-F 2 T A-9960 H H H H H 0 H H 2-0M e,34-F 2 A-9961 H H H H H 0 H H 2-0M e,3,5-F 2 A-9962 H H H H H 0 H H 2-OM e,3,6-F2 A-9963 H H H H H 0 H H 2-0M e,4,b-+ 2 T A-9964 H H H H H 0 H H 2-(CH2 33-3 1 A-9965 H H H H H 0 H H 2-(CH 2 )4 -3 1 A-9966 H H H H H 0 H H 2-(0CH 2CH 2)-3 T A-9967 H H H H H 0 H H 2-(0CH 2CH 2CH2)-3 T A-9968 H H H H H 0 H H 2-(CH 2CH 20)-3 1 A-9969 FH H H H 0 H H 2-(CH 2CH 2CH 20)-3 T A-9970 H H H H H 0 H H 3-(CH2 33-4 T
[0301]
[Table 176] com pound R' R R R' R A R" (R)m p A-9971 H H H H 0 H H 3-(GH 2) 4 -4 1 A-9972 H H H H 0 H H 3-(0H 2CH 2-4 1 A-9973 H H H H 0 H H 3-(0H 2 CH 2CH2)-4 1
A-9974 H H H H 0 H H 3-(H 2CH 2 0)-4 T A-9975 H H H H i 0 H H 3-(GH 20 20 2U)-4 T A-9976 H H H H i 0 H H 2-(0H 20)-3 T A-9977 H H H H i 0 H H 3-(0H 20)-4 T A-9978 H H H f0 H H H 2-(0H 20H 2 0)-3 T A-9979 H H H H 0Di H H 3-(0H 2CH 20)-4 1 A-9980 H H H H 0 H H 2-(0GF 20)-3 T A-9981 H H H H H0 H H 3-(0GF 20)-4 T A-9982 H H H H 0 H H 2-M e,6-Et 1 A-9983 H H H H 0 H H 2-M e,4,5-F 2 T A-9984 H H H f0 H H H 2-cyclopropyl,6-OM e A-9985 H H H f0 H H H 2-M e,b-Et T A-9986 H H H H H H H 2,6-Et2 T A-9987 H H H H 0 H H 2-Et,6-F 1 A-9988 H H H H 0 H H 2-0H 20H 3 ,6-CI 1 A-9989 H H H H D if 0 H H 2-0H20H2CH3,6-CI 1 A-9990 H H H H 0 H H 2-CH 2 NMe 2 T A-9991 H H H H 0 H H 2-0H 20H 3 ,6-UMe 0 A-9992 H H H H f0 H H 2-0H 20H 3 ,6-UMe 1 A-9993 H H H H f0 pyridin-2-yh ethyl H 2-M e 0 A-9994 H H H H f0 pyridin-3-yh ethyl H 2-M e 0
[0302]
[Table 177]
R3 R2 A KR
1 5 (0), R R 4 cornpound R' Tz Rj R Rb A Rb R' 0 p B-0002 H H H H H 0 H H Br 0 B-0003 H H H H H 0 H H Br 0 B-0004 H H H H H 0 H H nahhln1y 0 B-0004 H H H H H 0 H H 2 naphtha len-1-y1 0 B-0006 H H H H H 0 H H 2-M -naphtha ln-1-y1 0 B-0006 H H H H H 0 H H 2-Me3-naphtha len-1-yI1 0 B-0008 H H H H H 0 H H 2-0CM -naphthalen- -y1 0 B-0009 H H H H H 0 H H 2O naphthaen--yI 0 B-0010 H H H H H 0 H H I Fnaphthaen-2-y1 0 B-00101 H H H H H 0 H H I -F-naphtha en-2-y1 0 B-00112 H H H H H 0 H H 1 -tF3-naphtha Ien-2-yI1 0 B-00123 H H H H H 0 H H 1 -0CM -naphtha In-2-y1 0 B-00134 H H H H H 0 H H -M-naphthaen-2-yI 0 B-00145 H H H H H 0 H H 3-MF-naphtha en-2-y1 0 B-00156 H H H H H 0 H H 3-tF3-naphtha Ien-2-yI1 0 B-00167 H H H H H 0 H H 3-0CM -naphthaen-2-y1 0 B-001 8 H H H H H 0 H H 3-O ide-naptal2-yI 0 B-001 9 H H H H H 0 H H pyrii-2-y1 0 B-0020 H H H H H 0 H H 4-F-pyridi-2-yI1 0 B-0021 H H H H H 0 H H 5-F-pyrid i-2-yI1 0 -0021 H H H H H 0 H H 6-F-pyri i-2-yI1 0 B-0023 H H H H H 0 H H 3-C -pyrki in-2-yI1 0 B-0024 H H H H H 0 H H 43-C Ipyrid in-2-yI1 0 -0024 H H H H H 0 H H 5-C Ipyridin-2-yI1 0 B-0025 H H H H H 0 H H 6-C Ipyridin-2-yI1 0 B-0027 H H H H H 0 H H 3-MCbpyrid in-2-y1 0 B-0028 H H H H H 0 H H 4-M e-pyri i-2-yI1 0 B-0029 H H H H H 0 H H 5-M e-pyri -2-yI1 0 B-0029 H H H H H 0 H H 6-M e-pyridih,-2-yI1 0 -0030 H H H H H 0 H H 3-CFe-pyridi,-2-yI1 0 --0031 H H H H H 0 H H 4-CF 3 -Pyrid i-2-yI1 0 -0032 H H H H H 0 H H 4--CF 3 -pyrid i-2-yI1 0 --0033 H H H H H 0 H H 6-CF 3 -Pyrid i-2-y 1 0 -0034 H H H H H 0 H H 3-0CM -pyrid in-2-y 1 0 -0036 H H H H H 0 H H 4-0 Me-pyri i-2-yI1 0 B-0036 H H H H H 0 H H 5-OM e-pyid i-2-yI1 0 B-0038 H H H H H 0 H H 6-0 Me-pyrid i-2-yI1 0 - 0038 H H H H H 0 H H 6-O+e-Pyri i-2-yI1 0 B-0039 H H H H H 0 H H 3,4-F2 -Pyrid i-2-yI1 0 B-0040 H H H H H 0 H H 3,5-F 2-pyriin-2-yI1 0 -0041 H H H H H 0 H H 3,4-C 2 -pyrid i-2-yI1 0 -0042 H H H H H 0 H H 3,5-C 6-pyrid in-2-yI1 0 -0043 H H H H H 0 H H 3,6-GC6-pyrki -2-yI1 0 -0044 H H H H H 0 H H 3-F--C-p y r idin-2 -y1 0 -0 0456 H H H H H 0 H H 3-F-4-C pyrkiin-2-yI1 0 -0046 H H H H H 0 H H 3-F-6-C pyrkiin-2-yI1 0 -0048 H H H H H 0 H H 3-F-6-Ckepyrkidin-2-y1 0 -0048 H H H H H 0 H H 3-F-4-M e-pyrid in-2-yI1 0 -0049 H H H H H 0 H H 3-F-6-M e-pyrid in-2-yI1 0 - 0051 H H H H H 0 H H 3-F-4-OM e-pyrid in-2-yI1 0 -0052 H H H H H 0 H H 3-F-5-0 Me-pyridin-2-yI1 0
[0303]
[Table 178]
com pound R' R2 Rj R4 R A R6 R p B-0053 H H H H H 0 H H 3-F-6-0Me-pyridin-2-yI 0 B-0054 H H H H H 0 H H 3-CI-4-F-pyridin-2-y 0 B-0055 H H H H H 0 H H 3-CI-5-F-pyridin-2-y 0 B-0056 H H H H H 0 H H 3-CI-6-F-pyridin-2-y 0 B-0057 H H H H H 0 H H 3-CI-4-M e-pyridh-2-y 0 B-0058 H H H H H 0 H H 3-CI-5-Me-pyridh-2-y 0 B-0059 H H H H H 0 H H 3-CI-6-M e-pyridh-2-y 0 B-0060 H H H H H 0 H H 3-M e-4-F-pyridin-2-y 0 B-0061 H H H H H 0 H H 3-M e-5-F-pyridin-2-y 0 B-0062 H H H H H 0 H H 3-M e-6-F-pyridin-2-y 0 B-0063 H H H H H 0 H H 3-M e-4-Cl-pyridh-2-y 0 B-0064 H H H H H 0 H H 3-M e-5-Cl-pyridh-2-y 0 B-0065 H H H H H 0 H H 3-M e-6-Cl-pyridh-2-y 0 B-0066 H H H H H 0 H H 3,4-(M e) 2-pyrid in-2-y 1 0 B-0067 H H H H H 0 H H 3,5-(Me) 2-pyridin-2-yI 0 B-0068 H H H H H 0 H H 3,6-(Me) 2-pyridin-2-yI 0 B-0069 H H H H H 0 H H 3-Me-4-0Me-pyridin-2-y 0 B-0070 H H H H H 0 H H 3-Me-5-0Me-pyridin-2-y 0 B-0071 H H H H H 0 H H 3-Me-6-0Me-pyridin-2-y 0 B-0072 H H H H H 0 H H 3-GF 3 -4-F-pyridin-2-yl 0 B-0073 H H H H H 0 H H 3-CF 3 -5-F-pyridin-2-y 0 B-0074 H H H H H 0 H H 3-CF 3 -6-F-pyridin-2-y 0 B-0075 H H H H H 0 H H 3-CF 3 -4-Me-pyridin-2-y 0 B-0076 H H H H H 0 H H 3-GF 3-b-M e-pyrdin-2-y 0 B-0077 H H H H H 0 H H 3-CF 3 -6-Me-pyridin-2-y 0 B-0078 H H H H H 0 H H 3-0Me-4-F-pyridin-2-yI 0 B-0079 H H H H H 0 H H 3-0Me-5-F-pyridin-2-yI 0 B-0080 H H H H H 0 H H 3-0Me-6-F-pyridin-2-yI 0 B-0081 H H H H H 0 H H 3-0Me-4-Cl-pyridin-2-y 0 B-0082 H H H H H 0 H H 3-0Me-5-Cl-pyridin-2-y 0 B-0083 H H H H H 0 H H 3-0Me-6-Cl-pyridin-2-yI 0 B-0084 H H H H H 0 H H 3-0Me-4-MAe-pyridin-2-y 0 B-0085 H H H H H 0 H H 3-0Me-5-MAe-pyridin-2-y 0 B-0086 H H H H H 0 H H 3-0Me-6-MAe-pyridin-2-y 0 B-0087 H H H H H 0 H H 3,4-(0Me) 2 -pyridin-2-y 0 B-0088 H H H H H 0 H H 3,5-(0Me) 2 -pyridin-2-y 0 B-0089 H H H H H 0 H H 3,6-(0Me) 2 -pyridin-2-y 0 B-0090 H H H H H 0 H H pyridin-3-yI 0 B-0091 H H H H H 0 H H 2-F-pyridn-3-yI 0 B-0092 H H H H H 0 H H 4-F-pyridh-3-yI 0 B-0093 H H H H H 0 H H 5-F-pyridh-3-yI 0 B-0094 H H H H H 0 H H 6-F-pyridh-3-yI 0 B-0095 H H H H H 0 H H 2-Cl-pyridin-3-y 0 B-0096 H H H H H 0 H H 4-Cl-pyridin-3-y 0 B-0097 H H H H H 0 H H 5-Cl-pyridin-3-y 0 B-0098 H H H H H 0 H H 6-Cl-pyridin-3-y 0 B-0099 H H H H H 0 H H 2-M e-pyridin-3-yI 0 B-0100 H H H H H 0 H H 4-M e-pyridin-3-yI 0 B-0101 H H H H H 0 H H 5-M e-pyridin-3-yI 0 B-0102 H H H H H 0 H H 6-M e-pyridin-3-yI 0 B-0103 H H H H H 0 H H 2-CF 3 -pyridin-3-yI 0 B-0104 H H H H H 0 H H 4-CF 3 -pyridin-3-yI 0 B-0105 H H H H H 0 H H 5-CF3 -pyridin-3-yI 0 B-0106 H H H H H 0 H H 6-CF 3-pyridin-3-yI 0 B-0107 H H H H H 0 H H 2-0Me-pyridin-3-yI 0 B-0108 H H H H H 0 H H 4-0Me-pyridin-3-yI 0 B-0109 H H H H H 0 H H 5-0Me-pyridin-3-yI 0
[0304]
[Table 179]
com pound R' R2 Rj R4 R A R6 R p B-0110 H H H H H 0 H H 6-0Me-pyridin-3-y 0 B-0111 H H H H H 0 H H 2,4-F 2-pyridin-3-yl 0 B-0112 H H H H H 0 H H 2,b-F 2-pyrdin-3-yl 0 B-0113 H H H H H 0 H H 2,6-F 2-pyridin-3-yl 0 B-0114 H H H H H 0 H H 4,b-F 2-pyrdin-3-yl 0 B-0115 H H H H H 0 H H 4,6-F 2-pyrdin-3-yl 0 B-0116 H H H H H 0 H H 2,4-C -pyridin-3-y 0 B-0117 H H H H H 0 H H 2,b-C -pyridin-3-yl 0 B-0118 H H H H H 0 H H 2,6-C -pyridin-3-yl 0 B-0119 H H H H H 0 H H 4,5-C -pyridin-3-yl 0 B-0120 H H H H H 0 H H 4,6-C -pyridin-3-yl 0 B-0121 H H H H H 0 H H 2-F-4-Cl-pyridin-3-y 0 B-0122 H H H H H 0 H H 2-F-5-Cl-pyridin-3-y 0 B-0123 H H H H H 0 H H 2-F-6-Cl-pyridin-3-y 0 B-0124 H H H H H 0 H H 4-F-2-Cl-pyridin-3-y 0 B-0125 H H H H H 0 H H 4-F-5-Cl-pyridin-3-y 0 B-0126 H H H H H 0 H H 4-F-6-Cl-pyridin-3-y 0 B-0127 H H H H H 0 H H 2-F-4-M e-pyridin-3-yl 0 B-0128 H H H H H 0 H H 2-F-5-M e-pyridin-3-yl 0 B-0129 H H H H H 0 H H 2-F-6-M e-pyridin-3-yl 0 B-0130 H H H H H 0 H H 4-F-2-M e-pyridin-3-yl 0 B-0131 H H H H H 0 H H 4-F-5-M e-pyridin-3-yl 0 B-0132 H H H H H 0 H H 4-F-6-M e-pyridin-3-yl 0 B-0133 H H H H H 0 H H 2-F-4-0Me-pyridin-3-y 0 B-0134 H H H H H 0 H H 2-F-5-0Me-pyridin-3-y 0 B-0135 H H H H H 0 H H 2-F-6-0Me-pyridin-3-yI 0 B-0136 H H H H H 0 H H 4-F-2-0Me-pyridin-3-yI 0 B-0137 H H H H H 0 H H 4-F-5-0Me-pyridin-3-yI 0 B-0138 H H H H H 0 H H 4-F-6-0Me-pyridin-3-yI 0 B-0139 H H H H H 0 H H 2-CI-5-F-pyridin-3-y 0 B-0140 H H H H H 0 H H 2-CI-6-F-pyridin-3-y 0 B-0141 H H H H H 0 H H 4-CI-5-F-pyridin-3-y 0 B-0142 H H H H H 0 H H 4-CI-6-F-pyridin-3-y 0 B-0143 H H H H H 0 H H 2-CI-4-Me-pyridh-3-y 0 B-0144 H H H H H 0 H H 2-CI-5-M e-pyridh-3-y 0 B-0145 H H H H H 0 H H 2-CI-6-M e-pyridh-3-y 0 B-0146 H H H H H 0 H H 4-CI-2-M e-pyridh-3-y 0 B-0147 H H H H H 0 H H 4-CI-5-Me-pyridh-3-y 0 B-0148 H H H H H 0 H H 4-CI-6-M e-pyridh-3-y 0 B-0149 H H H H H 0 H H 2-M e-5-F-pyridin-3-y 0 B-0150 H H H H H 0 H H 2-M e-6-F-pyridin-3-y 0 B-0151 H H H H H 0 H H 4-M e-5-F-pyridin-3-y 0 B-0152 H H H H H 0 H H 4-M e-6-F-pyridin-3-y 0 B-0153 H H H H H 0 H H 2-M e-5-Cl-pyridh-3-y 0 B-0154 H H H H H 0 H H 2-M e-6-Cl-pyridh-3-y 0 B-0155 H H H H H 0 H H 4-M e-5-Cl-pyridh-3-y 0 B-0156 H H H H H 0 H H 4-M e-6-Cl-pyridh-3-y 0 B-0157 H H H H H 0 H H 2,4-(Me) 2-pyridin-3-yI 0 B-0158 H H H H H 0 H H 2,5-(Me) 2-pyridin-3-yI 0 B-0159 H H H H H 0 H H 2,6-(Me) 2-pyridin-3-yI 0 B-0160 H H H H H 0 H H 4,5-(Me) 2-pyridin-3-yI 0 B-0161 H H H H H 0 H H 4,6-(Me) 2-pyridin-3-yI 0 B-0162 H H H H H 0 H H 2-Me-4-0Me-pyridin-3-y 0 B-0163 H H H H H 0 H H 2-Me-5-0Me-pyridin-3-y 0 B-0164 H H H H H 0 H H 2-Me-6-0Me-pyridin-3-y 0 B-0165 H H H H H 0 H H 4-Me-2-0Me-pyridin-3-y 0 B-0166 H H H H H 0 H H 4-Me-5-0Me-pyridin-3-y 0
[0305]
[Table 180]
com pound R' R2 Rj R4 R A R6 R p B-0167 H H H H H 0 H H 4-Me-6-OMe-pyridin-3-yl 0 B-0168 H H H H H 0 H H 2-CF 3 -4-F-pyridin-3-yl 0 B-0169 H H H H H 0 H H 2-GF 3 -b--pyrdin-3-yl 0 B-0170 H H H H H 0 H H 2-G 3-6-F-pyridin-3-yl 0 B-0171 H H H H H 0 H H 4-0F 3 -2-F-pyridin-3-yl 0 B-0172 H H H H H 0 H H 4-GF 3 -5-F-pyridin-3-yl 0 B-0173 H H H H H 0 H H 4-CF 3 -6-F-pyridin-3-yl 0 B-0174 H H H H H 0 H H 2-CF 3-4-Me-pyridin-3-yl 0 B-0175 H H H H H 0 H H 2-CF 3-b-Me-pyridin-3-yl 0 B-0176 H H H H H 0 H H 2-UF 3-6-M e-pyridin-3-yl 0 B-0177 H H H H H 0 H H 4-CF 3-2-M e-pyridin-3-yl 0 B-0178 H H H H H 0 H H 4-CF 3-b-Me-pyridin-3-yl 0 B-0179 H H H H H 0 H H 4-GCF-6-M e-pyridin-3-yl 0 B-0180 H H H H H 0 H H 2-0Me-b-F-pyridin-3-yI 0 B-0181 H H H H H 0 H H 2-0Me-6-F-pyridin-3-yI 0 B-0182 H H H H H 0 H H 4-0Me-5-F-pyridin-3-yI 0 B-0183 H H H H H 0 H H 4-0Me-6-F-pyridin-3-yI 0 B-0184 H H H H H 0 H H 2-0Me-4-Cl-pyridin-3-y 0 B-0185 H H H H H 0 H H 2-0Me-5-Cl-pyridin-3-y 0 B-0186 H H H H H 0 H H 2-0Me-6-Cl-pyridin-3-yI 0 B-0187 H H H H H 0 H H 4-0Me-2-Cl-pyridin-3-y 0 B-0188 H H H H H 0 H H 4-0Me-5-Cl-pyridin-3-y 0 B-0189 H H H H H 0 H H 4-0Me-6-Cl-pyridin-3-y 0 B-0190 H H H H H 0 H H 2-0Me-b-M e-pyridin-3-y 0 B-0191 H H H H H 0 H H 2-0Me-6-M e-pyridin-3-y 0 B-0192 H H H H H 0 H H 4-0Me-5-MAe-pyridin-3-y 0 B-0193 H H H H H 0 H H 4-0Me-6-MAe-pyridin-3-y 0 B-0194 H H H H H 0 H H 2,4-(0Me) 2 -pyridin-3-y 0 B-0195 H H H H H 0 H H 2,b-(OMe) 2 -pyrdin-3-y 0 B-0196 H H H H H 0 H H 2,6-(0Me)2-pyridin-3-yI 0 B-0197 H H H H H 0 H H 4,b-(0Me) 2 -pyridin-3-y 0 B-0198 H H H H H 0 H H 4,6-(0Me) 2 -pyridin-3-y 0 B-0199 H H H H H 0 H H pyridin-4-yI 0 B-0200 H H H H H 0 H H 2-F-pyridh-4-yI 0 B-0201 H H H H H 0 H H 3-F-pyridh-4-yI 0 B-0202 H H H H H 0 H H 2-Cl-pyridin-4-y 0 B-0203 H H H H H 0 H H 3-Cl-pyridin-4-y 0 B-0204 H H H H H 0 H H 2-M e-pyridin-4-yI 0 B-0205 H H H H H 0 H H 3-M e-pyridin-4-yI 0 B-0206 H H H H H 0 H H 2-0F 3 -pyridin-4-yl 0 B-0207 H H H H H 0 H H 3-CF 3 -pyridin-4-yI 0 B-0208 H H H H H 0 H H 2-0Me-pyridin-4-yI 0 B-0209 H H H H H 0 H H 3-0Me-pyridin-4-yI 0 B-0210 H H H H H 0 H H 2,3- 2-pyrdin-4-yl 0 B-0211 H H H H H 0 H H 2,b-F 2-pyridin-4-yI 0 B-0212 H H H H H 0 H H 2,64 2-pyridin-4-yl 0 B-0213 H H H H H 0 H H 3,b-F 2-pyridin-4-yI 0 B-0214 H H H H H 0 H H 2,3-C -pyridin-4-yl 0 B-0215 H H H H H 0 H H 2,b-C -pyridin-4-yl 0 B-0216 H H H H H 0 H H 2,6-C -pyridin-4-yl 0 B-0217 H H H H H 0 H H 3,b-C -pyridin-4-yl 0 B-0218 H H H H H 0 H H 3-F-2-Cl-pyridin-4-y 0 B-0219 H H H H H 0 H H 3-F-5-Cl-pyridin-4-y 0 B-0220 H H H H H 0 H H 3-F-6-Cl-pyridin-4-y 0 B-0221 H H H H H 0 H H 3-F-2-M e-pyridin-4-yl 0 B-0222 H H H H H 0 H H 3-F-5-Me-pyridin-4-y 0 B-0223 H H H H H 0 H H 3-F-6-Me-pyridin-4-y 0
[0306]
[Table 181]
com pound R' R2 Rj R4 R A R6 R p B-0224 H H H H H 0 H H 3-F-2-0Me-pyridin-4-yI 0 B-0225 H H H H H 0 H H 3-F-5-0Me-pyridin-4-yI 0 B-0226 H H H H H 0 H H 3-F-6-0Me-pyridin-4-yI 0 B-0227 H H H H H 0 H H 3-CI-2-F-pyridin-4-y 0 B-0228 H H H H H 0 H H 3-CI-6-F-pyridin-4-y 0 B-0229 H H H H H 0 H H 3-CI-2-M e-pyridh-4-y 0 B-0230 H H H H H 0 H H 3-CI-5-Me-pyridh-4-y 0 B-0231 H H H H H 0 H H 3-CI-6-M e-pyridh-4-y 0 B-0232 H H H H H 0 H H 3-M e-2-F-pyridin-4-y 0 B-0233 H H H H H 0 H H 3-M e-6-F-pyridin-4-y 0 B-0234 H H H H H 0 H H 3-M e-2-Cl-pyridh-4-y 0 B-0235 H H H H H 0 H H 3-M e-6-Cl-pyridh-4-y 0 B-0236 H H H H H 0 H H 2,3-(Me) 2-pyrdin-4-yl 0 B-0237 H H H H H 0 H H 3,b-(M e) 2-pyrid in-4-y 1 0 B-0238 H H H H H 0 H H 3,6-(Me) 2-pyridin-4-yI 0 B-0239 H H H H H 0 H H 3-Me-2-0Me-pyridin-4-y 0 B-0240 H H H H H 0 H H 3-Me-5-0Me-pyridin-4-y 0 B-0241 H H H H H 0 H H 3-Me-6-0Me-pyridin-4-y 0 B-0242 H H H H H 0 H H 3-CF 3 -2-F-pyridin-4-yl 0 B-0243 H H H H H 0 H H 3-GF 3 -5-F-pyrdin-4-yl 0 B-0244 H H H H H 0 H H 3-CF 3 -6-F-pyridin-4-yI 0 B-0245 H H H H H 0 H H 3-CF 3-2-Me-pyridin-4-y 0 B-0246 H H H H H 0 H H 3-CF 3-b-Me-pyridin-4-y 0 B-0247 H H H H H 0 H H 3-GF 3 -6-M e-pyrdin-4-y 0 B-0248 H H H H H 0 H H 3-0Me-2-F-pyridin-4-yI 0 B-0249 H H H H H 0 H H 3-0Me-6-F-pyridin-4-yI 0 B-0250 H H H H H 0 H H 3-0Me-2-Cl-pyridin-4-y 0 B-0251 H H H H H 0 H H 3-0Me-5-Cl-pyridin-4-yI 0 B-0252 H H H H H 0 H H 3-0Me-6-Cl-pyridin-4-y 0 B-0253 H H H H H 0 H H 3-0Me-2-MAe-pyridin-4-y 0 B-0254 H H H H H 0 H H 3-0Me-6-MAe-pyridin-4-y 0 B-0255 H H H H H 0 H H 2,3-(0Me) 2 -pyridin-4-y 0 B-0256 H H H H H 0 H H 3,b-(OMe) 2 -pyridin-4-y 0 B-0257 H H H H H 0 H H 3,6-(0Me) 2 -pyridin-4-y 0 B-0258 H H H H H 0 H H pyrin idin-2-yl 0 B-0259 H H H H H 0 H H pyrin idin-4-yl 0 B-0260 H H H H H 0 H H 5-F-pyrin idin-4-yl 0 B-0261 H H H H H 0 H H 5-MAe-pyrin idin-4-yI 0 B-0262 H H H H H 0 H H b-0F 3 -pyrm dn-4-yl 0 B-0263 H H H H H 0 H H 5-OMe-pyrm idin-4-yI 0 B-0264 H H H H H 0 H H pyrin idin-5-yl 0 B-0265 H H H H H 0 H H 4-F-pyrin idin-5-yl 0 B-0266 H H H H H 0 H H 4-ClF-pyrin idin-5-y 0 B-0267 H H H H H 0 H H 4-MAe-pyrin idin-5-y 0 B-0268 H H H H H 0 H H 4-CF 3-pyrin idh-5-yl 0 B-0269 H H H H H 0 H H 4-0Me-pyrm idin-5-yI 0 B-0270 H H H H H 0 H H pyridazh-3-yl 0 B-0271 H H H H H 0 H H 4-F-pyridazin-3-yI 0 B-0272 H H H H H 0 H H 4-Cl-pyridazin-3-yI 0 B-0273 H H H H H 0 H H 4-Me-pyridazh-3-y 0 B-0274 H H H H H 0 H H 4-CF 3-pyridazh-3-yI 0 B-0275 H H H H H 0 H H 4-0Me-pyridazin-3-y 0 B-0276 H H H H H 0 H H pyridazh-4-yI 0 B-0277 H H H H H 0 H H 3-F-pyridazin-4-yI 0 B-0278 H H H H H 0 H H 3-Cl-pyridazin-4-y 0 B-0279 H H H H H 0 H H 3-Me-pyridazh-4-y 0 B-C280 H H H H H 0 H H 3-F 3-pyridazn-4-yl 0
[0307]
[Table 182]
com pound R' R2 Rj R4 R A R6 R p B-0281 H H H H H 0 H H 3-OMe-pyridazin-4-yl 0 B-0282 H H H H H 0 H H 5-F-pyridazin-4-yI 0 B-0283 H H H H H 0 H H 5-Cl-pyridazin-4-y 0 B-0284 H H H H H 0 H H 5-Me-pyridazh-4-y 0 B-0285 H H H H H 0 H H b-GF 3-pyrdazn-4-yl 0 B-0286 H H H H H 0 H H 5-0Me-pyridazin-4-y 0 B-0287 H H H H H 0 H H thiophen-2-yI 0 B-0288 H H H H H 0 H H 3-F-thiophen-2-yI 0 B-0289 H H H H H 0 H H 3-Cl-thiophen-2-yI 0 B-0290 H H H H H 0 H H 3-M e-thiophen-2-yI 0 B-0291 H H H H H 0 H H 3-0F3-thiophen-2-y 0 B-0292 H H H H H 0 H H 3-0Me-thiophen-2-yI 0 B-0293 H H H H H 0 H H thiophen-3-yI 0 B-0294 H H H H H 0 H H 2-F-thiophen-3-yI 0 B-0295 H H H H H 0 H H 2-Cl-thiophen-3-yI 0 B-0296 H H H H H 0 H H 2-M e-thiophen-3-yI 0 B-0297 H H H H H 0 H H 2-CF 3 -thiophen-3-y 0 B-0298 H H H H H 0 H H 2-0Me-thiophen-3-yI 0 B-0299 H H H H H 0 H H 4-F-thiophen-3-yI 0 B-0300 H H H H H 0 H H 4-Cl-thiophen-3-yI 0 B-0301 H H H H H 0 H H 4-M e-thiophen-3-yI 0 B-0302 H H H H H 0 H H 4-CF 3 -thiophen-3-y 0 B-0303 H H H H H 0 H H 4-0Me-thiophen-3-y 0 B-0304 H H H H H 0 H H thiazol-2-yI 0 B-0305 H H H H H 0 H H thiazol-4-yI 0 B-0306 H H H H H 0 H H 5-F-thiazol-4-y 0 B-0307 H H H H H 0 H H 5-MAe-thibzol-4-yI 0 B-0308 H H H H H 0 H H b-F 3 -thiazol-4-yl 0 B-0309 H H H H H 0 H H b-OMe-thiazol-4-y 0 B-0310 H H H H H 0 H H thiazol-5-yI 0 B-0311 H H H H H 0 H H 4-F-thiazol-5-y 0 B-0312 H H H H H 0 H H 4-MAe-thibzol-5-yI 0 B-0313 H H H H H 0 H H 4-CF 3 -thiazol-5-yI 0 B-0314 H H H H H 0 H H 4-0Me-thiazol-5-yI 0 B-0315 H H H H H 0 H H 1 H-pyrrol1-yI 0 B-0316 H H H H H 0 H H 2-F-1 H-pyrrol1-yI 0 B-0317 H H H H H 0 H H 2-M e-1 H-pyrrol1-y 0 B-0318 H H H H H 0 H H 2-CF 3 -1 H-pyrrol1-yl 0 B-0319 H H H H H 0 H H 2-0Me-1 H-pyrrol1-yI 0 B-0320 H H H H H 0 H H 1 H-pyrrol-2-yI 0 B-0321 H H H H H 0 H H 1-MAe-1 H-pyrrol-2-yI 0 B-0322 H H H H H 0 H H 3-F-1 H-pyrrol-2-yI 0 B-0323 H H H H H 0 H H 3-Me-1 H-pyrrol-2-y 0 B-0324 H H H H H 0 H H 3- F 3 -1 H-pyrrol-2-yl 0 B-0325 H H H H H 0 H H 3-0Me-1 H-pyrrol-2-yI 0 B-0326 H H H H H 0 H H 1-M e-3-F-1 H-pyrrol-2-yl 0 B-0327 H H H H H 0 H H 1,3-(Me) 2-1 H-pyrrol-2-y 0 B-0328 H H H H H 0 H H 1-MAe-3-CF 3 -1 H-pyrrol-2-yl 0 B-0329 H H H H H 0 H H 1-MAe-3-0Me-1 H-pyrrol-2-yI 0 B-0330 H H H H H 0 H H 1 H-pyrrol-3-yI 0 B-0331 H H H H H 0 H H 1-MAe-1 H-pyrrolk3-yI 0 B-0332 H H H H H 0 H H 2-F-1 H-pyrrol-3-yI 0 B-0333 H H H H H 0 H H 2-M e-1 H-pyrrok3-y 0 B-0334 H H H H H 0 H H 2-CF 3 -1 H-pyrrolk3-yI 0 B-0335 H H H H H 0 H H 2-0Me-1H -pyrrol-3-yI 0 B-0336 H H H H H 0 H H 1-M e-2-F-1 H-pyrrol-3-yl 0 B-0337 H H H H H 0 H H 1,2-(Me) 2-1H -pyrrol-3-y 0
[0308]
[Table 183]
com pound R' R2 Rj R4 R A R6 R p B-0338 H H H H H 0 H H 1-M e-2-CF 3 -1H-pyrrol-3-yl 0 B-0339 H H H H H 0 H H 1-M e-2-OMe-1 H-pyrrol-3-yI 0 B-0340 H H H H H 0 H H 4-F-1H-pyrrol-3-yI 0 B-0341 H H H H H 0 H H 4-Me-1 H-pyrrol-3-yl 0 B-0342 H H H H H 0 H H 4-0F 3 -1H-pyrrol-3-yl 0 B-0343 H H H H H 0 H H 4-OMe-1H-pyrrol-3-yl 0 B-0344 H H H H H 0 H H 1-M e-4-F-1 H-pyrrol-3-yl 0 B-0345 H H H H H 0 H H 1,4-(Me) 2-1 H-pyrrol-3-yl 0 B-0346 H H H H H 0 H H 1-M e-4-CF 3 -1H-pyrrol-3-yl 0 B-0347 H H H H H 0 H H 1-M e-4-OMe-1 H-pyrrol-3-yI 0 B-0348 H H H H H 0 H H 1 H-pyrazol-yl 0 B-0349 H H H H H 0 H H 5-F-1 H-pyrazol-yl 0 B-0350 H H H H H 0 H H 5-C-1H-pyrazol-yl 0 B-0351 H H H H H 0 H H 5-M e-1 H-pyrazol1-yI 0 B-0352 H H H H H 0 H H 5-CF 3 -1H-pyrazol1-yI 0 B-0353 H H H H H 0 H H 5-0Me-1 H-pyrazol1-yI 0 B-0354 H H H H H 0 H H 1 H-pyrazol-3-yI 0 B-0355 H H H H H 0 H H 1 -M e-1 H-pyrazol-3-yI 0 B-0356 H H H H H 0 H H 4-F-1 H-pyrazol-3-yI 0 B-0357 H H H H H 0 H H 4-C-1H -pyrazol-3-yI 0 B-0358 H H H H H 0 H H 4-M e-1 H-pyrazol-3-yI 0 B-0359 H H H H H 0 H H 4-CF 3 -1H-pyrazol-3-yI 0 B-0360 H H H H H 0 H H 4-0Me-1 H-pyrazol-3-yI 0 B-0361 H H H H H 0 H H 1 -M e-4-F-1H-pyrazol-3-yI 0 B-0362 H H H H H 0 H H 1 -M e-4-CI-1H-pyrazol-3-y 0 B-0363 H H H H H 0 H H 1,4-(Me) 2 -1 H-pyrazol-3-y 0 B-0364 H H H H H 0 H H 1 -M e-4-CF 3-1 H-pyrazol-3-y 0 B-0365 H H H H H 0 H H 1 -M e-4-0Me-1 H-pyrazol-3-yI 0 B-0366 H H H H H 0 H H 1H -pyrazol-4-yI 0 B-0367 H H H H H 0 H H 1 -M e-1 H-pyrazol-4-yI 0 B-0368 H H H H H 0 H H 3-F-1 H-pyrazol-4-yI 0 B-0369 H H H H H 0 H H 3-C-1HH-pyrazol-4-yI 0 B-0370 H H H H H 0 H H 3-M e-1 H-pyrazol-4-yI 0 B-0371 H H H H H 0 H H 3-CF 3 -1H-pyrazol-4-yI 0 B-0372 H H H H H 0 H H 3-0Me-1 H-pyrazol-4-yI 0 B-0373 H H H H H 0 H H 1 -M e-3-F-1 H-pyrazol-4-y 0 B-0374 H H H H H 0 H H 1 -M e-3-CI-1H-pyrazol-4-y 0 B-0375 H H H H H 0 H H 1,3-(Me) 2 -1 H-pyrazol-4-yI 0 B-0376 H H H H H 0 H H 1-Me-3-CF 3-1 H-pyrazol-4-yl 0 B-0377 H H H H H 0 H H 1 -M e-3-0Me-1 H-pyrazol-4-yI 0 B-0378 H H H H H 0 H H 5-F-1 H-pyrazol-4-yI 0 B-0379 H H H H H 0 H H 5-CI-1H-pyrazol-4-yI 0 B-0380 H H H H H 0 H H 5-M e-1 H-pyrazol-4-yI 0 B-0381 H H H H H 0 H H b-GF 3 -1H-pyrazol-4-yl 0 B-0382 H H H H H 0 H H 5-0Me-1 H-pyrazol-4-yI 0 B-0383 H H H H H 0 H H 1-Me-5-F-1 H-pyrazol-4-y 0 B-0384 H H H H H 0 H H 1-M e-5-CI-1H-pyrazol-4-yl 0 B-0385 H H H H H 0 H H 1,5-(Me) 2 -1 H-pyrazol-4-y 0 B-0386 H H H H H 0 H H 1-M e-5-CF 3-1 H-pyrazol-4-yl 0 B-0387 H H H H H 0 H H 1 -M e-5-0Me-1 H-pyrazol-4-y 0 B-0388 H H H H H 0 H H 1 H-pyrazol-5-yI 0 B-0389 H H H H H 0 H H 1 -M e-1 H-pyrazol-5-yI 0 B-0390 H H H H H 0 H H 4-F-1 H-pyrazol-5-yI 0 B-0391 H H H H H 0 H H 4-CI1H-pyrazol-5-y 0 B-0392 H H H H H 0 H H 4-M e-1H-pyrazol-5-yI 0 B-0393 H H H H H 0 H H 4-CF 3 -1H-pyrazol-5-yI 0 B-0394 H H H H H 0 H H 4-0Me-1H-pyrazol-5-y 0
[0309]
[Table 184]
com pound R' R2 Rj R4 R A R6 R' p B-0395 H H H H H 0 H H 1-M e-4-F-1H-pyrazol-5-yl 0 B-0396 H H H H H 0 H H 1-M e-4-Ci-1H-pyrazol-5-yl 0 B-0397 H H H H H 0 H H 1,4-(Me) 2 -i1H-pyrazol-b-yl 0 B-0398 H H H H H 0 H H 1-Me-4-GF 3-1H-pyrazol-5-yl 0 B-0399 H H H H H 0 H H 1-M e-4-OMe-iH-pyrazol-b-yl 0 B-0400 H H H H H 0 H H furan-2-yl 0 B-0401 H H H H H 0 H H 3-F-furan-2-yl 0 B-0402 H H H H H 0 H H 3 -M e-furan-2-yl 0 B-0403 H H H H H 0 H H 3-CF3-furan-2-yl 0 B-0404 H H H H H 0 H H 3-0Me-fu ran-2-yl 0 B-0405 H H H H H 0 H H furan-3-yl 0 B-0406 H H H H H 0 H H 2-F-furan-3-yl 0 B-0407 H H H H H 0 H H 2 -M e-furan-3-yl 0 B-0408 H H H H H 0 H H 2-F 3-turan-3-yl 0 B-0409 H H H H H 0 H H 2-0Me-fu ran-3-yl 0 B-0410 H H H H H 0 H H 4-F-furan-3-yl 0 B-0411 H H H H H 0 H H 4-M e-furan-3-yl 0 B-0412 H H H H H 0 H H 4-GF 3-turan-3-yl 0 B-0413 H H H H H 0 H H 4-0Me-fu ran-3-yl 0 B-0414 H H H H H 0 H H isoxazol-3-yl 0 B-0415 H H H H H 0 H H 4-F-isoxazol-3-yl 0 B-0416 H H H H H 0 H H 4-M e-isoxazol-3-yl 0 B-0417 H H H H H 0 H H 4-CF 3 -isoxazol-3-yl 0 B-0418 H H H H H 0 H H 4-0Me-isoxazol-3-yl 0 B-0419 H H H H H 0 H H isoxazol-4-yl 0 B-0420 H H H H H 0 H H 5-F-isoxazol-4-yl 0 B-0421 H H H H H 0 H H 5-M e-isoxazol-4-yl 0 B-0422 H H H H H 0 H H b-GF 3 -isoxazol-4-yl 0 B-0423 H H H H H 0 H H b-OMe-isoxazol-4-y 0 B-0424 H H H H H 0 H H isoxazol-5-yl 0 B-0425 H H H H H 0 H H 4-F-isoxazol-5-yl 0 B-0426 H H H H H 0 H H 4-M e-isoxazol-5-yl 0 B-0427 H H H H H 0 H H 4-CF 3 -isoxazol-5-y 0 B-0428 H H H H H 0 H H 4-0Me-isoxazol-5-y 0 B-0429 H H H H H 0 H H 1H-1,2,3-triazol-i-yl 0 B-0430 H H H H H 0 H H 5-F-1iH-12,3-triazoli-1 0 B-0431 H H H H H 0 H H 5-Me-1H -1,2,3-triazol-1-y 0 B-0432 H H H H H 0 H H b-F3-1 H-1,2,3-triazoH-yl 0 B-0433 H H H H H 0 H H 5-0Me-1H-1,2,3-triazoH-y 0 B-0434 H H H H H 0 H H 1H-1,2,3-triazol-4-yl 0 B-0435 H H H H H 0 H H 5-F-1H-1,2,3-triazol-4-y 0 B-0436 H H H H H 0 H H 5-Me-1H-1,2,3-triazo-4-yl 0 B-0437 H H H H H 0 H H 5-CF 3-1H-1,2,3-triazo-4-y 0 B-0438 H H H H H 0 H H 5-0Me-1H-1,2,3-triazo-4-y 0 B-0439 H H H H H 0 H H 1H-1,2,3-triazol-5-yl 0 B-0440 H H H H H 0 H H 4-F-1H-1,2,3-triazol-5-y 0 B-0441 H H H H H 0 H H 4-Me-1H-1,2,3-triazol-5-y 0 B-0442 H H H H H 0 H H 4-CF 3-1H-1,2,3-triazo-5-y 0 B-0443 H H H H H 0 H H 4-0Me-1H-1,2,3-triazol-b-y 0 B-0444 H H H H H 0 H H 1H-1,2,4-triazo[H-yl1 0 B-0445 H H H H H 0 H H 5-Me-1H-1,2,4-triazoH-y 0 B-0446 H H H H H 0 H H 5-F-1H-1,2,4-triazoH-yl 0 B-0447 H H H H H 0 H H 5-CF 3-1H-1,2,4-triazoH-y 0 B-0448 H H H H H 0 H H 5-0Me-1H-1,2,4-triazoH-y 0 B-0449 H H H H H 0 H H 1H -1,2,4-triazol-3-yl 0 B-0450 H H H H H 0 H H 1-M e-1H-1,2,4-triazol-3-yl 0 B-04bI H H H H H 0 H H IH-1,2,4-triazol-5-yl 0
[0310]
[Table 185] cornpound mR' R RTR A R R o B-0452 H H H H H 0 H H 1 -Mve -1 H -1,2,4-tr ia zob-5-yI1 0 B -0 4 53 H H H H H 0 H H 3,5-(M e) 2 -iSoxaZo[-4-yI1 0 B-0454 H H H H H 0 H H 3,5-(Et)2 -SoxaZo[-4-v1 0 B-0455 H H H H H 0 H H 1,3,5-(M e) 3 -1 H-pyrazo[-4-y 1 0 B-0456 H H H H H 0 H H qu ho lin-4-yI1 0 B-0457 H H H H H 0 H H isoqu ho lin-4-yI1 0 B-0458 H H H H H 0 H H 3,6-(M e) 2 -pyriazin-4-yI 0 B-0459 IH IH IH IH IH 10 1H IH 2,4-(0M e) 2 -pyrmn iin-5-yI0
[0311]
[Table 186]
R3 R2 A KR
RO) R6
cornpound R'__ Rz RWR4 A Ru R 0 p B-5001 H H H H H 0 H H CI 1 B-5002 H H H H H 0 H H Br 1 B-5003 H H H H H 0 H H I 1 B-5004 H H H H H 0 H H naphtha len-1 -yI 1 B-5005 H H H H H 0 H H 2-F-naphtha ln-1 -yI 1 B-5006 H H H H H 0 H H 2-M e-naphtha ln-1 -yI 1 B-5007 H H H H H 0 H H 2-CF 3-naphtha len-1-y 1 1 B-5008 H H H H H 0 H H 2-0 Me-naphtha len-1 -yI 1 B-5009 H H H H H 0 H H naphtha len-2-y I 1 B-501l0 H H H H H 0 H H I -F-naphthalIen-2-y I 1 B-501 1 H H H H H 0 H H 1-iAle-naphtha In-2-y I 1 B-501 2 H H H H H 0 H H 1 -CF 3-naphtiialen-2-y 1 1 B-501 3 H H H H H 0 H H 1 -0 Me-naphtha In-2-y I 1 B-501 4 H H H H H 0 H H 3-F-naphtha In-2-y I 1 5-501 5 H H H H H 0 H H 3-M e-naphtha In-2-y I 1 B-501 6 H H H H H 0 H H 3-CF 3-naphthalIen-2-y 1 1 B-501 7 H H H H H 0 H H 3-OM e-naphthalIen-2-y I 1 B-501 8 H H H H H 0 H H pyrkidi-2-y I 1 B-501 9 H H H H H 0 H H 3-F-pyid in-2-y I1 B-5020 H H H H H 0 H H 4-F--pyriin-2-y I 1 B-5021 H H H H H 0 H H 5 -F-py r iin -2 -y I 1 B -5 02 2 H H H H H 0 H H 6-F--pyriin-2-y I 1 5-5023 H H H H H 0 H H 3-Cbpyriin-2-y I 1 5-5024 H H H H H 0 H H 4-C bpyrid in-2-y II 5-5025 H H H H H 0 H H 5-Cbpyriin-2-y I 1 B-5026 H H H H H 0 H H 6-C bpyriin-2-y I 1 B-5027 H H H H H 0 H H 3-M le-pyri i-2-y I 1 B-5028 H H H H H 0 H H 4-M le-pyriin-2-y I 1 5-5029 H H H H H 0 H H 5-M e-pyri i-2-y I 1 B-5030 H H H H H 0 H H 6-M e-pyri i-2-y I 1 5-5031 H H H H H 0 H H 3-CF 3 -pyri i-2-yI1 1 5-5032 H H H H H 0 H H 4-CF 3-pyrid i-2-yI1 1 5-5033 H H H H H 0 H H b-CUF 3 -Pyriri-2-yI1 1 5-5034 H H H H H 0 H H 6-CF 3 -Pyri i-2-y 1 1 5-5035 H H H H H 0 H H 3--0M e-pyridin-2-y I 1 5-5036 H H H H H 0 H H 4-OM e-pyriin-2-y I 1 5-5037 H H H H H 0 H H 5-OM e-pyriin-2-y I 1 5-5038 H H H H H 0 H H 6--0M e-pyridin-2-y I 1 5-5039 H H H H H 0 H H 3,4-F2 -Pyrid in-2-yI1 1 5-5040 H H H H H 0 H H 3,5-F2 -pyrid i-2-yI1 1 5-5041 H H H H H 0 H H 3,6-F2 -Pyrid i-2-yI1 1 5-5042 H H H H H 0 H H 3,4-C6-p yr i i-2-yI1 1 5-5 0 43 H H H H H 0 H H 3,5-C 6-pyrki i-2-yI1 1 5-5 0 44 H H H H H 0 H H 3,6-C 6-pyrkid i-2-yI1 1 5-5 0 45 H H H H H 0 H H 3 -F-4 -C I-p yr i i-2 -yI 1 B 504 6 H H H H H 0 H H 3-F-S-C pyri -2-y I 1 B 50 47 H H H H H 0 H H 3-F-6-CI-pyrid i-2-y I 1 B 504 8 H H H H H 0 H H 3-F-4-M e-pyrid i-2-y I 1 B 504 9 H H H H H 0 H H 3 -F-5 -M e-py r idin-2 -yI 1 B 5OS0 H H H H H 0 H H 3-F-6-M e-pyrid -2-y I1 B 5O5 1 H H H H H 0 H H 3 -F-4 -OM e-pyr idin-2 -y I 1 B 5052 H H H H H 0 H H 3 -F -5-0 Me-p y r in-2 -yI 1
[0312]
[Table 187]
com pound R' R2 Rj R4 R A R6 R p B-5053 H H H H H 0 H H 3-F-6-OMe-pyridh-2-yl 1 B-5054 H H H H H 0 H H 3-CI-4-F-pyridh-2-yI 1 B-5055 H H H H H 0 H H 3-CI-5-F-pyridh-2-yI 1 B-5056 H H H H H 0 H H 3-CI-6-F-pyridh-2-yI 1 B-5057 H H H H H 0 H H 3-CI-4-Me-pyridin-2-y 1 B-5058 H H H H H 0 H H 3-CI-5-Me-pyridin-2-y 1 B-5059 H H H H H 0 H H 3-CI-6-Me-pyridin-2-y 1 B-5060 H H H H H 0 H H 3-MAe-4-F-pyridin-2-yI 1 B-5061 H H H H H 0 H H 3-MAe-5-F-pyridin-2-y 1 B-5062 H H H H H 0 H H 3-MAe-6-F-pyridin-2-yI 1 B-5063 H H H H H 0 H H 3-Me-4-Cl-pyridin-2-y 1 B-5064 H H H H H 0 H H 3-Me-5-Cl-pyridin-2-yI 1 B-5065 H H H H H 0 H H 3-Me-6-Cl-pyridin-2-y 1 B-5066 H H H H H 0 H H 3,4-(M e) 2-pyridin-2-yI 1 B-5067 H H H H H 0 H H 3,5-(Me) 2-pyridin-2-yI 1 B-5068 H H H H H 0 H H 3,6-(Me) 2-pyridin-2-yI 1 B-5069 H H H H H 0 H H 3-MAe-4-0Me-pyridin-2-yI 1 B-5070 H H H H H 0 H H 3-M e-5-0Me-pyriin-2-yI 1 B-5071 H H H H H 0 H H 3-MAe-6-0Me-pyridin-2-yI 1 B-5072 H H H H H 0 H H 3-GF 3 -4-F-pyridin-2-yl 1 B-5073 H H H H H 0 H H 3-CF 3-5-F-pyridin-2-yI 1 B-5074 H H H H H 0 H H 3-CF 3-6-F-pyridin-2-yI 1 B-5075 H H H H H 0 H H 3-CF 3 -4-Me-pyridin-2-y 1 B-5076 H H H H H 0 H H 3-CF 3 -- M e-pyrdin-2-y 1 B-5077 H H H H H 0 H H 3-CF 3 -6-Me-pyridin-2-y 1 B-5078 H H H H H 0 H H 3-0Me-4-F-pyridh-2-y 1 B-5079 H H H H H 0 H H 3-0Me-5-F-pyridh-2-yI 1 B-5080 H H H H H 0 H H 3-0Me-6-F-pyridh-2-y 1 B-5081 H H H H H 0 H H 3-0Me-4-Cl-pyridh-2-yI 1 B-5082 H H H H H 0 H H 3-0Me-5-Cl-pyridh-2-yI 1 B-5083 H H H H H 0 H H 3-0Me-6-Cl-pyridh-2-yI 1 B-5084 H H H H H 0 H H 3-0Me-4-M e-pyridin-2-yI 1 B-5085 H H H H H 0 H H 3-0Me-5-M e-pyridin-2-yI 1 B-5086 H H H H H 0 H H 3-0Me-6-M e-pyridin-2-yI 1 B-5087 H H H H H 0 H H 3,4-(0Me) 2 -pyridin-2-y 1 B-5088 H H H H H 0 H H 3,5-(0Me) 2 -pyridin-2-yI 1 B-5089 H H H H H 0 H H 3,6-(0Me) 2 -pyridin-2-y 1 B-5090 H H H H H 0 H H pyridin-3-yI 1 B-5091 H H H H H 0 H H 2-F-pyridin-3-yI 1 B-5092 H H H H H 0 H H 4-F-pyridin-3-yI 1 B-5093 H H H H H 0 H H 5-F-pyridin-3-y 1 B-5094 H H H H H 0 H H 6-F-pyridin-3-yI 1 B-5095 H H H H H 0 H H 2-Cl-pyridin-3-yI 1 B-5096 H H H H H 0 H H 4-Cl-pyridin-3-yI 1 B-5097 H H H H H 0 H H 5-Cl-pyridin-3-yI 1 B-5098 H H H H H 0 H H 6-Cl-pyridin-3-yI 1 B-5099 H H H H H 0 H H 2-MAe-pyridin-3-y 1 B-5100 H H H H H 0 H H 4-M e-pyridin-3-y 1 B-5101 H H H H H 0 H H 5-M e-pyridin-3-y 1 B-5102 H H H H H 0 H H 6-M e-pyridin-3-y 1 B-5103 H H H H H 0 H H 2-CF 3-pyridin-3-yI 1 B-5104 H H H H H 0 H H 4-CF 3-pyridin-3-yI 1 B-5105 H H H H H 0 H H 5-CF 3-pyridin-3-yI 1 B-5106 H H H H H 0 H H 6-CF 3-pyridin-3-yI 1 B-5107 H H H H H 0 H H 2-OMe-pyridin-3-yI 1 B-5108 H H H H H 0 H H 4-OMe-pyridin-3-yI 1 B-5109 H H H H H 0 H H 5-OMe-pyridin-3-y 1
[0313]
[Table 188]
com pound R' R2 Rj R4 R A R6 R p B-5110 H H H H H 0 H H 6-OMe-pyridin-3-y 1 B-5111 H H H H H 0 H H 2,4-F 2-pyridin-3-yl 1 B-5112 H H H H H 0 H H 2,b-F 2-pyrdin-3-yl 1 B-5113 H H H H H 0 H H 2,6-F 2-pyrdin-3-yl 1 B-5114 H H H H H 0 H H 4,b-F 2-pyrdin-3-yl 1 B-5115 H H H H H 0 H H 4,6-F 2-pyridin-3-yl 1 B-5116 H H H H H 0 H H 2,4-Cl2-pyridin-3-yl 1 B-5117 H H H H H 0 H H 2,b-Cl2-pyridin-3-yl 1 B-5118 H H H H H 0 H H 2,6-Cl2-pyridin-3-yl 1 B-5119 H H H H H 0 H H 4,b-Cl2-pyrdin-3-yl 1 B-5120 H H H H H 0 H H 4,6-Cl2-pyrdin-3-yl 1 B-5121 H H H H H 0 H H 2-F-4-Cl-pyridh-3-yI 1 B-5122 H H H H H 0 H H 2-F-5-Cl-pyridh-3-yI 1 B-5123 H H H H H 0 H H 2-F-6-Cl-pyridh-3-yI 1 B-5124 H H H H H 0 H H 4-F-2-Cl-pyridh-3-yI 1 B-5125 H H H H H 0 H H 4-F-5-Cl-pyridh-3-yI 1 B-5126 H H H H H 0 H H 4-F-6-Cl-pyridh-3-yI 1 B-5127 H H H H H 0 H H 2-F-4-MAe-pyridin-3-yI 1 B-5128 H H H H H 0 H H 2-F-5-MAe-pyridin-3-yI 1 B-5129 H H H H H 0 H H 2-F-6-MAe-pyridin-3-yI 1 B-5130 H H H H H 0 H H 4-F-2-M e-pyridin-3-yI 1 B-5131 H H H H H 0 H H 4-F-5-M e-pyridin-3-yI 1 B-5132 H H H H H 0 H H 4-F-6-M e-pyridin-3-yI 1 B-5133 H H H H H 0 H H 2-F-4-0Me-pyridh-3-yI 1 B-5134 H H H H H 0 H H 2-F-5-0Me-pyridh-3-y 1 B-5135 H H H H H 0 H H 2-F-6-0Me-pyridh-3-y 1 B-5136 H H H H H 0 H H 4-F-2-0Me-pyridh-3-y 1 B-5137 H H H H H 0 H H 4-F-5-0Me-pyridh-3-y 1 B-5138 H H H H H 0 H H 4-F-6-0Me-pyridh-3-y 1 B-5139 H H H H H 0 H H 2-CI-5-F-pyridh-3-yI 1 B-5140 H H H H H 0 H H 2-CI-6-F-pyridh-3-yI 1 B-5141 H H H H H 0 H H 4-CI-5-F-pyridh-3-yI 1 B-5142 H H H H H 0 H H 4-CI-6-F-pyridh-3-yI 1 B-5143 H H H H H 0 H H 2-CI-4-MAe-pyridin-3-y 1 B-5144 H H H H H 0 H H 2-CI-5-Me-pyridin-3-yI 1 B-5145 H H H H H 0 H H 2-CI-6-M e-pyridin-3-y 1 B-5146 H H H H H 0 H H 4-CI-2-M e-pyridin-3-y 1 B-5147 H H H H H 0 H H 4-CI-5-Me-pyridin-3-yI 1 B-5148 H H H H H 0 H H 4-CI-6-M e-pyridin-3-y 1 B-5149 H H H H H 0 H H 2-MAe-5-F-pyridin-3-yI 1 B-5150 H H H H H 0 H H 2-MAe-6-F-pyridin-3-yI 1 B-5151 H H H H H 0 H H 4-M e-5-F-pyridin-3-yI 1 B-5152 H H H H H 0 H H 4-M e-6-F-pyridin-3-yI 1 B-5153 H H H H H 0 H H 2-M e-5-Cl-pyridin-3-yl 1 B-5154 H H H H H 0 H H 2-M e-6-Cl-pyridin-3-y 1 B-5155 H H H H H 0 H H 4-M e-5-Cl-pyridin-3-yl 1 B-5156 H H H H H 0 H H 4-M e-6-Cl-pyridin-3-y 1 B-5157 H H H H H 0 H H 2,4-(Me) 2-pyridin-3-yl 1 B-5158 H H H H H 0 H H 2,5-(Me) 2-pyridin-3-yl 1 B-5159 H H H H H 0 H H 2,6-(Me) 2-pyridin-3-yl 1 B-5160 H H H H H 0 H H 4,5-(Me) 2-pyridin-3-yl 1 B-5161 H H H H H 0 H H 4,6-(Me) 2-pyridin-3-yI 1 B-5162 H H H H H 0 H H 2-M e-4-0Me-pyridin-3-yI 1 B-5163 H H H H H 0 H H 2-MAe-5-0Me-pyridin-3-yI 1 B-5164 H H H H H 0 H H 2-MAe-6-0Me-pyridin-3-yI 1 B-5165 H H H H H 0 H H 4-MAe-2-0Me-pyridin-3-yI 1 B-5166 H H H H H 0 H H 4-M e-b-0Me-pyridin-3-yI 1
[0314]
[Table 189]
com pound R' R2 Rj R4 R A R6 R p B-5167 H H H H H 0 H H 4-MAe-6-0Me-pyridin-3-yI 1 B-5168 H H H H H 0 H H 2-CF 3-4-F-pyridin-3-y 1 B-5169 H H H H H 0 H H 2-0F 3-b-F-pyridin-3-yl 1 B-5170 H H H H H 0 H H 2-CF 3-6-F-pyridin-3-yl 1 B-5171 H H H H H 0 H H 4-0F 3-2-F-pyridin-3-y 1 B-5172 H H H H H 0 H H 4-CF 3-b--pyridin-3-yl 1 B-5173 H H H H H 0 H H 4-CF 3-6-F-pyridin-3-y 1 B-5174 H H H H H 0 H H 2-CF3 -4-MAe-pyridin-3-y 1 B-5175 H H H H H 0 H H 2-CF 3-5 -Me-pyridin-3-y 1 B-5176 H H H H H 0 H H 2-CF 3 -6-MAe-pyridin-3-yl 1 B-5177 H H H H H 0 H H 4-CF 3 -2-MAe-pyridin-3-yl 1 B-5178 H H H H H 0 H H 4-CF 3-5 -Me-pyridin-3-y 1 B-5179 H H H H H 0 H H 4-CF 3 -6-MAe-pyridin-3-yl 1 B-5180 H H H H H 0 H H 2-0Me-5-F-pyridh-3-y 1 B-5181 H H H H H 0 H H 2-0Me-6-F-pyridh-3-y 1 B-5182 H H H H H 0 H H 4-0Me-5-F-pyridh-3-y 1 B-5183 H H H H H 0 H H 4-0Me-6-F-pyridh-3-y 1 B-5184 H H H H H 0 H H 2-0Me-4-Cl-pyridh-3-yI 1 B-5185 H H H H H 0 H H 2-0Me-5-Cl-pyridh-3-yI 1 B-5186 H H H H H 0 H H 2-0Me-6-Cl-pyridh-3-yI 1 B-5187 H H H H H 0 H H 4-0Me-2-Cl-pyridh-3-yI 1 B-5188 H H H H H 0 H H 4-0Me-5-Cl-pyridh-3-yI 1 B-5189 H H H H H 0 H H 4-0Me-6-Cl-pyridh-3-yI 1 B-5190 H H H H H 0 H H 2-0Me-b-M e-pyridin-3-yI 1 B-5191 H H H H H 0 H H 2-0Me-6-M e-pyridin-3-yI 1 B-5192 H H H H H 0 H H 4-0Me-5-M e-pyridin-3-yI 1 B-5193 H H H H H 0 H H 4-0Me-6-M e-pyridin-3-yI 1 B-5194 H H H H H 0 H H 2,4-(0Me) 2 -pyridin-3-y 1 B-5195 H H H H H 0 H H 2,b-(OMe) 2 -pyridin-3-y 1 B-5196 H H H H H 0 H H 2,6-(0Me) 2 -pyridin-3-y 1 B-5197 H H H H H 0 H H 4,b-(0Me) 2 -pyridin-3-y 1 B-5198 H H H H H 0 H H 4,6-(0Me) 2 -pyridin-3-y 1 B-5199 H H H H H 0 H H pyridin-4-yI 1 B-5200 H H H H H 0 H H 2-F-pyridin-4-yI 1 B-5201 H H H H H 0 H H 3-F-pyridin-4-yI 1 B-5202 H H H H H 0 H H 2-Cl-pyridin-4-yI 1 B-5203 H H H H H 0 H H 3-Cl-pyridin-4-yI 1 B-5204 H H H H H 0 H H 2-M e-pyridin-4-y 1 B-5205 H H H H H 0 H H 3-M e-pyridin-4-y 1 B-5206 H H H H H 0 H H 2-GF 3-pyrdin-4-yl 1 B-5207 H H H H H 0 H H 3-CF 3-pyridin-4-yI 1 B-5208 H H H H H 0 H H 2-OMe-pyridin-4-yI 1 B-5209 H H H H H 0 H H 3-OMe-pyridin-4-yI 1 B-5210 H H H H H 0 H H 2,3-F 2-pyridin-4-yl 1 B-5211 H H H H H 0 H H 2,5-F 2-pyridin-4-y 1 B-5212 H H H H H 0 H H 2,6-F 2-pyrd in-4-yl 1 B-5213 H H H H H 0 H H 3,5-F 2-pyridin-4-y 1 B-5214 H H H H H 0 H H 2,3-Cl2-pyridin-4-yl 1 B-5215 H H H H H 0 H H 2,5-Cl2-pyridin-4-yl 1 B-5216 H H H H H 0 H H 2,6-Cl2-pyrdin-4-yl 1 B-5217 H H H H H 0 H H 3,5-Cl2-pyridin-4-yl 1 B-5218 H H H H H 0 H H 3-F-2-Cl-pyridh-4-yI 1 B-5219 H H H H H 0 H H 3-F-5-Cl-pyridh-4-yI 1 B-5220 H H H H H 0 H H 3-F-6-Cl-pyridh-4-yI 1 B-5221 H H H H H 0 H H 3-F-2-M e-pyridin-4-yI 1 B-5222 H H H H H 0 H H 3-F-5-M e-pyridin-4-yI 1 B-5223 H H H H H 0 H H 3-F-6-M e-pyridin-4-yI 1
[0315]
[Table 190]
com pound R' R2 Rj R4 R A R6 R p B-5224 H H H H H 0 H H 3-F-2-OMe-pyridh-4-yl 1 B-5225 H H H H H 0 H H 3-F-5-OMe-pyridh-4-yl 1 B-5226 H H H H H 0 H H 3-F-6-OMe-pyridh-4-yl 1 B-5227 H H H H H 0 H H 3-CI-2-F-pyridh-4-yI 1 B-5228 H H H H H 0 H H 3-CI-6-F-pyridh-4-yI 1 B-5229 H H H H H 0 H H 3-CI-2-Me-pyridin-4-y 1 B-5230 H H H H H 0 H H 3-CI-5-Me-pyridin-4-y 1 B-5231 H H H H H 0 H H 3-CI-6-Me-pyridin-4-y 1 B-5232 H H H H H 0 H H 3-MAe-2-F-pyridin-4-yI 1 B-5233 H H H H H 0 H H 3-MAe-6-F-pyridin-4-yI 1 B-5234 H H H H H 0 H H 3-Me-2-Cl-pyridin-4-y 1 B-5235 H H H H H 0 H H 3-Me-6-Cl-pyridin-4-y 1 B-5236 H H H H H 0 H H 2,3-(Me) 2-pyridin-4-yI 1 B-5237 H H H H H 0 H H 3,b-(M e) 2-pyridin-4-yI 1 B-5238 H H H H H 0 H H 3,6-(Me) 2-pyridin-4-yI 1 B-5239 H H H H H 0 H H 3-M e-2-0Me-pyridin-4-yI 1 B-5240 H H H H H 0 H H 3-MAe-5-0Me-pyridin-4-yI 1 B-5241 H H H H H 0 H H 3-MAe-6-0Me-pyridin-4-yI 1 B-5242 H H H H H 0 H H 3-0F 3-2-F-pyridin-4-yl 1 B-5243 H H H H H 0 H H 3-CF 3 -b-F-pyridin-4-yl 1 B-5244 H H H H H 0 H H 3-CF 3-6-F-pyridin-4-yI 1 B-5245 H H H H H 0 H H 3-CF 3-2-Me-pyridin-4-y 1 B-5246 H H H H H 0 H H 3-CF 3 -5-Me-pyridin-4-y 1 B-5247 H H H H H 0 H H 3-CF 3-6-Me-pyrdin-4-y 1 B-5248 H H H H H 0 H H 3-0Me-2-F-pyridh-4-y 1 B-5249 H H H H H 0 H H 3-0Me-6-F-pyridh-4-y 1 B-5250 H H H H H 0 H H 3-0Me-2-Cl-pyridh-4-yI 1 B-5251 H H H H H 0 H H 3-0Me-5-Cl-pyridh-4-yI 1 B-5252 H H H H H 0 H H 3-0Me-6-Cl-pyridh-4-yI 1 B-5253 H H H H H 0 H H 3-0Me-2-MAe-pyridin-4-yI 1 B-5254 H H H H H 0 H H 3-0Me-6-MAe-pyridin-4-yI 1 B-5255 H H H H H 0 H H 2,3-(0Me) 2 -pyridin-4-y 1 B-5256 H H H H H 0 H H 3,5-(0Me) 2 -pyridin-4-y 1 B-5257 H H H H H 0 H H 3,6-(0Me) 2 -pyridin-4-y 1 B-5258 H H H H H 0 H H pyril idin-2-yl 1 B-5259 H H H H H 0 H H pyril idin-4-yl 1 B-5260 H H H H H 0 H H 5-F-pyrim1 idin-4-yl 1 B-5261 H H H H H 0 H H 5-Me-pyrifl idh-4-yI 1 B-5262 H H H H H 0 H H b-0F 3 -pyrm idin-4-yl 1 B-5263 H H H H H 0 H H 5-0Me-pyril id h-4-yI 1 B-5264 H H H H H 0 H H pyrifl idin-5-yl 1 B-5265 H H H H H 0 H H 4-F-pyrim1 idin-5-yl 1 B-5266 H H H H H 0 H H 4-C[-pyril idin-5-yI 1 B-5267 H H H H H 0 H H 4-Me-pyrifl idh-5-yI 1 B-5268 H H H H H 0 H H 4-CF 3-pyril idin-5-yl 1 B-5269 H H H H H 0 H H 4-OMe-pyril id h-5-yI 1 B-5270 H H H H H 0 H H pyridazin-3-yl 1 B-5271 H H H H H 0 H H 4-F-pyridazh-3-yl 1 B-5272 H H H H H 0 H H 4-Cl-pyridazin-3-yl 1 B-5273 H H H H H 0 H H 4-M e-pyridazin-3-y 1 B-5274 H H H H H 0 H H 4-CF 3-pyridazh-3-yl 1 B-5275 H H H H H 0 H H 4-OMe-pyridazh-3-yl 1 B-5276 H H H H H 0 H H pyridazin-4-yl 1 B-5277 H H H H H 0 H H 3-F-pyridazh-4-yl 1 B-5278 H H H H H 0 H H 3-Cl-pyridazin-4-yl 1 B-5279 H H H H H 0 H H 3-Me-pyridazin-4-y 1 B-5280 H H H H H 0 H H 3-GF 3-pyridazn-4-yl 1
[0316]
[Table 191]
com pound R' R2 Rj R4 R A R6 R p B-5281 H H H H H 0 H H 3-OMe-pyridazh-4-yl 1 B-5282 H H H H H 0 H H 5-F-pyridazh-4-yl 1 B-5283 H H H H H 0 H H 5-CI-pyridazin-4-yl 1 B-5284 H H H H H 0 H H 5-Me-pyridazin-4-y 1 B-5285 H H H H H 0 H H b-GF 3-pyrdazn-4-yl 1 B-5286 H H H H H 0 H H 5-OMe-pyridazh-4-yl 1 B-5287 H H H H H 0 H H thiophen-2-yl 1 B-5288 H H H H H 0 H H 3-F-thiophen-2-yl 1 B-5289 H H H H H 0 H H 3-Cl-thiophen-2-yI 1 B-5290 H H H H H 0 H H 3-M e-thiophen-2-yI 1 B-5291 H H H H H 0 H H 3-G0%-thiophen-2-yl 1 B-5292 H H H H H 0 H H 3-0Me-thiophen-2-yI 1 B-5293 H H H H H 0 H H thiophen-3-yI 1 B-5294 H H H H H 0 H H 2-F-thiophen-3-y 1 B-5295 H H H H H 0 H H 2-Cl-thiophen-3-yI 1 B-5296 H H H H H 0 H H 2-M e-thiophen-3-yI 1 B-5297 H H H H H 0 H H 2-CF 3-thiophen-3-yI 1 B-5298 H H H H H 0 H H 2-0Me-thiophen-3-yI 1 B-5299 H H H H H 0 H H 4-F-thiophen-3-y 1 B-5300 H H H H H 0 H H 4-Cl-thiophen-3-yI 1 B-5301 H H H H H 0 H H 4-M e-thiophen-3-yI 1 B-5302 H H H H H 0 H H 4-CF 3-thiophen-3-yI 1 B-5303 H H H H H 0 H H 4-0Me-thiophen-3-yI 1 B-5304 H H H H H 0 H H thiazol-2-y 1 B-5305 H H H H H 0 H H thibzol-4-y 1 B-5306 H H H H H 0 H H 5-F-thiazol-4-yI 1 B-5307 H H H H H 0 H H 5-M e-thibzol-4-y 1 B-5308 H H H H H 0 H H b-GF 3 -thiazol-4-yl 1 B-5309 H H H H H 0 H H b-0Me-thibzol-4-yI 1 B-5310 H H H H H 0 H H thibzol-5-y 1 B-5311 H H H H H 0 H H 4-F-thiazol-5-yI 1 B-5312 H H H H H 0 H H 4-M e-thibzol-5-y 1 B-5313 H H H H H 0 H H 4-CF 3 -thiazol-5-y 1 B-5314 H H H H H 0 H H 4-0Me-thbzol-5-yI 1 B-5315 H H H H H 0 H H 1 H-pyrrol1-yI 1 B-5316 H H H H H 0 H H 2-F-1 H-pyrrol-1-yI 1 B-5317 H H H H H 0 H H 2-M e-1H -pyrrol-1-y 1 B-5318 H H H H H 0 H H 2-F 3-1 H-pyrrol-1-yl 1 B-5319 H H H H H 0 H H 2-0Me-1H-pyrrol-1-y 1 B-5320 H H H H H 0 H H 1 H-pyrrol-2-yI 1 B-5321 H H H H H 0 H H 1-M e-1 H-pyrrol-2-y 1 B-5322 H H H H H 0 H H 3-F-1H-pyrrol-2-yI 1 B-5323 H H H H H 0 H H 3-M e-1 H-pyrrol-2-y 1 B-5324 H H H H H 0 H H 3-F 3-1 H-pyrrol-2-yl 1 B-5325 H H H H H 0 H H 3-0Me-1H-pyrrol-2-yI 1 B-5326 H H H H H 0 H H 1-M e-3-F-1H-pyrrol-2-y 1 B-5327 H H H H H 0 H H 1,3-(Me) 2-1 H-pyrrol-2-y 1 B-5328 H H H H H 0 H H 1-Me-3-CF 3 -1 H-pyrrol-2-y 1 B-5329 H H H H H 0 H H 1-M e-3-0Me-1 H-pyrrol-2-yl 1 B-5330 H H H H H 0 H H 1 H-pyrrol-3-yI 1 B-5331 H H H H H 0 H H 1-M e-1 H-pyrrol-3-y 1 B-5332 H H H H H 0 H H 2-F-1H-pyrrol-3-yI 1 B-5333 H H H H H 0 H H 2-M e-1 H-pyrrol-3-y 1 B-5334 H H H H H 0 H H 2-CF 3-1 H-pyrrol-3-y 1 B-5335 H H H H H 0 H H 2-0Me-1H-pyrrol-3-yI 1 B-5336 H H H H H 0 H H 1-M e-2-F-1H-pyrrol-3-y 1 B-5337 H H H H H 0 H H 1,2-(Me) 2-1H -pyrrol-3-yI 1
[0317]
[Table 192]
com pound R' R2 Rj R4 R A R6 R p B-5338 H H H H H 0 H H 1-Me-2-CF 3 -1 H-pyrrol-3-yl 1 B-5339 H H H H H 0 H H 1-M e-2-OMe-1 H-pyrrol-3-yl 1 B-5340 H H H H H 0 H H 4-F-1H-pyrrol-3-yl 1 B-5341 H H H H H 0 H H 4-M e-1H-pyrrol-3-yl 1 B-5342 H H H H H 0 H H 4-0F 3 -1H-pyrrol-3-yl 1 B-5343 H H H H H 0 H H 4-OMe-1H-pyrrol-3-yl 1 B-5344 H H H H H 0 H H 1-M e-4-F-1 H-pyrrol-3-yl 1 B-5345 H H H H H 0 H H 1,4-(Me) 2-1H-pyrrol-3-yI 1 B-5346 H H H H H 0 H H 1-Me-4-CF 3 -1H-pyrrol-3-yl 1 B-5347 H H H H H 0 H H 1-M e-4-OMe-1 H-pyrrol-3-yl 1 B-5348 H H H H H 0 H H 1 H-pyrazol-yl 1 B-5349 H H H H H 0 H H 5-F-1 H-pyrazol-yl 1 B-5350 H H H H H 0 H H 5-CI-1H-pyrazol-y 1 B-5351 H H H H H 0 H H 5-M e-1H-pyrazol-yl 1 B-5352 H H H H H 0 H H 5-CF 3 -1H-pyrazol-yl 1 B-5353 H H H H H 0 H H 5-OMe-1H-pyrazol-yI 1 B-5354 H H H H H 0 H H 1 H-pyrazol-3-yl 1 B-5355 H H H H H 0 H H 1-M e-1H-pyrazol-3-yl 1 B-5356 H H H H H 0 H H 4-F-1 H-pyrazol-3-yl 1 B-5357 H H H H H 0 H H 4-C-1H -pyrazol-3-yI 1 B-5358 H H H H H 0 H H 4-M e-1H-pyrazol-3-yl 1 B-5359 H H H H H 0 H H 4-CF-i1H-pyrazol-3-yl 1 B-5360 H H H H H 0 H H 4-OMe-1H-pyrazol-3-yl 1 B-5361 H H H H H 0 H H 1-M e-4-F-1 H-pyrazol-3-yl 1 B-5362 H H H H H 0 H H 1-Me-4-C-1H -pyrazol-3-yl 1 B-5363 H H H H H 0 H H 1,4-(Me) 2 -1H-pyrazol-3-yl 1 B-5364 H H H H H 0 H H 1-Me-4-CF 3 -1 H-pyrazol-3-yI 1 B-5365 H H H H H 0 H H 1-M e-4-0Me-1H-pyrazol-3-yI 1 B-5366 H H H H H 0 H H 1H-pyrazol-4-y 1 B-5367 H H H H H 0 H H 1-M e-1 H-pyrazol-4-yI 1 B-5368 H H H H H 0 H H 3-F-1 H-pyrazol-4-yI 1 B-5369 H H H H H 0 H H 3-C-1HH-pyrazol-4-yI 1 B-5370 H H H H H 0 H H 3-M e-1 H-pyrazol-4-y 1 B-5371 H H H H H 0 H H 3-CF-i1H-pyrazol-4-y 1 B-5372 H H H H H 0 H H 3-0Me-1 H-pyrazol-4-yI 1 B-5373 H H H H H 0 H H 1-Me-3-F-1 H-pyrazol-4-y 1 B-5374 H H H H H 0 H H 1-Me-3-C-1H -pyrazol-4-y 1 B-5375 H H H H H 0 H H 1,3-(Me) 2 -1 H-pyrazoI-4-yI 1 B-5376 H H H H H 0 H H 1-M e-3-0F 3 -1 H-pyrazol-4-yl 1 B-5377 H H H H H 0 H H 1 -M e-3-0Me-1 H-pyrazol-4-y 1 B-5378 H H H H H 0 H H 5-F-1 H-pyrazol-4-y 1 B-5379 H H H H H 0 H H 5-C-1HH-pyrazol-4-yI 1 B-5380 H H H H H 0 H H 5-M e-1 H-pyrazol-4-y 1 B-5381 H H H H H 0 H H 5-C-F1H-pyrazol-4-yl 1 B-5382 H H H H H 0 H H 5-0Me-1 H-pyrazol-4-yI 1 B-5383 H H H H H 0 H H 1-Me-5-F-1 H-pyrazol-4-y 1 B-5384 H H H H H 0 H H 1-Me-5-C-1HH-pyrazol-4-y 1 B-5385 H H H H H 0 H H 1,5-(Me) 2 -1 H-pyrazol-4-yI 1 B-5386 H H H H H 0 H H 1-Me-5-CF 3 -1 H-pyrazol-4-y 1 B-5387 H H H H H 0 H H 1 -M e-5-0Me-1 H-pyrazol-4-y 1 B-5388 H H H H H 0 H H 1 H-pyrazol-5-y 1 B-5389 H H H H H 0 H H 1 -M e-1 H-pyrazol-5-yI 1 B-5390 H H H H H 0 H H 4-F-1 H-pyrazol-5-yl 1 B-5391 H H H H H 0 H H 4-C-1HH-pyrazol-5-yI 1 B-5392 H H H H H 0 H H 4-M e-1 H-pyrazol-5-y 1 B-5393 H H H H H 0 H H 4-C-i1H-pyrazol-5-y 1 B-5394 H H H H H 0 H H 4-0Me-1H -pyrazol-5-y 1
[0318]
[Table 193]
com pound R' R2 Rj R4 R A R6 R p B-5395 H H H H H 0 H H 1-Me-4-F-1H-pyrazol-5-yl 1 B-5396 H H H H H 0 H H 1-Me-4-C-H-pyrazol-5-yl 1 B-5397 H H H H H 0 H H 1,4-(Me) 2-1iH-pyrazol-b-y 1 B-5398 H H H H H 0 H H 1-M e-4-GF 3 -1H-pyrazol-b-yl 1 B-5399 H H H H H 0 H H 1-MAe-4-0Me-1H-pyrazol-b-y 1 B-5400 H H H H H 0 H H furan-2-yI 1 B-5401 H H H H H 0 H H 3-F-fu ran-2-yI 1 B-5402 H H H H H 0 H H 3-M e-furan-2-yI 1 B-5403 H H H H H 0 H H 3-CF3-furan-2-yI 1 B-5404 H H H H H 0 H H 3-0Me-fu ran-2-y 1 B-5405 H H H H H 0 H H furan-3-yI 1 B-5406 H H H H H 0 H H 2-F-fu ran-3-yI 1 B-5407 H H H H H 0 H H 2-M e-furan-3-yI 1 B-5408 H H H H H 0 H H 2-CF3 -turan-3-yl 1 B-5409 H H H H H 0 H H 2-0Me-fu ran-3-y 1 B-5410 H H H H H 0 H H 4-F-fu ran-3-yI 1 B-5411 H H H H H 0 H H 4-M e-furan-3-yI 1 B-5412 H H H H H 0 H H 4-CF 3-turan-3-yl 1 B-5413 H H H H H 0 H H 4-0Me-furan-3-y 1 B-5414 H H H H H 0 H H isoxazol-3-yI 1 B-5415 H H H H H 0 H H 4-F-isoxazol-3-yI 1 B-5416 H H H H H 0 H H 4-M e-isoxazol-3-y 1 B-5417 H H H H H 0 H H 4-CF 3 -isoxazol-3-yI 1 B-5418 H H H H H 0 H H 4-0Me-isoxazol-3-yI 1 B-5419 H H H H H 0 H H isoxazol-4-yI 1 B-5420 H H H H H 0 H H 5-F-isoxazol-4-yI 1 B-5421 H H H H H 0 H H 5-M e-isoxazol-4-y 1 B-5422 H H H H H 0 H H b-GF 3-soxazol-4-yl 1 B-5423 H H H H H 0 H H b-OMe-isoxazol-4-yI 1 B-5424 H H H H H 0 H H isoxazol-5-yI 1 B-5425 H H H H H 0 H H 4-F-isoxazol-5-yI 1 B-5426 H H H H H 0 H H 4-Me-isoxazol-5-y 1 B-5427 H H H H H 0 H H 4-CF 3 -isoxazol-5-yI 1 B-5428 H H H H H 0 H H 4-0Me-isoxazol-5-yI 1 B-5429 H H H H H 0 H H 1H -1,2,3-trbzol-1-y 1 B-5430 H H H H H 0 H H 5-F-1H -1,2,3-triazo-1-y 1 B-5431 H H H H H 0 H H 5-Me-1H-1,2,3-triazol-1-y 1 B-5432 H H H H H 0 H H 5-0%-1H-1,2,3-triazol-1-y 1 B-5433 H H H H H 0 H H 5-0Me-1H-1,2,3-triazol-1-y 1 B-5434 H H H H H 0 H H 1H -1,2,3-trbzol-4-y 1 B-5435 H H H H H 0 H H 5-F-1H-12,3-triazo-4-y 1 B-5436 H H H H H 0 H H 5-Me-1H-1,2,3-triazol-4-y 1 B-5437 H H H H H 0 H H 5-CF 3-1H-1,2,3-triazol-4-y 1 B-5438 H H H H H 0 H H 5-0Me-1H-12,3-triazol-4-y 1 B-5439 H H H H H 0 H H 1H -1,2,3-trbzol-5-y 1 B-5440 H H H H H 0 H H 4-F-1H-12,3-triazol-5-y 1 B-5441 H H H H H 0 H H 4-Me-1H-1,2,3-triazol-5-y 1 B-5442 H H H H H 0 H H 4-CF 3-1H-1,2,3-triazol-b-y 1 B-5443 H H H H H 0 H H 4-0Me-1H-12,3-triazol-b-y 1 B-5444 H H H H H 0 H H 1H-1,2,4-trbzol-1-y 1 B-5445 H H H H H 0 H H 5-Me-1H-1,2,4-triazol-1-y 1 B-5446 H H H H H 0 H H 5-F-1H-12,4-triazo-1-y 1 B-5447 H H H H H 0 H H 5-CF 3-1H-1,2,4-triazol-1-y 1 B-5448 H H H H H 0 H H 5-0Me-1-1,2,4-triazol-1-y 1 B-5449 H H H H H 0 H H 1H-1,2,4-tribzol-3-y 1 B-5450 H H H H H 0 H H 1-MAe-1H-1,2,4-triazol-3-y 1 B-5451 H H H H H 0 H H 1H-1,2,4-trbzol--y 1
[0319]
[Table 194] cornpound mR' R2 RTR A R6 R/ o B-5452 H H H H H 0 H H 1-M e-1M-1,2,4-triazokb5-yI 1 B-5453 H H H H H 0 H H 3,5-(M e) 2 L o A -yI1 1 B-5454 H H H H H 0 H H 3,5-(Et)2 -iSoxaZo[-4-yI1 1 B-5455 H H H H H 0 H H 1,3,5-(M e) 3 -1 H -pyrazo[-4-yI1 1 B-5456 H H H H H 0 H H qu inolh-4-yI1 1 B-5457 H H H H H 0 H H Loqu ino lin-4-yI1 1 B-5458 H H H H H 0 H H 3,6-(M e) 2 -pyriazin-4-yI1 1 B-5459 IH IH IH IH IH 10 1H IH 2,4-(0 M e) 2 -pyrin id in-5-y I1
[0320]
[Table 195]
3 2
4 R /\N (Os R1 R 5 1 cornpound R~ ~~ RdTz R bmP -0001 H H H H H H 0 -0002 H H H H H 2-F0 -0003 H H H H H 3-F 0 C-0004 H H H H H 4-F 0 -0005 H H H H H 2-C01 0 -0006 H H H H H 3-C01 0 -0007 H H H H H 4-C01 0 -0008 H H H H H 2-B r0 -0009 H H H H H 3-B r 0 -00 10 H H H H H 4-B r 0 -0011I H H H H H 2-1 0 -001 2 H H H H H 3-1 0 -001 3 H H H H H 4-1 -0014 H H H H H 2-O H0 -00 15 H H H H H 3-O H 0 -001 6 H H H H H 4-O H 0 -00 17 H H H H H 2-SH0 -00 18 H H H H H 3-SH 0 -00 19 H H H H H 4-SH0 ~~O7W2- WR T R R24e 0 C-0021 H TH H H -F4 3 e10 0 -0 0 22 H H H H H 4-M e0 0-0023 H H H H H 2-Et 0 0-0024 H H H H H 3-Et 0 0-0025 H H H H H 4-Et 0 0-0026 H H H H H 2-Pr 0 0-0027 H H H H H 3-Pr 0 0-0028 H H H H H 4-P r 0 0-00 29 H H H H H 2-i-Pr 0 0-0030 H H H H H 3-i-Pr 0 0-00 31 H H H H H 4-i-Pr 0 -uTn - W-F- R-F T-F RF R 2-B u0 -77OW W-F -- F- TF RF TH 3 -Bu 0 0-0034 H H H H H 4 -B u 0 0 -0 0 35 H H H H H 2 -s -Bu 0 0 -0 0 36 H H H H H 3 -s -Bu 0 0 -0 0 37 H H H H H 4-s-B u 0 0-00 38 H H H H H 2-/-B u 07 -7:W 7TjR 3-i-B u0 0-0040 H H H H H 4-/-B u 0 0-0041 H H H H H 2 -t-B u0 0-0042 H H H H H 3 -t-B u 0 0-0043 H H H H H 4-t-B u 0 0-0044 H H H H H 2-O F, 0-0045 H H H H H 3-O F 3 0 0-0046 H H H H H 4-OCF 3 0 0-0047 H H H H H 2-CH F 2 0 0-0048 H H H H H 3-OH F 2 0 0-0049 H H H H H 4-OH F 2 0 0-0050 H H H H H 2-OH F 0 0-0051 H H H H H 3-OH F 0
[0321]
[Table 196]
cornpound R' R~ 2 ~ T R B4Rb(%p C-0052 H H H H H 4-CH 2F 0 -0053 H H H H H 2-0F 20 1 0 -0054 H H H H H 3-0F 20 1 0 -0055 H H H H H 4-C0F 20 1 0 -00566 H H H H H 2-C F(C F 3 ) 2 0 -006]7 H H H H H 3-C F (0F3) 2 0 -0068 H H H H H 4-C F (0F3) 2 0 -006 9 H H H H H 2 -cyc lop ropyl1 0 -00 60 H H H H H 3 -cyc lop rop y 0 -00 61 H H H H H 4 -cyo lop ropyI1 0 -00 62 H H H H H 2 -cycobu tyl1 0 -00 63 H H H H H 3 -cy o butyl1 0 -00 64 H H H H H 4-cyo bu tyl1 0 -00 66 H H H H H 2 -oycopentyI1 0 -00 66 H H H H H 3 -oycopentyI1 0 -006]7 H H H H H 4-oy op entyI1 0 -00 68 H H H H H 2-(oycopropyhiethyl) 0 -0069 H H H H H 3-(oycopropyhiethyl) 0 -0070 H H H H H 4-(oycopropyhiethyl) 0 -0071 H H H H H 2-(oy obutyhinethyl) 0 -0072 H H H H H 3-(oy obbutyhinethy) 0 -0073 H H H H H 4-(oy obbutyhinethy) 0 -0074 H H H H H 2-(oycopentyhiethy D 0 -0076 H H H H H 3-(oycopentyhiethy D 0 -0076 H H H H H 4-(oycopentyhinethy D 0 -0077 H H H H H 2-(oy opropy lethylD 0 -0078 H H H H H 3-(oy opropy lethy D 0 -0079 H H H H H 4-(oy opropy lethy D 0 -0080 H H H H H 2 -(2,2-Adifijorocycblp ropy D 0 -0081 H H H H H 3 -(2,2-Adifluorooy op ropy D 0 -0082 H H H H H 4-(2,2-d ifluorocycblp ropy D 0 -0083 H H H H H 2 -(2,2-Adch brocyolop ropy D 0 -0084 H H H H H 3 -(2,2-Adch brocyolop ropy D 0 -0086 H H H H H 4-(2,2-dkch brocyolop ropy D 0 -0 0 86 H H H H H 2 -e the ny1 0 -0 0 87 H H H H H 3 -e the nyl 0 -0088 H H H H H 4 -e the ny1 0 -0 0 89 H H H H H 2-a ll'1 0 -0090 H H H H H 3-a llbI0 -0091 H H H H H 4-a llyI 07 -0092 H H H H H 2-(prop-1 -en--y D0 -0093 H H H H H 3-(prop-1 -en- -yD 0 -0094 H H H H H 4-(prop-1 -en-1 -yD 0 -0096 H H H H H 2-(trifluoroethenyD 0 -0096 H H H H H 3-(trifluoroetheny D 0 -0097 H H H H H 4-(trifluoroetheny D 0 -0098 H H H H H 2-(2,2-d ichloroetheny) 0 -0099 H H H H H 3-(2,2-d ichloroetheny) 0 -01 00 H H H H H 4-(2,2-d ichloroetheny) 0 -01 01 H H H H H 2-ethynyl1 0 -01 02 H H H H H 3-ethynyl1 0 -01 03 H H H H H 4-ethynyl 0 -01 04 H H H H H 2-01-propyn-1 -yD 0 -01 06 H H H H H 3-01-propyn-1 -yD 0 -01 06 H H H H H 4-01-propyn-1 -yD 0 -01 07 H H H H H 2-(2-propyn-1 -y D 0
[0322]
[Table 197]
cornpound R' R~ 2 R R4 Rb(%P C-0108 H H H H H 3-(2-propyn-1-yD 0 -0109 H H H H H 4-(2-propyn-1-yD 0 -01 10 H H H H H 2-(2-oyo bp ropy lethyny D 0 -01 11 H H H H H 3-(2-oyo bp ropy lethyny D 0 -01 12 H H H H H 4-(2-oyo bp ropy lethynyD 0 -01 13 H H H H H 2-(2-oh broethyny D 0 -01 14 H H H H H 3-(2-oh broethyny D 0 -01 15 H H H H H 4-(2-oh broethyny D 0 -01 16 H H H H H 2-(2-bronoethyny D 0 -01 17 H H H H H 3-(2-bronoethyny D 0 -01 18 H H H H H 4-(2-bronoethyny D 0 -01 19 H H H H H 2-OM e0 -01 20 H H H H H 3-OM e 0 C-01 21 H H H H H 4-OM e 0 -01 22 H H H H H 2-0 Et0 -01 23 H H H H H 3-0 Et 0 -01 24 H H H H H 4-0 Et 0 -01 25 H H H H H 2-0OPr 0 -01 26 H H H H H 3-0OPr 0 -01 27 H H H H H 4-0OPr 0 -01 28 H H H H H 2 -0(i-Pr)0 -012 9 H H H H H 3 -0(i-P r) 0 -013 0 H H H H H 4 -0(i-P r) 0 -013 1 H H H H H 2 -0 Bu 0 -013 2 H H H H H 3 -0 Bu 0 -013 3 H H H H H 4 -0 Bu 0 -013 4 H H H H H 2-0 (s-E u) 0 -01365 H H H H H 3-0 (s-E u) 0 -013 6 H H H H H 4-0 (s-E u) 0 -013]7 H H H H H 2-0(/-B u) 0 -013 8 H H H H H 3-0(/-B u) 0 -013 9 H H H H H 4-0(/-E u) 0 -0 140 H H H H H 2-0 (t-Eu) 0 -0 141 H H H H H 3-0 (t-Eu) 0 -0 142 H H H H H 4-0 (t-Eu) 0 -0 143 H H H H H 2-00CF 3 0 -0 144 H H H H H 3-0 CF 3 0 -0 146 H H H H H 4-00CF 3 0 -0 146 H H H H H 2-0OCHF 2 0 -01 4] H H H H H 3-OCH F 2 0 -01 48 H H H H H 4-OCH F 2 0 -01 49 H H H H H 2-0CH 20F 3 0 -01650 H H H H H 3-0 CH 2 CF 3 0
-01651 H H H H H 4-0 CH 2 CF 3 0 -01652 H H H H H 2-(oyo lopropy bxy) 0 -01653 H H H H H 3-(oyo lopropy bxy) 07 -01654 H H H H H 4-(oyo lopropy bxy) 0 -01665 H H H H H 2-(oyobbuty bxy) 0 -01656 H H H H H 3-(oy obuty bxy) 0 -016]7 H H H H H 4-(oy obuty bxy) 0 -01658 H H H H H 2-(oyolopentyblxy) 0 -01659 H H H H H 3-(oyolopentyblxy) 0 -01 60 H H H H H 4-(oyolopentyblxy) 0 -01 61 H H H H H 2-((2,2-dkichbrooyopropy Doxy) 0 -01 62 H H H H H 3-((2,2-dkichblrooycopropy Doxy) 0 -01 63 H H H H H 4-((2,2-dkichblrooycopropy Doxy) 0
[0323]
[Table 198]
cornpound R' R 2 j R4 Rb(%P -01 64 H H H H H 2-(oycopropyhiethoxy) 0 -01 65 H H H H H 3-(oycopropyhiethoxy) 0 -01 66 H H H H H 4-(oycopropyhiethoxy) 0 -01 67 H H H H H 2-((2,2-d iflu orooy op ropy )mnethoxy) 0 -01 68 H H H H H 3-((2-,2-diflu orooy op ropyI)mnethoxy) 0 -01 69 H H H H H 4-((2,2-d flu orooy op ropy )mnethoxy) 0 -01 70 H H H H H 2-(oxiran-2-y D 0 -01 71 H H H H H 3-(oxiran-2-y D 0 -01 72 H H H H H 4-(oxiran-2-y D0 -01 73 H H H H H 2-(oxiran-2-yhiethyl) 0 -01 74 H H H H H 3-(oxiran-2-yhiethyl) 0 -01 75 H H H H H 4-(oxiran-2-yhiethyl) 0 -01 76 H H H H H 2-SIMe 0 -01]]7 H H H H H 3-SIMe 0 -01 78 H H H H H 4-SIMe0 -01 79 H H H H H 2-SEt 0 -01 80 H H H H H 3-SEt 0 -01 81 H H H H H 4-SEt 0 -01 82 H H H H H 2-S(=0)Me 0 -01 83 H H H H H 3-S(=0)Me 0 -01 84 H H H H H 4-S(=0)Me0 -01 85 H H H H H 2-S=0 ) 2 M e 0 -01 86 H H H H H 3-S=0 ) 2 M e 0 -01 87 H H H H H 4-S(=0) 2 M e 0 -01 88 H H H H H 2-SC F 3 0 -01 89 H H H H H 3-SC F 3 0 -01 90 H H H H H 4-SOPF3 0 -01 91 H H H H H 2-S=0 )0F3 0 -01 92 H H H H H 3-S=0 )0F3 0 -01 93 H H H H H 4-S=0 )0F3 0 -01 94 H H H H H 2-S=0 ) 2 C0F 3 0 -01 95 H H H H H 3-S(=U) 2C F 3 0 -01 96 H H H H H 4-S=0 ) 20CF 3 0 -01 97 H H H H H 2-SOF (0F3 ) 2 0 -01 98 H H H H H 3-SOF (0F3 ) 2 0 -01 99 H H H H H 4-SOF (0F3) 2 0 -0200 H H H H H 2-(oyobp ropy lthbi) 0 -0201 H H H H H 3-(oyobp ropy lthbi) 0 -0202 H H H H H 4-(oyobp ropy lthbi) 0 -0203 H H H H H 2-(oyobpropysufin yD 0 -0204 H H H H H 3-(oyobpropysufin yD 0 -0205 H H H H H 4-(oyobpropysufin yD 0 -0206 H H H H H 2-(oyo lopropybsu fony D 0 -0207 H H H H H 3 -(-yolop ropysu fony D 0 -0208 H H H H H 4-(oyolopropybsu fony D 0 -0209 H H H H H 2-((oyobpropyhinethy DThio) 0 -02 10 H H H H H 3-((oy op ropyhinethy Dth io) 0 -02 11 H H H H H 4-((oy op ropyhinethy Dth io) 0 -02 12 H H H H H 2-((oy op ropyhiethy Dsuf iny D 0 -02 13 H H H H H 3-((oy op ropyhiethy Dsuf iny D 0 -02 14 H H H H H 4-((oy op ropyhiethy Dsuf iny D 0 -02 15 H H H H H 2-((oycopropyhiethyDsu fony D 0 -02 16 H H H H H 3-((oycopropyhiethyDsu fony D 0 -02 17 H H H H H 4-((oy op ropyhiethy Dsu fony D 0 -02 18 H H H H H 2-(((2,2-d if borocycblp ropy )mnethy DTh 0 -02 19 H H H H H 3-(((2,2-d if borocycblp ropy )mnethy Dth io 0
[0324]
[Table 199]
com pound R' R2 Rj R4 Rb R p C-0220 H H H H H 4-(((2,2-d ifiorocycbpropyDm ethyDthio) 0 0-0221 H H H H H 2-(((2,2-difluorocycbpropyDm ethyDsulfinyD 0 0-0222 H H H H H 3-(((2,2-difluorocycbpropyDm ethyDsulfinyD 0 0-0223 H H H H H 4-(((2,2-difluorocycbpropyDm ethyDsulfinyD 0 0-0224 H H H H H 2-(((2,2-difluorocycbpropy)m ethyDsulfonyD 0 0-0225 H H H H H 3-(((2,2-difluorocycbpropy)mrethyDsulfonyD 0 0-0226 H H H H H 4-(((2,2-difluorocycbpropy)mrethyDsulfonyD 0 0-0227 H H H H H 2-C(=0)Me 0 -0228 H H H H H 3-C(=0)Me 0 -0229 H H H H H 4-C(=0)Me 0 -0230 H H H H H 2-C0(=)Et 0 -0231 H H H H H 3-C0(=)Et 0 -0232 H H H H H 4-C0(=)Et 0 -0233 H H H H H 2-C0(=)CF 3 0 -0234 H H H H H 3-C0(=)CF 3 0 -0235 H H H H H 4-C0(=)CF 3 0 -0236 H H H H H 2-C(=0)0Me 0 -0237 H H H H H 3-C(=0)0Me 0 -0238 H H H H H 4-C(=0)0Me 0 -0239 H H H H H 2-C(=0)0Et 0 -0240 H H H H H 3-C(=0)0Et 0 -0241 H H H H H 4-C(=0)0Et 0 -0242 H H H H H 2-C(=0)NH 2 0 -0243 H H H H H 3-C(=0)NH 2 0 -0244 H H H H H 4-C(=0)NH 2 0 -0245 H H H H H 2-C(=0)NHMe 0 -0246 H H H H H 3-C0(=)NHMe 0 -0247 H H H H H 4-C(=0)NHMe 0 -0248 H H H H H 2-C(=0)NMe 2 0 -0249 H H H H H 3-C(=0)NMe 2 0 -0250 H H H H H 4-C0(=)NMe 2 0 -0251 H H H H H 2-CH 2C0(=)CH 3 0 -0252 H H H H H 3-CH 2C0(=)CH 3 0 -0253 H H H H H 4-CH 2C0(=)CH 3 0 -0254 H H H H H 2-CH 2C0(=)CF3 0 -0255 H H H H H 3-CH 2C0(=)CF3 0 -0256 H H H H H 4-CH 2C(=0)CF 3 0 -0257 H H H H H 2-CH 2C0(=)0CH 3 0 -0258 H H H H H 3-CH 2C0(=)0CH 3 0 -0259 H H H H H 4-CH 2C0(=)0CH 3 0 -0260 H H H H H 2-CH20H 0 -0261 H H H H H 3-CH20H 0 -0262 H H H H H 4-CH20H 0 -0263 H H H H H 2-CH20CH 3 0 -0264 H H H H H 3-CH 20CH 3 0 -0265 H H H H H 4-CH 20CH3 0 -0266 H H H H H 2-CH 20CH 2CH 3 0 -0267 H H H H H 3-CH 20CH 2CH 3 0 -0268 H H H H H 4-CH 20CH 2CH 3 0 -0269 H H H H H 2-CH(CH 3 )0CH 3 0 -0270 H H H H H 3-CH(CH 3 )0CH 3 0 -0271 H H H H H 4-CH (CH 3 )0CH 3 0 -0272 H H H H H 2-CH 2CH 20CH 3 0 -0273 H H H H H 3-CH 2CH 20CH 3 0 -0274 H H H H H 4-CH 2CH 20 CH 3 0 -0275 H H H H H 2-CH 200F3 0
[0325]
[Table 200]
com pound R' R2 Rj R4 Rb R p C-0276 H H H H H 3-CH 200F, 0 0-0277 H H H H H 4-CH 200F3 0 0-0278 H H H H H 2-CF 2 0CH 3 0 0-0279 H H H H H 3-CF 2 0CH 3 0 0-0280 H H H H H 4-0F2 0CH 3 0 0-0281 H H H H H 2-CF 2CF 200F3 0 0-0282 H H H H H 3-CF 2CF 200F3 0 0-0283 H H H H H 4-CF 2CF 200F3 0 0-0284 H H H H H 2-00(=0)CH 3 0 0-0285 H H H H H 3-00(=0)CH 3 0 0-0286 H H H H H 4-00(=0)CH 3 0 0-0287 H H H H H 2-00(=0)CF 3 0 0-0288 H H H H H 3-00(=0)CF 3 0 0-0289 H H H H H 4-00(=0)CF 3 0 0-0290 H H H H H 2-00(=0)NH 2 0 0-0291 H H H H H 3-00(=0)NH 2 0 0-0292 H H H H H 4-00(=0)NH 2 0 0-0293 H H H H H 2-00(=0)NHCH 3 0 0-0294 H H H H H 3-00(=0)NHCH 3 0 0-0295 H H H H H 4-00(=0)NHCH 3 0 0-0296 H H H H H 2-00(=0)N(CH 3) 2 0 0-0297 H H H H H 3-00(=0)N(CH 3) 2 0 0-0298 H H H H H 4-00 (=0)N (CH 3) 2 0 0-0299 H H H H H 2-CH 200(=0)NH 2 0 0-0300 H H H H H 3-CH 20C(=0)NH 2 0 0-0301 H H H H H 4-CH20C(=0)NH2 0 0-0302 H H H H H 2-CH 200(=0)NHCH 3 0 0-0303 H H H H H 3-CH 200(=0)NHCH 3 0 0-0304 H H H H H 4-CH 200 (=0)NHCH 3 0 0-0305 H H H H H 2-CH 2 00(=0)N(CH 3) 2 0 0-0306 H H H H H 3-CH 2 00(=0)N(CH 3) 2 0 0-0307 H H H H H 4-OH 2 0C(=0)N(CH 3) 2 0 0-0308 H H H H H 2-00(=0)0CH3 0 -0309 H H H H H 3-00(=0)0CH 3 0 -0310 H H H H H 4-00(=0)0CH 3 0 -0311 H H H H H 2-CH 2 00 (=0)0CH 3 0 -0312 H H H H H 3-OH 2 0C (=0)0CH 3 0 -0313 H H H H H 4-CH 2 00 (=0)0CH 3 0 -0314 H H H H H 2-CH 200(=0)CH3 0 -0315 H H H H H 3-CH 200(=0)CH 3 0 -0316 H H H H H 4-CH 200(=0)CH 3 0 -0317 H H H H H 2-0S(=0) 2CH 3 0 -0318 H H H H H 3-0S(=0) 2CH3 0 -0319 H H H H H 4-0S(=0) 2CH 3 0 -0320 H H H H H 2-CH 2 SCH 3 0 -0321 H H H H H 3-CH 2 SCH 3 0 -0322 H H H H H 4-CH 2 SCH 3 0 -0323 H H H H H 2-CH 2S(=0)CH3 0 -0324 H H H H H 3-CH 2S(=0)CH 3 0 -0325 H H H H H 4-CH 2S(=0)CH 3 0 -0326 H H H H H 2-CH 2S(=0) 2CH 3 0 -0327 H H H H H 3-CH 2S(=0) 2CH 3 0 -0328 H H H H H 4-CH 2S(= 0) 2CH 3 0 -0329 H H H H H 2-CH 2SCF3 0 -0330 H H H H H 3-CH 2SCF3 0 -0331 H H H H H 4-CH 2SCF3 0
[0326]
[Table 201]
com pound R' R2 Rj R4 Rb R p -0332 H H H H H 2-CH 2S(=O)CF 0 -0333 H H H H H 3-CH 2S(=O)CF 3 0 -0334 H H H H H 4-CH 2S(=O)CF 3 0 -0335 H H H H H 2-CH 2S(=0) 2CF3 0 -0336 H H H H H 3-CH 2 S(=0 2 CF 3 0 -0337 H H H H H 4-CH 2S(=0) 2CF3 0 -0338 H H H H H 2-phenyl 0 -0339 H H H H H 3-phenyl 0 -0340 H H H H H 4-phenyl 0 -0341 H H H H H 2-(phenybxy) 0 -0342 H H H H H 3-(phenybxy) 0 -0343 H H H H H 4-(phenybxy) 0 -0344 H H H H H 2-benzy 1 0 -0345 H H H H H 3-benzy 1 0 -0346 H H H H H 4-benzy 1 0 -0347 H H H H H 2-(benzy bxy) 0 -0348 H H H H H 3-(benzy bxy) 0 -0349 H H H H H 4-(benzy bxy) 0 -0350 H H H H H 2-((2-fluorobenzyDoxy) 0 -0351 H H H H H 3-((2-fluorobenzyDoxy) 0 -0352 H H H H H 4-((2-fluorobenzyDoxy) 0 -0353 H H H H H 2-((3-fluorobenzyDoxy) 0 -0354 H H H H H 3-((3-fluorobenzyDoxy) 0 -0355 H H H H H 4-((3-fluorobenzyDoxy) 0 -0356 H H H H H 2-((4-fluorobenzyDoxy) 0 -0357 H H H H H 3-((4-fluorobenzyDoxy) 0 -0358 H H H H H 4-((4-fluorobenzyDoxy) 0 -0359 H H H H H 2-((2-chbrobenzyDoxy) 0 -0360 H H H H H 3-((2-chbrobenzyDoxy) 0 -0361 H H H H H 4-((2-chbrobenzyDoxy) 0 -0362 H H H H H 2-((3-chbrobenzyDoxy) 0 -0363 H H H H H 3-((3-chbrobenzyDoxy) 0 -0364 H H H H H 4-((3-chbrobenzyDoxy) 0 -0365 H H H H H 2-((4-chbrobenzyDoxy) 0 -0366 H H H H H 3-((4-chbrobenzyDoxy) 0 -0367 H H H H H 4-((4-chbrobenzyDoxy) 0 -0368 H H H H H 2-((2--m ethy lbenzy Doxy) 0 -0369 H H H H H 3-((2-m ethylbenzyDoxy) 0 -0370 H H H H H 4-((2-m ethylbenzyDoxy) 0 -0371 H H H H H 2-((3-m ethylbenzyDoxy) 0 -0372 H H H H H 3-((3-m ethylbenzyDoxy) 0 -0373 H H H H H 4-((3-m ethylbenzyDoxy) 0 -0374 H H H H H 2-((4-m ethylbenzyDoxy) 0 -0375 H H H H H 3-((4-m ethylbenzyDoxy) 0 -0376 H H H H H 4-((4-m ethylbenzyDoxy) 0 -0377 H H H H H 2-((2-(trifluorom ethyDbenzyDoxy) 0 -0378 H H H H H 3-((2-(trifluorom ethyDbenzyDoxy) 0 -0379 H H H H H 4-((2-(trifluorom ethyDbenzyDoxy) 0 -0380 H H H H H 2-((3-(trifluorom ethyDbenzyDoxy) 0 -0381 H H H H H 3-((3-(trifluorom ethyDbenzyDoxy) 0 -0382 H H H H H 4-((3-(trifluorom ethyDbenzyDoxy) 0 -0383 H H H H H 2-((4-(trifluorom ethyDbenzyDoxy) 0 -0384 H H H H H 3-((4-(trifluorom ethyDbenzyDoxy) 0 -0385 H H H H H 4-((4-(trifluorom ethyDbenzyDoxy) 0 -0386 H H H H H 2-((2-m ethoxybenzyDoxy) 0 -0387 H H H H H 3-((2-m ethoxybenzyDoxy) 0
[0327]
[Table 202]
com pound R' R2 Rj R4 Rb R p -0388 H H H H H 4-((2-m ethoxybenzyDoxy) 0 -0389 H H H H H 2-((3-m ethoxybenzyDoxy) 0 -0390 H H H H H 3-((3-m ethoxybenzyDoxy) 0 -0391 H H H H H 4-((3-m ethoxybenzyDoxy) 0 -0392 H H H H H 2-((4-m ethoxybenzyDoxy) 0 -0393 H H H H H 3-((4-m ethoxybenzyDoxy) 0 -0394 H H H H H 4-((4-m ethoxybenzyDoxy) 0 -0395 H H H H H 2-((2-(trifluorom ethoxy)benzy Doxy) 0 -0396 H H H H H 3-((2-(trifluorom ethoxy)benzy Doxy) 0 -0397 H H H H H 4-((2-(trifluorom ethoxy)benzy Doxy) 0 -0398 H H H H H 2-((3-(trifluorom ethoxy)benzy Doxy) 0 -0399 H H H H H 3-((3-(trifluorom ethoxy)benzy Doxy) 0 -0400 H H H H H 4-((3-(trifluorom ethoxy)benzy Doxy) 0 -0401 H H H H H 2-((4-(trifluorom ethoxy)benzy Doxy) 0 -0402 H H H H H 3-((4-(trifluorom ethoxy)benzy Doxy) 0 -0403 H H H H H 4-((4-(trifluorom ethoxy)benzy Doxy) 0 -0404 H H H H H 2-((2-(m ethylthb)benzyDoxy) 0 -0405 H H H H H 3-((2-(m ethylthb)benzyDoxy) 0 -0406 H H H H H 4-((2-(m ethylthb)benzyDoxy) 0 -0407 H H H H H 2-((3-(m ethylthb)benzyDoxy) 0 -0408 H H H H H 3-((3-(m ethylthb)benzyDoxy) 0 -0409 H H H H H 4-((3-(m ethylthb)benzyDoxy) 0 -0410 H H H H H 2-((4-(m ethylthb)benzyDoxy) 0 -0411 H H H H H 3-((4-(m ethylthb)benzyDoxy) 0 -0412 H H H H H 4-((4-(mnethylthb)benzyloxy) 0 -0413 H H H H H 2-((2-(mnethysulinyDbenzyloxy) 0 -0414 H H H H H 3-((2-(mnethyIsulfinyDbenzyDoxy) 0 -0415 H H H H H 4-((2-(m ethyIsulfinyDbenzyDoxy) 0 -0416 H H H H H 2-((3-(m ethyIsulfinyDbenzyDoxy) 0 -041] H H H H H 3-((3-(m ethyIsulfinyDbenzyDoxy) 0 -0418 H H H H H 4-((3-(m ethyIsulfinyDbenzyDoxy) 0 -0419 H H H H H 2-((4-(m ethyIsulfinyDbenzyDoxy) 0 -0420 H H H H H 3-((4-(m ethyIsulfinyDbenzyDoxy) 0 -0421 H H H H H 4-((4-(m ethyIsulfinyDbenzyDoxy) 0 -0422 H H H H H 2-((2-(m ethylsulfonyDbenzyDoxy) 0 -0423 H H H H H 3-((2-(m ethyIsulfonyDbenzyDoxy) 0 -0424 H H H H H 4-((2-((m ethy Isu fony Dbenzy Doxy) 0 -0426 H H H H H 2-((3-(m ethyIsufonyDbenzyDoxy) 0 -0426 H H H H H 3-((3-(methyIsulfonyDbenzyDoxy) 0 -042] H H H H H 4-((3-(m ethyIsulfonyDbenzyDoxy) 0 -0428 H H H H H 2-((4-(m ethyIsulfonyDbenzyDoxy) 0 -0429 H H H H H 3-((4-(m ethylsulfonyDbenzyDoxy) 0 -0430 H H H H H 4-((4-(m ethylsulfonyDbenzyDoxy) 0 -0431 H H H H H 2-((2-(trfluorom ethylthio)benzyDoxy) 0 -0432 H H H H H 3-((2-(trifluorom ethylthio)benzy)oxy) 0 -0433 H H H H H 4-((2-(trifluorom ethylthio)benzy)oxy) 0 -0434 H H H H H 2-((3-(trifluorom ethylthio)benzy)oxy) 0 -0436 H H H H H 3-((3-(trifluorom ethylthio)benzy)oxy) 0 -0436 H H H H H 4-((3-(trifluorom ethylthio)benzy)oxy) 0 -0437 H H H H H 2-((4-(trifluorom ethythio)benzy)oxy) 0 -0438 H H H H H 3-((4-(trifluorom ethylthio)benzy)oxy) 0 -0439 H H H H H 4-((4-(trifluorom ethylthio)benzy)oxy) 0 -0440 H H H H H 2-((2-(trifluorom ethysufinyDbenzy)oxy) 0 -0441 H H H H H 3-((2-(trifluorom ethyIsuIfinyDbenzyI)oxy) 0 -0442 H H H H H 4-((2-(trifluorom ethyIsuIfinyDbenzyI)oxy) 0 -0443 H H H H H 2-((3-(trifluorom ethyIsuIfinyDbenzyI)oxy) 0
[0328]
[Table 203]
cornpound R' R2 j R4 R p C-0444 H H H H H 3-((3-(trfluorom ethy Isu ffinyDbenzy Doxy) 0 C-0445 H H H H H 4-((3-(trfluorom ethy Isu ffinyDbenzy Doxy) 0 C-0446 H H H H H 2-((4-(trfluorom ethy Isu ffinyDbenzy Doxy) 0 C-0447 H H H H H 3-((4-(trfluorom ethy Isu ffinyDbenzy Doxy) 0 C-0448 H H H H H 4-((4-(trfluorom ethy Isu ffinyDbenzy Doxy) 0 C-0449 H H H H H 2-((2-(trifluorom ethy Isu fony Dbenzy Doxy) 0 C-0450 H H H H H 3-((2-(trifluorom ethy Isu fony Dbenzy Doxy) 0 C-0451 H H H H H 4-((2-(trifluorom ethy Isu fony Dbenzy Doxy) 0 C-0452 H H H H H 2-((3-(trifluorom ethy Isu fony Dbenzy Doxy) 0 C-0453 H H H H H 3-((3-(trifluorom ethy Isu fony Dbenzy Doxy) 0 C-0454 H H H H H 4-((3-(trifluorom ethy Isu fony Dbenzy Doxy) 0 C-0455 H H H H H 2-((4-(trfuorom ethy Isu ffony DbenzyIDoxy) 0 C-0456 H H H H H 3 -T4-tr if Iu oromethy Isu fony DbenzyIDoxy) 0 C-0457 H H H H H 4-((4-(trfluorom ethy Isu ffony D benzy Doxy) 0 C-0458 H H H H H 2-((2-am inobenzyDoxy) 0 C-0459 H H H H H 3-((2-am inobenzyDoxy) 0 C-0460 H H H H H 4-((2-am inobenzyDoxy) 0 C-0461 H H H H H 2-((3-am inobenzyDoxy) 0 C-0462 H H H H H 3-((3-am inobenzyDoxy) 0 C-0463 H H H H H 4-((3-am inobenzyI~oxy) 0 C-0464 H H H H H 2-((4-am inobenzyDoxy) 0 C-0465 H H H H H 3-((4-am inobenzy Doxy) 0 C-0466 H H H H H 4-7(-am inobenzyI~oxy) 0 C-0467 H H H H H 2-((2-(m ethy lm ino)ben zy Doxy) 0 C-0468 H H H H H 3-((2-(m ethy lam ino)ben zy Doxy) 0 C-0469 H H H H H 4-((2-(m ethy lm ino)ben zyDoxy) 0 C-0470 H H H H H 2-((3-(m ethy lm ino)ben zy Doxy) 0 C-0471 H H H H H 3-((3-(m ethy lm ino)ben zy Doxy) 0 C-0472 H H H H H 4-((3-(m ethy lam ino)ben zy Doxy) 0 C-0473 H H H H H 2-((4-(m ethy lm ino)benzyDoxy) 0 C-0474 H H H H H 3-((4-(m ethy lm ino)benzyDoxy) 0 C-0475 H H H H H 4-((4-(m ethy lm ino)benzyDoxy) 0 C-0476 H H H H H 2-((2-(d i~iethy lm ino)benzy Doxy) 0 C-0477 H H H H H 3-((2-(d iniethy lm ino)benzy Doxy) 0 C-0478 H H H H H 4-((2-(d iniethy lm ino)benzy Doxy) 0 C-0479 H H H H H 2-((3-(d iniethy lm ino)benzy Doxy) 0 C-0480 H H H H H 3-((3-diethy lm ino)benzyDoxy) 0 C-0481 H H H H H 4-((3-(diethy lm ino)benzy Doxy) 0 C-0482 H H H H H 2-((4-(diethy lm ino)benzy Doxy) 0 C-0483 H H H H H 3-((4-(d hi ethy lam ino)benzy Doxy) 0 C-0484 H H H H H 4-((4-(diethy lm ino)benzy Doxy) 0 C-0485 H H H H H 2-((2-cyanobenzy Doxy) 0 C-0486 H H H H H 3-((2-cyanobenzy Doxy) 0 C-0487 H H H H H 4-((2-cyanobenzy Doxy) 0 C-0488 H H H H H 2-((3-cyanobenzy Doxy) 0 C-0489 H H H H H 3-((3-cyanobenzy Doxy) 0 C-0490 H H H H H 4-((3-cyanobenzy Doxy) 0 C-0491 H H H H H 2-((4-cyanobenzy Doxy) 0 C-0492 H H H H H 3-((4-cyanobenzy Doxy) 0 C-0493 H H H H H 4-((4-cyanobenzy Doxy) 0 C-0494 H H H H H 2-((2-n trobenzyIDoxy) 0 C-0495 H H H H H 3 -7(2 -n trobenzyIDoxy) 0 C-0496 H H H H H 4-((2-n trobenzy Doxy) 0 C-0497 H H H H H 2-((3-n trobenzy Doxy) 0 C-0498 H H H H H 3-((3-n trobenzy Doxy) 0 C-0499 H H H H H 4-((3-n trobenzy Doxy) 0
[0329]
[Table 204] R com pound R' R2 Rj R4 b(R% P C-0500 H H H H H 2-((4-nitrobenzyDoxy) 0 C-0501 H H H H H 3-((4-nitrobenzyDoxy) 0 C-0502 H H H H H 4-((4-nitrobenzyDoxy) 0 C-0503 H H H H H 2-NH 2 0 C-0504 H H H H H 3-NH 2 0 C-0505 H H H H H 4-NH 2 0 C-0506 H H H H H 2-NHMe 0 C-0507 H H H H H 3-NHMe 0 C-0508 H H H H H 4-NHMe 0 C-0509 H H H H H 2-NHEt 0 C-0510 H H H H H 3-NHEt 0 C-0511 H H H H H 4-NHEt 0 C-0512 H H H H H 2-N(Me) 2 0 C-0513 H H H H H 3-N (Me) 2 0 C-0514 H H H H H 4-N(Me) 2 0 C-0515 H H H H H 2-N (Et) 2 0 C-0516 H H H H H 3-N (Et) 2 0 C-0517 H H H H H 4-N (Et) 2 0 C-0518 H H H H H 2-CHO 0 C-0519 H H H H H 3-CHO 0 C-0520 H H H H H 4-CHO 0 C-0521 H H H H H 2-C(=0)0H 0 C-0522 H H H H H 3-C(=0)0H 0 C-0523 H H H H H 4-C(=0)0H 0 C-0524 H H H H H 2-(1,3-d bxo an-2-y D 0 C-0525 H H H H H 3-(1,3-dbxolan-2-yID 0 C-0526 H H H H H 4-(1,3-dbxolan-2-yD 0 C-0527 H H H H H 2-(1,3-dbxan-2-yD 0 C-0528 H H H H H 3-(1,3-d bxan-2-y D 0 C-0529 H H H H H 4-(1,3-dbxan-2-yD 0 C-0530 H H H H H 2-(1H- idazol-2-yD 0 C-0531 H H H H H 3-(1H- idazol-2-yD 0 C-0532 H H H H H 4-(1H- idazol-2-yD 0 C-0533 H H H H H 2-(thiazol-2-yI) 0 C-0534 H H H H H 3-(thiazol-2-yI) 0 C-0535 H H H H H 4-(thiazol-2-yI) 0 C-0536 H H H H H 2-(oxazol-2-yD 0 C-0537 H H H H H 3-(oxazol-2-yD 0 C-0538 H H H H H 4-(oxazol-2-yD 0 C-0539 H H H H H 2-CH=N0H 0 C-0540 H H H H H 3-CH=N0H 0 C-0541 H H H H H 4-CH=N0H 0 C-0542 H H H H H 2-CH=NOMe 0 C-0543 H H H H H 3-CH=NOMe 0 C-0544 H H H H H 4-CH=NOMe 0 C-0545 H H H H H 2-(4,5-dihydro-3-isoxazolyD 0 C-0546 H H H H H 3-(4,5-dihydro-3-isoxazolyD 0 C-0547 H H H H H 4-(4,5-dihydro-3-isoxazolyD 0 C-0548 H H H H H 2-CN 0 C-0549 H H H H H 3-CN 0 C-0550 H H H H H 4-CN 0 C-0551 H H H H H 2-N0 2 0 C-0552 H H H H H 3-N0 2 0 C-0553 H H H H H 4-N0 2 0 C-0554 H H H H H 2,3-F 2 0 C-0555 H H H H H 2,4-F 2 0
[0330]
[Table 205] R com pound R' R2 Rj R4 b(R% P C-0556 H H H H H 2,5-F 2 0 C-0557 H H H H H 2,6-F 2 0 C-0558 H H H H H 3,4-F 2 0 C-0559 H H H H H 3,5-F 2 0 C-0560 H H H H H 2-F,3-C I 0 C-0561 H H H H H 2-F,4 -CI 0 C-0562 H H H H H 2-F,5-Cl 0 C-0563 H H H H H 2-F,6-CI 0 C-0564 H H H H H 3-F,2-C 1 0 C-0565 H H H H H 3-F,4-C I 0 C-0566 H H H H H 3-F,5-CI 0 C-0567 H H H H H 3-F,6-C| 0 C-0568 H H H H H 4-F, 2-C 0 C-0569 H H H H H 4-F,3-C I 0 C-0570 H H H H H 2-F,3-M e 0 C-0571 H H H H H 2-F4-M e 0 C-0572 H H H H H 2-F,5-M e 0 C-0573 H H H H H 2-F,6-M e 0 C-0574 H H H H H 3-F,2-M e 0 C-0575 H H H H H 3-F4-M e 0 C-0576 H H H H H 3-F,5-M e 0 C-577 H H H H H 3-F,6-M e 0 C-0578 H H H H H 4-F.2-M e 0 C-0579 H H H H H 4-F,3-M e 0 C-0580 H H H H H 2-F,3-0F3 0 C-0581 H H H H H 2-F,4-0F 0 C-0582 H H H H H 2-F,5-F3 0 C-0583 H H H H H 2-F, 6-0F3 0 C-0584 H H H H H 3-F,2-CF3 0 C-0585 H H H H H 3-F,4-0F3 0 C-0586 H H H H H 3-F,5-F3 0 C-0587 H H H H H 3-F, 6-0F3 0 C-0588 H H H H H 4-F, 2-0F3 0 C-0589 H H H H H 4-F,3-0F3 0 C-0590 H H H H H 2-F,3-0 M e 0 C-0591 H H H H H 2-F,4- M e 0 C-0592 H H H H H 2-F,5-0 M e 0 C-0593 H H H H H 2-F,6-0 M e 0 C-0594 H H H H H 3-F,2-0 M e 0 C-0595 H H H H H 3-F,4-0 M e 0 C-0596 H H H H H 3-F,5-0 M e 0 C-0597 H H H H H 3-F,6-0 M e 0 C-0598 H H H H H 4-F,2-0 M e 0 C-0599 H H H H H 4-F,3-0 M e 0 C-0600 H H H H H 2,3 -C 0 C-0601 H H H H H 2,4 -C 0 C-0602 H H H H H 2,5 -C 0 C-0603 H H H H H 2,6-C 0 C-0604 H H H H H 3,4 -C 0 C-0605 H H H H H 3,5-C 0 C-0606 H H H H H 2-C 1,3-M e 0 C-0607 H H H H H 2-C IA-M e 0 C-0608 H H H H H 2-C 1,5-M e 0 C-0609 H H H H H 2-C 1,6-M e 0 C-0610 H H H H H 3-C 1,2-Me 0 C-0611 H H H H H 3-C IA-M e 0
[0331]
[Table 206] R com pound R' R2 Rj R4 b(R% P C-0612 H H H H H 3-C 1,5-Me 0 C-0613 H H H H H 3-C 1,6-Me 0 C-0614 H H H H H 4-C 1,2-Me 0 C-0615 H H H H H 4-C I,3-Me 0 C-0616 H H H H H 2-C 1,3-CF, 0 C-0617 H H H H H 2-C 1,4-CF, 0 C-0618 H H H H H 2-C 1,5-CF 3 0 C-0619 H H H H H 2-C 1,6-CF 3 0 C-0620 H H H H H 3-C 1,2-CF 3 0 C-0621 H H H H H 3-C I,4-CF3 0 C-0622 H H H H H 3-C 1,5-CF 3 0 C-0623 H H H H H 3-0 1,6-F 3 0 C-0624 H H H H H 4-C 1,2-CF 3 0 C-0625 H H H H H 4-C I,3-CF3 0 C-0626 H H H H H 2-C 1,3-0Me 0 C-0627 H H H H H 2-C 4-Me 0 C-0628 H H H H H 2-C 1,5-0Me 0 C-0629 H H H H H 2-C 1,6-0Me 0 C-0630 H H H H H 3-C 1,2-0Me 0 C-0631 H H H H H 3-C I,4-0Me 0 C-0632 H H H H H 3-C 1,5-0Me 0 C-0633 H H H H H 3-C 1,6-0Me 0 C-0634 H H H H H 4-0 1,2-0 M e 0 C-0635 H H H H H 4-0 1,3-0 M e 0 C-0636 H H H H H 2,3-M e 2 0 C-0637 H H H H H 2,4-M e 2 0 C-0638 H H H H H 2,5- e 2 0 C-0639 H H H H H 2,6-M e 2 0 C-0640 H H H H H 3,4-M e 2 0 C-0641 H H H H H 3,5-M e 2 0 C-0642 H H H H H 2-M e,3-CF3 0 C-0643 H H H H H 2-M e,4-C0F3 0 C-0644 H H H H H 2-M e,5-CF3 0 C-0645 H H H H H 2-M e,6-CF3 0 C-0646 H H H H H 3-M e,2-CF3 0 C-0647 H H H H H 3-M e,4-C0F3 0 C-0648 H H H H H 3-M e,5-F3 0 C-0649 H H H H H 3-M e,6-CF3 0 C-0650 H H H H H 4-M e,2-CF3 0 C-0651 H H H H H 4-M e,3-CF3 0 C-0652 H H H H H 2-M e,3-0 M e 0 C-0653 H H H H H 2-M e,4-0 M e 0 C-0654 H H H H H 2-M e,5-0 M e 0 C-0655 H H H H H 2-M e,6-0 M e 0 C-0656 H H H H H 3-M e,2-0 M e 0 C-0657 H H H H H 3-M e,4-0 M e 0 C-0658 H H H H H 3-M e,5-0 M e 0 C-0659 H H H H H 3-M e,6-0 M e 0 C-0660 H H H H H 4-M e,2-0 M e 0 C-0661 H H H H H 4-M e,3-0 M e 0 C-0662 H H H H H 2,3-0 M e 2 0 C-0663 H H H H H 2,4-0 M e 2 0 C-0664 H H H H H 2,5-0 M e 2 0 C-0665 H H H H H 2,6-0 M e 2 0 C-0666 H H H H H 3,4-0 M e 2 0 C-0667 H H H H H 3,5-0 Me 2 0
[0332]
[Table 207] (R% com pound R' R2 Rj R4 Rb p C-0668 H H H H H 2-0Me,3-CF3 0 C-0669 H H H H H 2-0Me,4-CF3 0 C-0670 H H H H H 2-0Me,5-CF3 0 C-0671 H H H H H 2-0Me,6-CF3 0 C-0672 H H H H H 3-0Me,2-CF 3 0 C-0673 H H H H H 3-0Me,4-CF 3 0 C-0674 H H H H H 3-0Me,5-CF 3 0 C-0675 H H H H H 3-0Me,6-CF 3 0 C-0676 H H H H H 4-0Me,2-CF3 0 C-0677 H H H H H 4-0Me,3-CF3 0 C-0678 H H H H H 2-CHF 2 ,3-F 0 C-0679 H H H H H 2-CHF 2 ,4-F 0 C-0680 H H H H H 2-CHF 2 ,5-F 0 C-0681 H H H H H 2-CHF 2 ,6-F 0 C-0682 H H H H H 2-CH F 2 ,3-M e 0 C-0683 H H H H H 2-CH F 2 ,4-M e 0 C-0684 H H H H H 2-CH F 2 ,5-M e 0 C-0685 H H H H H 2-CH F 2 ,6-M e 0 C-0686 H H H H H 2-cycbpropyl,3-F 0 C-0687 H H H H H 2-cycbpropyl,4-F 0 C-0688 H H H H H 2-cycbpropyl,5-F 0 C-0689 H H H H H 2-cycbpropyl,6-F 0 C-0690 H H H H H 2-cycbpropyl,3-Me 0 C-0691 H H H H H 2-cycbpropyl,4-Me 0 C-0692 H H H H H 2-cycbpropyl,5-Me 0 C-0693 H H H H H 2-cycbpropyl,6-Me 0 C-0694 H H H H H 2-ethenyl,3-F 0 C-0695 H H H H H 2-ethenyl,4-F 0 C-0696 H H H H H 2-etheny L,5-F 0 C-0697 H H H H H 2-ethenyl,6-F 0 C-0698 H H H H H 2-ethenyl,3-Me 0 C-0699 H H H H H 2-ethenyl,4-Me 0 C-0700 H H H H H 2-ethenyL,5-Me 0 C-0701 H H H H H 2-ethenyl,6-Me 0 C-0702 H H H H H 2-0 Et,3-F 0 C-0703 H H H H H 2-0 Et,4-F 0 C-0704 H H H H H 2-0 Et,5-F 0 C-0705 H H H H H 2-0 Et,6-F 0 C-0706 H H H H H 2-0 Et,3-C I 0 C-0707 H H H H H 2-0 Et,4-C I 0 C-0708 H H H H H 2-0 Et,5-C I 0 C-0709 H H H H H 2-0 Et,6-C I 0 C-0710 H H H H H 2-0 Et,3-M e 0 C-0711 H H H H H 2-0 Et,4-M e 0 C-0712 H H H H H 2-0 Et,5-M e 0 C-0713 H H H H H 2-0 Et,6-M e 0 C-0714 H H H H H 2-0 Pr,3-F 0 C-0715 H H H H H 2-0 Pr,4-F 0 C-0716 H H H H H 2-0 Pr,5-F 0 C-0717 H H H H H 2-0 Pr,6-F 0 C-0718 H H H H H 2-0Pr,3-Me 0 C-0719 H H H H H 2-0Pr,4-Me 0 C-0720 H H H H H 2-0Pr,5-Me 0 C-0721 H H H H H 2-0Pr,6-Me 0 C-0722 H H H H H 2-0(i-Pr),3-F 0 C-0723 H H H H H 2-0(i-Pr),4-F 0
[0333]
[Table 208] R com pound R' R2 Rj R4 b(R% P C-0724 H H H H H 2-0(/-Pr),5-F 0 C-0725 H H H H H 2-0(/-Pr),6-F 0 C-0726 H H H H H 2-0(i-Pr),3-Me 0 C-0727 H H H H H 2-0(-Pr),4-Me 0 C-0728 H H H H H 2-0(i-Pr),5-Me 0 C-0729 H H H H H 2-0(-Pr),6-Me 0 C-0730 H H H H H 2-0CF 3 ,3-F 0 C-0731 H H H H H 2-0CF3 ,4-F 0 C-0732 H H H H H 2-0CF 3 ,5-F 0 C-0733 H H H H H 2-0CF 3 ,6-F 0 C-0734 H H H H H 2-0CF,3-Me 0 C-0735 H H H H H 2-0CF 3 ,4-Me 0 C-0736 H H H H H 2-0CF 3 ,5-Me 0 C-0737 H H H H H 2-0CF 3 ,6-Me 0 C-0738 H H H H H 2-0CHF 2 ,3-F 0 C-0739 H H H H H 2-0CHF 2 ,4-F 0 C-0740 H H H H H 2-0CHF 2 ,5-F 0 C-0741 H H H H H 2-0CHF 2 ,6-F 0 C-0742 H H H H H 2-0CHF 2 ,3-Me 0 C-0743 H H H H H 2-0CHF 2,4-Me 0 C-0744 H H H H H 2-0CHF 2 ,5-Me 0 C-0745 H H H H H 2-0CHF 2 ,6-Me 0 C-0746 H H H H H 2-(cycbpropybxy),3-F 0 C-0747 H H H H H 2-(cycbpropybxy),4-F 0 C-0748 H H H H H 2-(cycbpropy bxy),5-F 0 C-0749 H H H H H 2-(cycbpropybxy),6-F 0 C-0750 H H H H H 2-(cycbpropybxy),3-Me 0 C-0751 H H H H H 2-(cycbpropybxy),4-Me 0 C-0752 H H H H H 2-(cycbpropy bxy),5-M e 0 C-0753 H H H H H 2-(cycbpropybxy),6-Me 0 C-0754 H H H H H 2-(oxiran-2-yD,3-F 0 C-0755 H H H H H 2-(oxiran-2-yD,4-F 0 C-0756 H H H H H 2-(oxiran-2-yD,5-F 0 C-0757 H H H H H 2-(oxiran-2-yD,6-F 0 C-0758 H H H H H 2-(oxiran-2-yD,3-Me 0 C-0759 H H H H H 2-(oxiran-2-yD,4-Me 0 C-0760 H H H H H 2-(oxiran-2-yD,5-Me 0 C-0761 H H H H H 2-(oxiran-2-yD,6-Me 0 C-0762 H H H H H 2-(oxiran-2-yh ethyD,3-F 0 C-0763 H H H H H 2-(ox iran-2-y hi ethy D,4-F 0 C-0764 H H H H H 2-(oxiran-2-yh ethyD,5-F 0 C-0765 H H H H H 2-(oxiran-2-yh ethyD,6-F 0 C-0766 H H H H H 2-(oxiran-2-yI ethyD,3-Me 0 C-0767 H H H H H 2-(oxiran-2-yI ethyD,4-Me 0 C-0768 H H H H H 2-(oxiran-2-yI ethyD,5-Me 0 C-0769 H H H H H 2-(oxiran-2-yI ethyD,6-Me 0 C-0770 H H H H H 2-SMe,3-F 0 C-0771 H H H H H 2-SMe,4-F 0 C-0772 H H H H H 2-SMe,5-F 0 C-0773 H H H H H 2-SMe,6-F 0 C-0774 H H H H H 2-SMe,3-Me 0 C-0775 H H H H H 2-SMe,4-Me 0 C-0776 H H H H H 2-SMe,5-Me 0 C-0777 H H H H H 2-SMe,6-Me 0 C-0778 H H H H H 2-SEt,3-F 0 C-0119 H H H H H 2-SEt,4-F 0
[0334]
[Table 209]
com pound R' R2 Rj R4 R b(R% P C-0780 H H H H H 2-SEt,5-F 0 C-0781 H H H H H 2-SEt,6-F 0 C-0782 H H H H H 2-SEt,3-Me 0 C-0783 H H H H H 2-SEt,4-Me 0 C-0784 H H H H H 2-SEt,5-Me 0 C-0785 H H H H H 2-SEt,6-Me 0 C-0786 H H H H H 2-S(=0)Me,3-F 0 C-0787 H H H H H 2-S(=0)Me,4-F 0 C-0788 H H H H H 2-S(=0)Me,5-F 0 C-0789 H H H H H 2-S(=0)Me,6-F 0 C-0790 H H H H H 3-S(=0)Me,2-F 0 C-0791 H H H H H 3-S(=0)Me,4-F 0 C-0792 H H H H H 3-S(=0)Me,5-F 0 C-0793 H H H H H 3-S(=0)Me,6-F 0 C-0794 H H H H H 2-S(=0)Me,3-Me 0 C-0795 H H H H H 2-S(=0)Me,4-Me 0 C-0796 H H H H H 2-S(0)Me,5-Me 0 C-0797 H H H H H 2-S( 0)Me,6-Me 0 C-0798 H H H H H 3-S( 0)Me,2-Me 0 C-0799 H H H H H 3-S( 0)Me4-Me 0 C-0800 H H H H H 3-S( 0)Me,5-Me 0 C-0801 H H H H H 3 -S( 0)Me,6-Me 0 C-0802 H H H H H 2-S( 0) 2 Me,3-F 0 C-0803 H H H H H 2-S( 0) 2 Me,4-F 0 C-0804 H H H H H 2-S( 0) 2 Me,5-F 0 C-0805 H H H H H 2-S( 0) 2 Me,6-F 0 C-0806 H H H H H 2-S(=0) 2Me,3-Me 0 C-0807 H H H H H 2-S(=0) 2Me,4-Me 0 C-0808 H H H H H 2-S(=0) 2Me,5-Me 0 C-0809 H H H H H 2-S(=0) 2Me,6-Me 0 C-0810 H H H H H 2-SCF3 ,3-F 0 C-0811 H H H H H 2-SCF3 ,4-F 0 C-0812 H H H H H 2-SCF3 ,5-F 0 C-0813 H H H H H 2-SCF3 ,6-F 0 C-0814 H H H H H 2-SCF 3 ,3-M e 0 C-0815 H H H H H 2-SCF 3 ,4-M e 0 C-0816 H H H H H 2-SCF 3 ,5-M e 0 C-0817 H H H H H 2-SCF 3 ,6-M e 0 C-0818 H H H H H 2-S(=0)CF 3 ,3-F 0 C-0819 H H H H H 2-S(=0)CF 3 ,4-F 0 C-0820 H H H H H 2-S(=0)CF 3 ,5-F 0 C-0821 H H H H H 2-S(=0)CF 3 ,6-F 0 C-0822 H H H H H 2-S(=0)CF 3,3-Me 0 C-0823 H H H H H 2-S(=0)CF 3 ,4-Me 0 C-0824 H H H H H 2-S(=0)CF 3 ,5-Me 0 C-0825 H H H H H 2-S(=0)CF 3,6-Me 0 C-0826 H H H H H 2-S(=0) 2 CF3 ,3-F 0 C-0827 H H H H H 2-S(=0) 2CF 3 ,4-F 0 C-0828 H H H H H 2-S(=0) 2 CF3 ,5-F 0 C-0829 H H H H H 2-S (= 0 ) 2 CF 3 ,6-F 0 C-0830 H H H H H 2-S(=0) 2CF 3 ,3-Me 0 C-0831 H H H H H 2-S(=0) 2CF 3,4-Me 0 C-0832 H H H H H 2-S(=0) 2CF3 ,5-Me 0 C-0833 H H H H H 2-S(=0) 2CF3 ,6-Me 0 C-0834 H H H H H 2-(cycbpropylbio),3-F 0 C-0835 H H H H H 2-(cycbpropylb o),4-F 0
[0335]
[Table 210]
com pound R R2 RP R4 Rb (R% m C-0836 H H H H H 2-(cycbpropyltho),5-F 0 C-0837 H H H H H 2-(cycbpropylth b),6-F 0 C-0838 H H H H H 2-(cycbpropylth),3-Me 0 C-0839 H H H H H 2-(cycbpropylth),4-Me 0 C-0840 H H H H H 2-(cycbpropylth),5-Me 0 C-0841 H H H H H 2-(cycbpropylth),6-Me 0 C-0842 H H H H H 2-C(=0)Me,3-F 0 C-0843 H H H H H 2-C(=0)Me,4-F 0 C-0844 H H H H H 2-C(=0)Me,5-F 0 C-0845 H H H H H 2-C(=0)Me,6-F 0 C-0846 H H H H H 2-C(=0)Me,3-Me 0 C-0847 H H H H H 2-C(=0)Me4-Me 0 C-0848 H H H H H 2-C(=0)Me,5-Me 0 C-0849 H H H H H 2-C(=0)Me,6-Me 0 C-0850 H H H H H 3-C(=0)Me,2-F 0 C-0851 H H H H H 3-C(=0)Me,4-F 0 C-0852 H H H H H 3-C(=0)Me,5-F 0 C-0853 H H H H H 3-C(=0)Me,6-F 0 C-0854 H H H H H 3-C(=0)Me,2-Me 0 C-0855 H H H H H 3-C(=0)Me,4-Me 0 C-0856 H H H H H 3-C(=0)Me,5-Me 0 C-0857 H H H H H 3-C(=0)Me,6-Me 0 C-0858 H H H H H 2-C(=0)0Me,3-F 0 C-0859 H H H H H 2-C(=0)0Me,4-F 0 C-0860 H H H H H 2-C(=0)0Me,5-F 0 C-0861 H H H H H 2-C(=0)0Me,6-F 0 C-0862 H H H H H 2-C(=0)0Me,3-Me 0 C-0863 H H H H H 2-C(=0)0Me,4-Me 0 C-0864 H H H H H 2-C(=0)0Me,5-Me 0 C-0865 H H H H H 2-C(=0)0Me,6-Me 0 C-0866 H H H H H 2-C(=0)0Et,3-F 0 C-0867 H H H H H 2-C(=0)0Et,4-F 0 C-0868 H H H H H 2-C(=0)0Et,5-F 0 C-0869 H H H H H 2-C(=0)0Et,6-F 0 C-0870 H H H H H 2-C(=0)0Et,3-Me 0 C-0871 H H H H H 2-C(=0)0Et4-Me 0 C-0872 H H H H H 2-C(=0)0Et,5-Me 0 C-0873 H H H H H 2-C(=0)0Et,6-Me 0 C-0874 H H H H H 2-C(=0)NH 2,3-F 0 C-0875 H H H H H 2-C(=0)NH 2 ,4-F 0 C-0876 H H H H H 2-C(=0)NH 2 ,5-F 0 C-0877 H H H H H 2-C(=0)NH 2,6-F 0 C-0878 H H H H H 2-C(=0)NH 2,3-Me 0 C-0879 H H H H H 2-C(=0)NH 2,4-Me 0 C-0880 H H H H H 2-C(=0)NH 2,5-Me 0 C-0881 H H H H H 2-C(=0)NH 2,6-Me 0 C-0882 H H H H H 2-C(=0)NHMe,3-F 0 C-0883 H H H H H 2-C(=0)NHMe,4-F 0 C-0884 H H H H H 2-C(=0)NHMe,5-F 0 C-0885 H H H H H 2-C(=0)NHMe,6-F 0 C-0886 H H H H H 2-C(=0)NHMe,3-Me 0 C-0887 H H H H H 2-C(=O)NHMe,4-Me 0 C-0888 H H H H H 2-C(=0)NHMe,5-Me 0 C-0889 H H H H H 2-C(=0)NHMe,6-Me 0 C-0890 H H H H H 2-C(=0)NMe 2 ,3-F 0 C-0891 H H H H H 2-C0(=O)NM e 2 ,4-F 0
[0336]
[Table 211] R com pound R' R2 Rj R4 b(R% P C-0892 H H H H H 2-C(=0)NMe 2 ,5-F 0 C-0893 H H H H H 2-C(=0)NMe 2 ,6-F 0 C-0894 H H H H H 2-C(=0)NMe 2 ,3-Me 0 C-0895 H H H H H 2-C (=0)N M e 2 ,4-M e 0 C-0896 H H H H H 2-C(=0)NMe 2 ,5-Me 0 C-0897 H H H H H 2-C(=0)NMe 2 ,6-Me 0 C-0898 H H H H H 2-CH20H,3-F 0 C-0899 H H H H H 2-CH 2 0H,4-F 0 C-0900 H H H H H 2-CH 2 0H,5-F 0 C-0901 H H H H H 2-CH 2 0H,6-F 0 C-0902 H H H H H 2-CH 20H,3-Me 0 C-0903 H H H H H 2-CH 20H,4-Me 0 C-0904 H H H H H 2-CH 20H,5-Me 0 C-0905 H H H H H 2-CH 20H,6-Me 0 C-0906 H H H H H 2-CH 2 0CH ,3-F 0 C-0907 H H H H H 2-CH20CH 3 ,4-F 0 C-0908 H H H H H 2-CH 2 0CH ,5-F 0 C-0909 H H H H H 2-CH 2 0CH ,6-F 0 C-0910 H H H H H 2-CH 20CH 3 ,3-Me 0 C-0911 H H H H H 2-H 2 0 CH,4Ae 0 C-0912 H H H H H 2-CH 20CH ,5-Me 0 C-0913 H H H H H 2-CH 20CH ,6-Me 0 C-0914 H H H H H 2-CH 2 0CH 2 CH 3,3-F 0 C-0915 H H H H H 2-CH20CH2CH 3 ,4-F 0 C-0916 H H H H H 2-CH 2 0CH 2CH 3 ,5-F 0 C-0917 H H H H H 2-CH 2 0CH 2CH 3 ,6-F 0 C-0918 H H H H H 2-CH 20CH 2CH 3 ,3-Me 0 C-0919 H H H H H 2-CH 20CH 2CH ,4-Me 0 C-0920 H H H H H 2-CH 20CH 2CH 3 ,5-M e 0 C-0921 H H H H H 2-CH 20CH 2CH 3 ,6-Me 0 C-0922 H H H H H 2-0C(=0)CH ,3-F 0 C-0923 H H H H H 2-0C(=0)CH 3 ,4-F 0 C-0924 H H H H H 2-0C(=0)CH ,5-F 0 C-0925 H H H H H 2-0C(=0)CH ,6-F 0 C-0926 H H H H H 2-0C(=0)CH 3 ,3-Me 0 C-0927 H H H H H 2-0C(=0)CH 3 ,4-Me 0 C-0928 H H H H H 2-C0(=U)CH 3 ,5Ae 0 C-0929 H H H H H 2-0C(=0)CH 3 ,6-Me 0 C-0930 H H H H H 2-OS(=0) 2 CH 3 ,3-F 0 C-0931 H H H H H 2-0S(=0)2CH 3 ,4-F 0 C-0932 H H H H H 2-0S(=0)2CH 3 ,5-F 0 C-0933 H H H H H 2-0S(=0) 2 CH 3 ,6-F 0 C-0934 H H H H H 2-OS(=0) 2 CH,3-Me 0 C-0935 H H H H H 2-0S(=0) 2 CH 3A,4-Me 0 C-0936 H H H H H 2-0S(=0) 2 CH 3 ,5-Me 0 C-0937 H H H H H 2-0S(=0) 2 CH 3 ,6-Me 0 C-0938 H H H H H 2-CH2SCH 3 ,3-F 0 C-0939 H H H H H 2-CH 2SCH 3 ,4-F 0 C-0940 H H H H H 2-CH 2SCH 3 ,5-F 0 C-0941 H H H H H 2-CH 2 SCH,6-F 0 C-0942 H H H H H 2-CH 2SCH ,3-Me o C-0943 H H H H H 2-CH 2SCH 3 ,4-Me 0 C-0944 H H H H H 2-CH 2SCH 3 ,5-Me 0 C-0945 H H H H H 2-CH 2SCH 3 ,6-Me 0 C-0946 H H H H H 2-CH 2 SCF 3 ,3-F 0 C-0947 H H H H H 2-CH 2 SCF 3 ,4-F 0
[0337]
[Table 212] com pound R1 Rz R3 R4 R (R)m P C-0948 H H H H H 2-CH 2SCF 3 ,5-F 0 C-0949 H H H H H 2-CH 2SCF 3 ,6-F 0 C-0950 H H H H H 2-CH 2 SCF3 ,3-Me 0 C-0951 H H H H H 2-CH 2 SCF3 ,4-Me 0 C-0952 H H H H H 2-CH 2 SC F3 ,5-Me 0 C-0953 H H H H H 2-CH 2 SCF3 ,6-Me 0 C-0954 H H H H H 2-(benzy bxy),3-F 0 C-0955 H H H H H 2-(benzylbxy),4-F 0 C-0956 H H H H H 2-(benzylbxy),5-F 0 C-0957 H H H H H 2-(benzylbxy),6-F 0 C-0958 H H H H H 2-(benzyloxy),3-Me 0 C-0959 H H H H H 2-(benzyloxy),4-Me 0 C-0960 H H H H H 2-(benzyloxy),5-Me 0 C-0961 H H H H H 2-(benzyloxy),6-Me 0 C-0962 H H H H H 2-NH 2 ,3-F 0 C-0963 H H H H H 2-NH 2 ,4-F 0 C-0964 H H H H H 2-NH 2 ,5-F 0 C-0965 H H H H H 2-N H 2 ,6-4 0 C-0966 H H H H H 2-NH 2 ,3-Me 0 C-0967 H H H H H 2-NH 2,4-Me 0 C-0968 H H H H H 2-NH 2 ,5-Me 0 C-0969 H H H H H 2-NH 2 ,6-Me 0 C-0970 H H H H H 2-NH M e,3-F 0 C-0971 H H H H H 2-NH M e,4-F 0 C-0972 H H H H H 2-NH M e,5-F 0 C-0973 H H H H H 2-NH M e,6-F 0 C-0974 H H H H H 2-NHMe,3-M e 0 C-0975 H H H H H 2-NHMe,4-M e 0 C-0976 H H H H H 2-NHMe,5-Me 0 C-0977 H H H H H 2-NHMe,6-M e 0 C-0978 H H H H H 2-NH Et3-F 0 C-0979 H H H H H 2-NH Et4-F 0 C-0980 H H H H H 2-NH Et5-F 0 C-0981 H H H H H 2-NH Et6-F 0 C-0982 H H H H H 2-NHEt3-Me 0 C-0983 H H H H H 2-NH Et4-M e 0 C-0984 H H H H H 2-NHEt5-Me 0 C-0985 H H H H H 2-NH Et6-M e 0 C-0986 H H H H H 2-NM e 2 ,3-F 0 C-0987 H H H H H 2-NM e 2 ,4-F 0 C-0988 H H H H H 2-NM e 2,5-F 0 C-0989 H H H H H 2-NM e 2 ,6-F 0 C-0990 H H H H H 2-NMe 2 ,3-Me 0 C-0991 H H H H H 2-NAMe 2 ,4-Me 0 C-0992 H H H H H 2-NMe 2 ,5-Me 0 C-0993 H H H H H 2-NMe 2 ,6-Me 0 C-0994 H H H H H 2-NEt2 ,3-F 0 C-0995 H H H H H 2-NEt 2 ,4-F 0 C-0996 H H H H H 2-NEt2 ,5-F 0 C-0997 H H H H H 2-NAEt 2 ,6-F 0 C-0998 H H H H H 2-NEt2 ,3-M e 0 C-0999 H H H H H 2-NEt2 ,4-M e 0 C-1000 H H H H H 2-NEt 2 ,5-Me 0 C-1001 H H H H H 2-NEt2 ,6-M e 0 C-1002 H H H H H 2-CH0,3-F 0 C-1003 H H H H H 2-CH0,4-F 0
[0338]
[Table 213] cornpound R '1 -r R2 WR fRfU (Rb m -10 04 H H H H H 2-COHO, 5-F 0 -10 05 H H H H H 2-0H 0,6-F 0 -10 06 H H H H H 2 -C HO,3-M e 0 -100]7 H H H H H 2 -C HO,4-M e 0 -10 08 H H H H H 2 -C HO5-M e 0 -10 09 H H H H H 2 -C HO,6-M e 0 -10 10 H H H H H 2-C(=0 )OH,3-F 0 -1 011 H H H H H 2-C(=0 )OH,4-F 0 -1 012 H H H H H 2-C(=0 )OH,5-F 0 -1 013 H H H H H 2-C(=0 )OH,6-F 0 -1 014 H H H H H 2-C00H,3-M e 0 -1 015 H H H H H 2-C00H,4-M e 0 -1 016 H H H H H 2-C00H,5-M e 0 -10 17 H H H H H 2-C00H,6-M e 0 -1 018 H H H H H 2-01,3-d bxolIan-2-yI1),3-F 0 -1 019 H H H H H 2-(0,3-d bxolIan-2-yI),4-F 0 -1 020 H H H H H 2-(1,3-d bxo Ian-2-y 1),5-F 0 -1 021 H H H H H 2-01,3-d bxolIan-2-yI1),6-F 0 -1 022 H H H H H 2-(1,3-d ioxolIan-2-yI),3-M e 0 -1 023 H H H H H 2-(1,3-d ioxolIan-2-yI),4-Me 0 -1 024 H H H H H 2-(1,3-d ioxolIan-2-yI),5-M e 0 -1 025 H H H H H 2-(1,3-d ioxolIan-2-yI),6-M e 0 -1 026 H H H H H 2-(1,3-d bxan-2-y1,3-F 0 -1 027 H H H H H 2-(1,3-d bxan-2-y1)4-F 0 -1 028 H H H H H 2-(1,3-d bxan-2-y),5-F 0 -1 029 H H H H H 2-(1,3-d bxan-2-y),6-F 0 -1 030 H H H H H 2-(1,3-d bxan-2-y1),3-M e 0 -1 031 H H H H H 2-(1,3-d bxan-2-y1)4-M e 0 -1 032 H H H H H 2-(1,3-d bxan-2-y1),5-M e 0 -1 033 H H H H H 2-(1,3-d bxan-2-y1),6-M e 0 -1 034 H H H H H 2 -(th iazo[-2-yI),3-F 0 -1 035 H H H H H 2 -(th iazo[P2 -y)4-F 0 -10 36 H H H H H 2 -(th iazo[P2 -Y)5 -F 0 -103]7 H H H H H 2-(th iazo[P2-y )6 -F 0 -10 38 H H H H H 2 -(thia zo[P2 -y1)3 -Me 0 -10 39 H H H H H 2 -(thia zo[P2 -y )4 -Me 0 -10 40 H H H H H 2 -(th ia zolP2-Y)5 -Me 0 -10 41 H H H H H 2 -(thia zo[P2 -y1)6 -Me 0 -10 42 H H H H H 2 -(ox azo[1-2 -Y),3 -F 0 -10 43 H H H H H 2-(oxazo[1-2-y1),4-F 0 -1 044 H H H H H 2-(oxazo[1-2-Y1),5-F 0 -1 045 H H H H H 2-(oxazo[1-2-Y1),6-F 0 -1 046 H H H H H 2-(oxazo [-2-y 1)3-M e 0 -1 04] H H H H H 2-(oxazo[1-2-y )4-W e 0 -1 048 H H H H H 2-(oxazo[1-2-Y ),5-M e 0 -1 049 H H H H H 2-(oxazo[1-2-y1),6-W e 0 -1 050 H H H H H 2-OH = NOH,3-F 0 -1 051 H H H H H 2-OH = NOH,4-F 0 -1 052 H H H H H 2-OH = NOH,5-F 0 -1 053 H H H H H 2-OH = NOH,6-F 0 -1 054 H H H H H 2-C H= NOH,3-M e 0 -1 055 H H H H H 2-C H= NOH,4-M e 0 -1 056 H H H H H 2-C H= NOH,5-M e 0 -1 057 H H H H 2-C H= NOH,6-M e 0 -1 058 H H H H H 2-C H= NO Me,3-F 0 -1 059 H H H H H 2-C H= NO Me,4-F 0
[0339]
[Table 214] com pound R1 Rz R3 R4 R (R)m P C-1060 H H H H H 2-CH=N0Me,5-F 0 C-1061 H H H H H 2-CH= NOM e,6-F 0 C-1062 H H H H H 2-CH=N0Me,3-Me 0 C-1063 H H H H H 2-CH=N0Me,4-Me 0 C-1064 H H H H H 2-CH=N0Me,5-Me 0 C-1065 H H H H H 2-CH=N0Me,6-M e 0 C-1066 H H H H H 2-CN,3-F 0 C-1067 H H H H H 2-CN,4-F 0 C-1068 H H H H H 2-CN,5-F 0 C-1069 H H H H H 2-CN,6-F 0 C-1070 H H H H H 2-CN,3-CI 0 C-1071 H H H H H 2-CN,4-CI 0 C-1072 H H H H H 2-CN,5-CI 0 C-1073 H H H H H 2-CN,6-CI 0 C-1074 H H H H H 2-CN,3-Me 0 C-1075 H H H H H 2-CN,4-Me 0 C-1076 H H H H H 2-CN,5-Me 0 C-1077 H H H H H 2-CN,6-Me 0 C-1078 H H H H H 2-CN,3-0Me 0 C-1079 H H H H H 2-CN,4-0Me 0 C-1080 H H H H H 2-CN,5-0Me 0 C-1081 H H H H H 2-CN,6-0Me 0 C-1082 H H H H H 3-CN,2-F 0 C-1083 H H H H H 3-CN,4-F 0 C-1084 H H H H H 3-CN,5-F 0 C-1085 H H H H H 3-CN,6-F 0 C-1086 H H H H H 3-CN,2-CI 0 C-1087 H H H H H 3-CN,4-CI 0 C-1088 H H H H H 3-CN,5-CI 0 C-1089 H H H H H 3-CN,6-CI 0 C-1090 H H H H H 3-CN,2-Me 0 C-1091 H H H H H 3-CN,4-Me 0 C-1092 H H H H H 3-CN,5-Me 0 C-1093 H H H H H 3-CN,6-Me 0 C-1094 H H H H H 3-CN,2-0Me 0 C-1095 H H H H H 3-CN,4-0Me 0 C-1096 H H H H H 3-CN,5-0Me 0 C-1097 H H H H H 3-CN,6-0Me 0 C-1098 H H H H H 4-CN,2-F 0 C-1099 H H H H H 4-CN,3-F 0 C-1100 H H H H H 4-CN,2-CI 0 C-1101 H H H H H 4-CN,3-CI 0 C-1102 H H H H H 4-CN,2-Me 0 C-1103 H H H H H 4-CN,3-Me 0 C-1104 H H H H H 4-CN,2-0Me 0 C-1105 H H H H H 4-CN,3-0Me 0 C-1106 H H H H H 2-NJ0 2 ,3-4 0 C-1107 H H H H H 2-N0 2 ,4-F 0 C-1108 H H H H H 2-N0 2 ,5-F 0 C-1109 H H H H H 2-NJ0 2 ,6-4 0 C-1110 H H H H H 2-N0 2,3-Me 0 C-1111 H H H H H 2-N 0 2,4-M e 0 C-1112 H H H H H 2-N0 2,5-Me 0 C-1113 H H H H H 2-N0 2,6-Me 0 C-1114 H H H H H 2-Me,3,4-F 2 0 C-1115 H H H H H 2-Me,3,5-F 2 0
[0340]
[Table 215]
cornpound R2 R3 R~4 WR (Rb~ WR p C0-1 116 H H H H H 2 -M e,3,6 -F 2 0 -11 17 H H H H H 2 -M e,4,5 -F 2 0 -1 118 H H H H H 2-OM e,3,4-F2 0 -1 119 H H H H H 2-OM e,3,5-F2 0 C0-1 120 H H H H H 2-OM e,3,6-F2 0 -1 121 1 H H H H H 2-OM e,4,5-F2 0 -1 122 H H H H H 2-(C0H 2-3 0 -1 123 H H H H H 2-(C0H 2-3 0 -1 124 H H H H H 2 -(00CH 2 C0H2)-3 0 -1 125 H H H H H 2- (OCH 2 COH 2 COH2-3 0 C0-1 126 H H H H H 2 -(C H2 CH2 0)-3 0 C0-11 27 H H H H H 2- (C0H2 C0H 2 C0H 2 0)-3 0 -1128 H H H H H 3 -(C0H 23 -4 0 -1129 H H H H H 3 -(C0H 24 -4 0 C0-1 130 H H H H H 3 -(0UC H2 CH 2)-4 0 -1131 H H H H H 3- (00CH 2 C0H 2 C0H 2 )-4 0 -1132 H H H H H 3-(C0H 2 C0H 2 0)-4 0 -1133 H H H H H 3- (C0H 2 C0H 2 C0H 2 0)-4 0 -1134 H H H H H 2 -(00CH 20)5-3 0 -1135 H H H H H 3 -(00CH 20 )-4 0 -1136 H H H H H 2- (00CH 2 C0H 2 0)-3 0 -11 37 H H H H H 3- (00CH 2 C0H 20)-4 0 -1138 H H H H H 2- ( CF2U )-3 0 -1139 H H H H H 3- (00CF20)-4 0 -1140 H H H H H 2-M e,6-Et 0 -1141 H H H H H 2 -CH2 0TB S 0 -1142 H H H H H 2 -cyc bp ro py1,3-OM e 0 -1143 H H H H H 2 -cyc bp ro py1,4-OM e 0 -1144 H H H H H 2 -cyc bp ro py 1,b-0Me 0 -1145 H H H H H 2 -cyc bp ro py1,6-OM e 0 -1146 H H H H H 2 -M e,3-Me, 6-M e 0 -114] H H H H H 2 -M e,4 -0Me, 6-M e 0 -1 148 H H H H H 2 -0M e,3-M e, 6-Me 0 -1 149 H H H H H 2 -0M e,5-M e, 6-Me 0 -1 150 H H H H H 2 -0M e, 3-F, 6-M e 0 -1151 H H H H H 2 -0M e, 5-F,6-M e 0 -1152 H H H H H 2 -0M e, 5-M e, 6-F 0 -1153 H H H H H 2- 1,3-M e,6-F 0 -1154 H H H H H 2- 1,5-M e,6-F 0 -1 155 H H H H H 2 -C1,3 -0M e,6-F 0 -1 156 H H H H H 2 -C1,5 -0M e,6-F 0 -115] H H H H H 2-M e,-Et 0 -1158 H H H H H 2,6-E t 2 0 -1159 H H H H H 2-Et,6-F 0 -1160 H H H H H 2 -CH2 0C H3 ,6-CI1 0 -1161 H H H H H 2 -CH 2 00CH 2 CH,B-0I1 0 -1162 H H H H H 2-0OMe, 5-C H= NOM e 0 -1163 H H H H H 2-COHANM e 2 0 -1164 H H H H H 2 -CH 2 0CH3 ,6-C0F, 0 0-15 H H F H H 2-M e 10
[0341]
[Table 216]
R' R' 0 4 R /\ NN a' R' (O)p R'
cornpound R1 ~ R2 Rj R4 R (R%) p C-5001 H H H H H HI 1 C-5002 H H H H H 2-F 1 C-5003 H H H H H 3-F 1 C-5004 H H H H H 4-F 1 C-5005 H H H H H 2-Cl1 C-5006 H H H H H 3-Cl1 1 C-5007 H H H H H 4-Cl1 1 C-5008 H H H H H 2-B r 1 C-5009 H H H H H 3-B r 1 C-501 0 H H H H H 4-B r 1 C-501 1 H H H H H 2-1 1 C-501 2 H H H H H 3-1 1 C-501 3 H H H H H 4-1 1 C-501 4 H H H H H 2-0OH 1 C-501 5 H H H H H 3-O H 1 C-501 6 H H H H H 4-0OH 1 C-501 7 H H H H H 2-SH 1 C-501 8 H H H H H 3-SH 1 C-501 9 H H H H H 4-SH 1 C-5020 H H H H H 2-M e 1 C-5021 H H H H H 3-M e 1 C-5022 H H H H H 4-M e 1 C-5023 H H H H H 2-Et 1 C-5024 H H H H H 3-Et 1 C-5025 H H H H H 4-Et 1 C-5026 H H H H H 2-Pr 1 C-5027 H H H H H 3-Pr 1 C-5028 H H H H H 4-Pr 1 C-5029 H H H H H 2-i-Pr 1 C-5030 H H H H H 3-i-Pr 1 C-5031 H H H H H 4-i-Pr 1 C-5032 H H H H H 2-Bu 1 C-5033 H H H H H 3-Eu 1 C-5034 H H H H H 4-B u 1 C -5035 H H H H H 2-s-B u 1 C -503 6 H H H H H 3-s-E u 1 C -503 7 H H H H H 4-s-E u 1 C -5038 H H H H H 2-/-B u 1 C -503 9 H H H H H 3--B u 1 C -5040 H H H H H 4-/-B u 1 C -5041 H H H H H 2-t-Bu 1 C -5042 H H H H H 3-t-B u 1 C -5043 H H H H H 4-t-B u 1 C -5044 H H H H H 2-C F 3 1 C -5045 H H H H H 3-CUF, 1 C -5046 H H H H H 4-C F, 1 C -5 04 7 H H H H H 2 -UCHF 2 1 C -5 04 8 H H H H H 3 -C HF 2 1 C -5 04 9 H H H H H 4 --CHF 2 1 C -5 05 0 H H H H H 2-C H 2F 1 C -5 05 1 j H H H H H 3 -C H 2F 1 C;-b 05b2 1 H H H H H 4 -C H 2 F
[0342]
[Table 217]
cornpound R] -R - R- R- r (R)m p 0-5053 H H H H H 2-0F 20 1 1 0-5054 H H H H H 3-0F 20 1 1 0-5055 H H H H H 4-C0F 20C1 1 0-5056 H H H H H 2-CF(CF 3 ) 2 1 0-5057 H H H H H 3-CF(CF 3 ) 2 1 0-5058 H H H H H 4-CF(CF 3 ) 2 1 0-5059 H H H H H 2-oycopropyl 1 0-5060 H H H H H 3-oycopropyl 1 0-5061 H H H H H 4-oycopropyl 1 0-5062 H H H H H 2-cyolobutyl 1 0-5063 H H H H H 3-cyolobutyl 1 0-5064 H H H H H 4-cyolobutyl 1 0-5065 H H H H H 2-oycopentyl 1 0-5066 H H H H H 3-oycopentyl 1 0-5067 H H H H H 4-oycopentyl 1 0-5068 H H H H H 2-(oyolopropyhi ethy D 1 0-5069 H H H H H 3-(oyolopropyhi ethy D 1 0-5070 H H H H H 4-(oyolopropyhi ethy D 1 0-5071 H H H H H 2-(oyobbutyhi ethy D 1 0-5072 H H H H H 3-(oycobutyhIethy D 1 0-5073 H H H H H 4-(oycobutyhIethy D 1 0-5074 H H H H H 2-(oycopentyhethyl) 1 0-5075 H H H H H 3-(oycobpentyhiethyl 1 0-5076 H H H H H 4-(oycopentyhethy D 1 0-5077 H H H H H 2-(oyo lop ropy lethy D 1 0-5078 H H H H H 3-(oyo lop ropy lethy D 1 0-5079 H H H H H 4-(oyo lop ropy lethy D 1 0-5080 H H H H H 2-(2,2-difluorooycopropyD 1 0-5081 H H H H H 3-(2,2-difluorooycopropyD 1 0-5082 H H H H H 4-(2,2-difluorooycopropyD 1 0-5083 H H H H H 2-(2,2-d ichbrooy op ropyl) 1 0-5084 H H H H H 3-(2,2-d iohbrooy op ropyl) 1 0-5085 H H H H H 4-(2,2-d iohbrooy op ropyl) 1 0-5086 H H H H H 2-ethenyl1 1 0-5087 H H H H H 3-ethenyl1 1 0-5088 H H H H H 4-ethenyl1 1 0-5089 H H H H H 2-a ll'I 1 0-5090 H H H H H 3-a llyI 1 0-5091 H H H H H 4-a llyI 1 0-5092 H H H H H 2-(prop-1 -en-1 -y D 1 0-5093 H H H H H 3-Qprop-1 -en-1 -y D 1 0-5094 H H H H H 4-(prop-1 -en-1 -y D 1 0-5095 H H H H H 2-(trffluoroetheny D 1 0-5096 H H H H H 3-(trffluoroetheny D 1 0-5097 H H H H H 4-(trffluoroethenyl) 1 0-5098 H H H H H 2-(2,2-d ithbroetheny D 1 0-5099 H H H H H 3-(2,2-d ithbroetheny D 1 0-51 00 H H H H H 4-(2,2-d ithbroetheny D1 0-51 01 H H H H H 2-ethynyl1 1 0-51 02 H H H H H 3-ethynyl1 1 0-51 03 H H H H H 4-ethynyl1 1 0-51 04 H H H H H 2-01-propyn-1 -yI) 1 0-51 05 H H H H H 3-01-propyn-1 -yD 1 0-51 06 H H H H H 4-01-propyn-1 -yI) 1 0-51 07 H H H H H 2-(2-propyn-1 -y D 1 0-51 08 H H H H H 3-(2-propyn-1 -yI) 1 0-51 09 H H H H H 4-(2-p ro pyn-1-y D1
[0343]
[Table 218]
cornpound R] r R2 r r- Rr 4(Rd)m p -51 10 H H H H H 2-(2-oy op ropy lethyny D 1 C-51 11 H H H H H 3-(2-oy op ropy lethyny D 1 -51 12 H H H H H 4-(2-cy op ropy lethyny D 1 -51 13 H H H H H 2-(2--chblroethynyD 1 -51 14 H H H H H 3-(2--chblroethynyD 1 -51 15 H H H H H 4-(2--chblroethynyD 1 -51 16 H H H H H 2-(2-brom oethynyl) 1 -51 17 H H H H H 3-(2-brom oethynyl) 1 -51 18 H H H H H 4-(2-brom oethynyl) 1 -51 19 H H H H H 2-OM e 1 -51 20 H H H H H 3-OM e 1 -51 21 H H H H H 4-OM e 1 -51 22 H H H H H 2-0 Et 1 -51 23 H H H H H 3-0 Et 1 -51 24 H H H H H 4-0 Et 1 -51 25 H H H H H 2-0 Pr 1 -51 26 H H H H H 3-0 Pr 1 -51 27 H H H H H 4-0 Pr 1 -51 28 H H H H H 2-0 (/-Pr) 1 -51 29 H H H H H 3-0 (/-Pr) 1 -51 30 H H H H H 4-0 (/-Pr) 1 -51 31 H H H H H 2-0 Bu 1 -51 32 H H H H H 3-0 Bu 1 -51 33 H H H H H 4-0 Bu 1 -51 34 H H H H H 2-0 (s-B u) 1 -51 35 H H H H H 3-0 (s-B u) 1 -51 36 H H H H H 4-0 (s-B u) 1 -51 37 H H H H H 2-0 (/-B u) 1 -51 38 H H H H H 3-0 (/-B u) 1 -51 39 H H H H H 4-0 (/-BEu) 1 -51 40 H H H H H 2-0 (t-Eu) 1 -51 41 H H H H H 3-0 (t-Bu) 1 -51 42 H H H H H 4-0 (t-Bu) 1 -51 43 H H H H H 2-00%, 1 -51 44 H H H H H 3-00%3 1 -5145 H H H H H 4-00%3 1 -5146 H H H H H 2-0 CH F2 1 -51 47 H H H H H 3-0 CH F2 1 -51 48 H H H H H 4-0 CH F2 1 -51 49 H H H H H 2-0CH 20F 3 1 -51 50 H H H H H 3-0CH 20F 3 1 -51 51 H H H H H 4-0CH 20F 3 1 -51 52 H H H H H 2-(oy opropyblxy) 1 -51 53 H H H H H 3-(oy opropyblxy) 1 -51 54 H H H H H 4-(oy opropyblxy) 1 -51 55 H H H H H 2-(oyolobutyblxy) 1 -51 56 H H H H H 3-(oyolobutyblxy) 1 -51 57 H H H H H 4-(oyolobutyblxy) 1 -51 58 H H H H H 2-(oyo lopentyblxy) 1 -51 59 H H H H H 3-(oyo lopentyblxy) 1 -51 60 H H H H H 4-(oyo lopentyblxy) 1 -51 61 H H H H H 2-((2,2-d ichbroy op ropy Doxy) 1 -51 62 H H H H H 3-((2,2-d ichbroy op ropy Doxy) 1 -51 63 H H H H H 4-((2,2-d ichbroy op ropy Doxy) 1 -51 64 H H H H H 2-(oyobpropyhiethoxy) 1 -51 65 H H H H H 3-(oyobpropyhiethoxy) 1 -51 66 H H H H H 4-(oyobp ropy hiethoxy)1
[0344]
[Table 219]
com pound R R2 R R (R)m P C-5167 H H H H H 2-((2,2-difluorocycbpropyDm ethoxy) 1 C-5168 H H H H H 3-((2,2-difluorocycbpropyDm ethoxy) 1 C-5169 H H H H H 4-((2,2-difluorocycbpropyDm ethoxy) 1 C-5170 H H H H H 2-(oxiran-2-yI) 1 C-5171 H H H H H 3-(oxiran-2-yI) 1 C-5172 H H H H H 4-(oxiran-2-yI) 1 C-5173 H H H H H 2-(oxiran-2-yh ethyl) 1 C-5174 H H H H H 3-(oxiran-2-yh ethyl) 1 C-5175 H H H H H 4-(oxiran-2-yh ethyl) 1 C-5176 H H H H H 2-SM e 1 C-5177 H H H H H 3-SM e 1 C-5178 H H H H H 4-SM e 1 C-5179 H H H H H 2-SEt 1 C-5180 H H H H H 3-SEt 1 C-5181 H H H H H 4-SEt 1 C-5182 H H H H H 2-S(=0)Me 1 C-5183 H H H H H 3-S(=0)Me 1 C-5184 H H H H H 4-S(=0)Me 1 C-5185 H H H H H 2-S (=0) 2M e 1 C-5186 H H H H H 3-S (=0) 2M e 1 C-5187 H H H H H 4-S (=0) 2M e 1 C-5188 H H H H H 2-SCF 1 C-5189 H H H H H 3-SCF 1 C-5190 H H H H H 4-SCF, 1 C-5191 H H H H H 2-S(=0)CF 3 1 C-5192 H H H H H 3-S(=0)CF 3 1 C-5193 H H H H H 4-S(=0)CF3 1 C-5194 H H H H H 2-S(=0) 20F 3 1 C-5195 H H H H H 3-S(=0) 2CF 3 1 C-5196 H H H H H 4-S(=0) 2CF3 1 C-5197 H H H H H 2-SCF (F 3 ) 2 1 C-5198 H H H H H 3-SCF (CF 3) 2 1 C-5199 H H H H H 4-SCF (CF 3) 2 1 C-5200 H H H H H 2-(cycbpropylthio) 1 C-5201 H H H H H 3-(cycbpropylthio) 1 C-5202 H H H H H 4-(cycbpropylthio) 1 -5203 H H H H H 2-(cycbpropysulfinyD 1 -5204 H H H H H 3-(cycbpropysulfinyD 1 C-5205 H H H H H 4-(cycbpropylsulfinyl) 1 C-5206 H H H H H 2-(cycbpropyIsulfonyD 1 C-5207 H H H H H 3-(cycbpropyIsulfonyD 1 C-5208 H H H H H 4-(cycbpropyIsulfonyD 1 C-5209 H H H H H 2-((cycbpropyI ethyI)thio) 1 -5210 H H H H H 3-((cycbpropyI ethyl)thio) 1 C-5211 H H H H H 4-((cycbpropyI ethyl)thio) 1 -5212 H H H H H 2-((cycbpropyh ethyDsulfinyD 1 -5213 H H H H H 3-((cycbpropyh ethyDsulfinyD 1 C-5214 H H H H H 4-((cycobpropy Iethyl)sulfinyD 1 -5215 H H H H H 2-((cycbpropy ethyDsulfonyD 1 -5216 H H H H H 3-((cycbpropy ethyDsulfonyD 1 -5217 H H H H H 4-((cycbpropy IethylsulfonyD 1 C-5218 H H H H H 2-(((2,2-difluorocycbpropyl)m ethyl)thio) 1 -5219 H H H H H 3-(((2,2-difluorocycbpropyDm ethyDthio) 1 C-5220 H H H H H 4-(((2,2-difluorocycbpropyl)m ethyl)thio) 1 -5221 H H H H H 2-(((2,2-diflorocycobpropyDm ethyDsulfinyD 1 C-5222 H H H H H 3-(((2,2-diflorocycobpropyl)m ethyl)sulfinyl) 1 -5223 H H H H H 4-(((2,2-diflorocycobpropyDm ethyDsulfiny 1
[0345]
[Table 220]
com pound R' R2 R- R44 R (Rd)m P C-5224 H H H H H 2-(((2,2-difluorocycobpropyl)m ethyl)sulfonyD 1 C-5225 H H H H H 3-(((2,2-difluorocycobpropyl)m ethyl)sulfonyD 1 -5226 H H H H H 4-(((2,2-difluorocycobpropyl)m ethyl)sulfonyD 1 -5227 H H H H H 2-C (=0)Me 1 -5228 H H H H H 3-C(=0)Me 1 -5229 H H H H H 4-C (=0)Me 1 -5230 H H H H H 2-C (=0)Et 1 -5231 H H H H H 3-C (=0)Et 1 -5232 H H H H H 4-C (=0)Et 1 C-5233 H H H H H 2-C (=0)0%, 1 C-5234 H H H H H 3-C (=0)0F3 1 C-5235 H H H H H 4-C (=0)CF3 1 -5236 H H H H H 2-C(=0)0Me 1 -5237 H H H H H 3-C(=0)0Me 1 -5238 H H H H H 4-C(=0)0Me 1 -5239 H H H H H 2-(=0)0Et 1 C-5240 H H H H H 3-C(=0)0Et 1 C-5241 H H H H H 4-C(=0)0Et 1 C-5242 H H H H H 2-C(=0)NH 2 1 C-5243 H H H H H 3-C(=0)NH 2 1 C-5244 H H H H H 4-C (=0)NH2 1 -5245 H H H H H 2-C(=0)NHMe 1 -5246 H H H H H 3-C(=0)NHMe 1 -5247 H H H H H 4-C(=0)NHMe 1 -5248 H H H H H 2-C(=0)NMe 2 1 -5249 H H H H H 3-C(=0)NMe 2 1 -5250 H H H H H 4-C(=0)NMe 2 1 C-5251 H H H H H 2-CH 2 0(=0)H 3 1 C-5252 H H H H H 3-CH 2 0(=0)H 3 1 C-5253 H H H H H 4-CH 2 C(=0)CH 3 1 C-5254 H H H H H 2-CH 2 0(=0)CF 3 1 C-5255 H H H H H 3-CH 2C(=0)CF 3 1 -5256 H H H H H 4-CH 2C(=0)CF3 1 -5257 H H H H H 2-CH 2C(=0)0CH 3 1 -5258 H H H H H 3-CH 2C(=0)0CH 3 1 -5259 H H H H H 4-CH 2C(=0)0CH 3 1 -5260 H H H H H 2-CH20H 1 C-5261 H H H H H 3-CH20H 1 C-5262 H H H H H 4-CH20H 1 C-5263 H H H H H 2-CH 200H 3 1 C-5264 H H H H H 3-CH 20CH 3 1 C-5265 H H H H H 4-CH 200H 3 1 C-5266 H H H H H 2-CH 2 0CH 2CH 3 1 C-5267 H H H H H 3-CH 2 00H 20H 3 1 C-5268 H H H H H 4-CH 2 0CH 2CH 3 1 C-5269 H H H H H 2-CH(CH 3)0CH 3 1 -5270 H H H H H 3-CH(CH 3)0CH 3 1 -5271 H H H H H 4-CH (CH 3)0CH 3 1 C-5272 H H H H H 2-CH 2 CH 20CH 3 1 C-5273 H H H H H 3-CH 2 CH2 00CH 3 1 C-5274 H H H H H 4-CH 2 CH 20CH 3 1 C-5275 H H H H H 2-CH 20CF3 1 C-5276 H H H H H 3-CH 20CF3 1 C-5277 H H H H H 4-CH 20CF3 1 C-5278 H H H H H 2-0F 200H 3 1 C-5279 H H H H H 3-CF 20CH 3 1 C-5280 H H H H H 4-GF 200H 3
[0346]
[Table 221]
com pound R' R2 R- R- R (R°)m P -5281 H H H H H 2-0F 20F 2 0F 1 -5282 H H H H H 3-0F 20F 2 0F 1 -5283 H H H H H 4-GF 2 F 2 0F 1 -5284 H H H H H 2-0C(=0)GH 3 1 -5285 H H H H H 3-0C(=0)GH 3 -5286 H H H H H 4-0C(=0)GH 3 1 -5287 H H H H H 2-U0(=U)0F 3 1 -5288 H H H H H 3-0(=U)F 3 1 -5289 H H H H H 4-0(=U)CF 3 1 -5290 H H H H H 2-UC(=0)NH2 1 -5291 H H H H H 3-UC(=0)NH 2 1 -5292 H H H H H 4-U0(=U)NH 2 1 -5293 H H H H H 2-UC(=0)NHCH 3 1 -5294 H H H H H 3-UC(=0)NHCH 3 1 -5295 H H H H H 4-00(=U)NHCH 3 1 -5296 H H H H H 2-0(=U)N (H 3) 2 1 -5297 H H H H H 3-0(=U)N (H 3) 2 1 -5298 H H H H H 4-C(=0)N (GH 3)2 1 -5299 H H H H H 2-CH 2 00(=0)NH 2 1 -5300 H H H H H 3-CH 2 00(=0)NH 2 1 -5301 H H H H H 4-0H 200(=)NH 2 1 -5302 H H H H H 2-GH 2 00(=U)NHCH 3 1 -5303 H H H H H 3-GH 2 00(=U)NHCH 3 1 -5304 H H H H H 4-CH 2 00(=0)NHCH 3 1 -5305 H H H H H 2-0H 200(=O)N (H 3 3)2 -5306 H H H H H 3-0H 200(=O)N (H 3 3)2 -5307 H H H H H 4-0H 200(=O)N (H 3 3)2 -5308 H H H H H 2-0C(=0)0H3 1 -5309 H H H H H 3-0C(=0)0H3 1 -5310 H H H H H 4-U0(=U)0H3 1 -5311 H H H H H 2-GH 20(=0)0H 3 1 -5312 H H H H H 3-GH 20(=U)0H 3 1 -5313 H H H H H 4-0H 20(=U)0H 3 1 -5314 H H H H H 2-GH 20(=U)CH 3 1 -5315 H H H H H 3-0H 20(=U)CH 3 1 -5316 H H H H H 4-GH 20(=U)0H 3 1 -5317 H H H H H 2-U S=0)2CH 3 -5318 H H H H H 3-OS=U)20 3 -5319 H H H H H 4-OS=U)20 3 -5320 H H H H H 2-CH 2 SCH 3 1 -5321 H H H H H 3-CH 2SH 3 1 -5322 H H H H H 4-CH 2 SCH 3 -5323 H H H H H 2-CH 2 S(=U)CH 3 -5324 H H H H H 3-CH 2 S=0)GH 3 1 -5325 H H H H H 4-CH 2 S(=U)CH 3 -5326 H H H H H 2-CH 2S=U)20 3 1 -5327 H H H H H 3-CH 2S(=U) 2 CH3 -5328 H H H H H 4-CH 2S(=U) 2 CH3 -5329 H H H H H 2-CH 2SO F 3 -5330 H H H H H 3-CH 2SC F 3 -5331 H H H H H 4-CH 2SO F 3 -5332 H H H H H 2-CH 2 S(=U)CF 3 -5333 H H H H H 3-CH 2 S(=U)CF 3 -5334 H H H H H 4-CH 2 S(=0)CF 3 -5335 H H H H H 2-CH 2S=0) 2CF 3 -5336 H H H H H 3-CH 2 S(=) 20 3 -5337 H H H H H 4-CH 2S=U)20F 3
[0347]
[Table 222]
com pound R' R2 R R4 R (Rd)m P C-5338 H H H H H 2-phenyl 1 C-5339 H H H H H 3-phenyl 1 C-5340 H H H H H 4-phenyl 1 C-5341 H H H H H 2-(phenylbxy) 1 C-5342 H H H H H 3-(phenylbxy) 1 C-5343 H H H H H 4-(phenylbxy) 1 C-5344 H H H H H 2-benzyl 1 C-5345 H H H H H 3-benzyl 1 C-5346 H H H H H 4-benzyl 1 C-5347 H H H H H 2-(benzybxy) 1 C-5348 H H H H H 3-(benzybxy) 1 C-5349 H H H H H 4-(benzybxy) 1 C-5350 H H H H H 2-((2-fluorobenzyDoxy) 1 C-5351 H H H H H 3-((2-fluorobenzyDoxy) 1 C-5352 H H H H H 4-((2-fluorobenzyDoxy) 1 C-5353 H H H H H 2-((3-fluorobenzyDoxy) 1 C-5354 H H H H H 3-((3-fluorobenzyDoxy) 1 C-5355 H H H H H 4-((3-fluorobenzyDoxy) 1 C-5356 H H H H H 2-((4-fluorobenzyDoxy) 1 C-5357 H H H H H 3-((4-fluorobenzyDoxy) 1 C-5358 H H H H H 4-((4-fluorobenzyDoxy) 1 C-5359 H H H H H 2-((2-ch brobenzy Doxy) 1 C-5360 H H H H H 3-((2-ch brobenzy Doxy) 1 C-5361 H H H H H 4-((2-ch brobenzy Doxy) 1 C-5362 H H H H H 2-((3-ch brobenzy Doxy) 1 C-5363 H H H H H 3-((3-ch brobenzy Doxy) 1 C-5364 H H H H H 4-((3-ch brobenzy Doxy) 1 C-5365 H H H H H 2-((4-ch brobenzy Doxy) 1 C-5366 H H H H H 3-((4-ch brobenzy Doxy) 1 C-5367 H H H H H 4-((4-ch brobenzy Doxy) 1 C-5368 H H H H H 2-((2-methylbenzyDoxy) 1 C-5369 H H H H H 3-((2-methylbenzyDoxy) 1 C-5370 H H H H H 4-((2-methylbenzyDoxy) 1 C-5371 H H H H H 2-((3-methylbenzyDoxy) 1 C-5372 H H H H H 3-((3-methylbenzyDoxy) 1 C-5373 H H H H H 4-((3-methylbenzyDoxy) 1 C-5374 H H H H H 2-((4-methylbenzyDoxy) 1 C-5375 H H H H H 3-((4-methylbenzyDoxy) 1 C-5376 H H H H H 4-((4-methylbenzyDoxy) 1 C-5377 H H H H H 2-((2-(trifluorom ethyDbenzyDoxy) 1 C-5378 H H H H H 3-((2-(trifluorom ethyDbenzyDoxy) 1 C-5379 H H H H H 4-((2-(trifluorom ethyDbenzyDoxy) 1 C-5380 H H H H H 2-((3-(trifluorom ethyDbenzyDoxy) 1 C-5381 H H H H H 3-((3-(trifluorom ethyDbenzyDoxy) 1 C-5382 H H H H H 4-((3-(trifluorom ethyDbenzyDoxy) 1 C-5383 H H H H H 2-((4-(trifluorom ethyDbenzyDoxy) 1 C-5384 H H H H H 3-((4-(trifluorom ethyDbenzyDoxy) 1 C-5385 H H H H H 4-((4-(trifluorom ethyDbenzyDoxy) 1 C-5386 H H H H H 2-((2-m ethoxybenzyl)oxy) 1 C-5387 H H H H H 3-((2-m ethoxybenzyl)oxy) 1 C-5388 H H H H H 4-((2-m ethoxybenzyl)oxy) 1 C-5389 H H H H H 2-((3-m ethoxybenzy)oxy) 1 C-5390 H H H H H 3-((3-m ethoxybenzyl)oxy) 1 C-5391 H H H H H 4-((3-m ethoxybenzy)oxy) 1 C-5392 H H H H H 2-((4-m ethoxybenzyl)oxy) 1 C-5393 H H H H H 3-((4-m ethoxybenzy)oxy) 1 0-5394 H H H H H 4-((4-m ethoxybenzyl)oxy) 1
[0348]
[Table 223]
com pound R' R2 Rj R4 Rp)m P C-5395 H H H H H 2-((2-(trifluorom ethoxy)benzyDoxy) 1 C-5396 H H H H H 3-((2-(trifluorom ethoxy)benzyDoxy) 1 C-5397 H H H H H 4-((2-(trifluorom ethoxy)benzyDoxy) 1 C-5398 H H H H H 2-((3-(trifluoromethoxy)benzyDoxy) 1 C-5399 H H H H H 3-((3-(trifluorom ethoxy)benzyDoxy) 1 C-5400 H H H H H 4-((3-(trifluorom ethoxy)benzyDoxy) 1 C-5401 H H H H H 2-((4-(trifluorom ethoxy)benzyDoxy) 1 C-5402 H H H H H 3-((4-(trifluorom ethoxy)benzyDoxy) 1 C-5403 H H H H H 4-((4-(trifluorom ethoxy)benzyDoxy) 1 C-5404 H H H H H 2-((2-(m e thb)benzyloxy) 1 C-5405 H H H H H 3-((2-(m ethylthb)benzyDoxy) 1 C-5406 H H H H H 4-((2-(m ethylthb)benzyDoxy) 1 C-5407 H H H H H 2-((3-(m ethylthb)benzyDoxy) 1 C-5408 H H H H H 3-((3-(m ethylthb)benzyDoxy) 1 C-5409 H H H H H 4-((3-(m ethylthb)benzyloxy) 1 C-5410 H H H H H 2-((4-(m ethylthb)benzyDoxy) 1 C-5411 H H H H H 3-((4-(m ethylthb)benzyDoxy) 1 C-5412 H H H H H 4-((4-(m ethylthb)benzyDoxy) 1 C-5413 H H H H H 2-((2-(methyIsuftinyDbenzyDoxy) 1 C-5414 H H H H H 3-((2-(iethyIsulfinyDbenzyDoxy) 1 C-5415 H H H H H 4-((2-(iethyIsulfinyDbenzyDoxy) 1 C-5416 H H H H H 2-((3-(methyIsulfinyDbenzyDoxy) 1 C-5417 H H H H H 3-((3-(methyIsulfinyDbenzyDoxy) 1 C-5418 H H H H H 4-((3-(methyIsulfinyDbenzyDoxy) 1 C-5419 H H H H H 2-((4- (ethyIsulfinyDbenzyDoxy) 1 C-5420 H H H H H 3-((4-(iethyIsulfinyDbenzyDoxy) 1 C-5421 H H H H H 4-((4-(iethyIsulfinyDbenzyDoxy) 1 C-5422 H H H H H 2-((2-(iethyIsulfonyDbenzyDoxy) 1 C-5423 H H H H H 3-((2-(iethyIsulfonyDbenzyDoxy) 1 C-5424 H H H H H 4-((2- (ethyIsulfonyDbenzyDoxy) 1 C-5425 H H H H H 2-((3-(iethyIsulfonyDbenzyDoxy) 1 C-5426 H H H H H 3-((3- (ethyIsulfonyDbenzyDoxy) 1 C-5427 H H H H H 4-((3-m ethyIsulfonyDbenzyDoxy) 1 C-5428 H H H H H 2-((4-m ethyIsulfonyDbenzyDoxy) 1 C-5429 H H H H H 3-((4- (ethyIsulfonyDbenzyDoxy) 1 C-5430 H H H H H 4-((4- (ethyIsulfonyDbenzyDoxy) 1 C-5431 H H H H H 2-((2-(trifluoromethythio)benzylDoxy) 1 C-5432 H H H H H 3-((2-(trifluorom ethylthio)benzyDoxy) 1 C-5433 H H H H H 4-((2-(trifluorom ethylthio)benzyDoxy) 1 C-5434 H H H H H 2-((3-(trifluorom ethylthio)benzyDoxy) 1 C-5435 H H H H H 3-((3-(trifluorom ethylthio)benzyDoxy) 1 C-5436 H H H H H 4-((3-(trifluorom ethylthio)benzyDoxy) 1 C-5437 H H H H H 2-((4-(trifluorom ethythio)benzyDoxy) 1 C-5438 H H H H H 3-((4-(trifluorom ethythio)benzyDoxy) 1 C-5439 H H H H H 4-((4-(trifluorom ethythio)benzyDoxy) 1 C-5440 H H H H H 2-((2-(trifluorom ethysufthy)benzy)oxy) 1 C-5441 H H H H H 3-((2-(trifluorom ethyIsulfhyDbenzyI)oxy) 1 C-5442 H H H H H 4-((2-(trifluorom ethyIsulfhyDbenzyI)oxy) 1 C-5443 H H H H H 2-((3-(trifluorom ethyIsulfhyDbenzyI)oxy) 1 C-5444 H H H H H 3-((3-(trifluorom ethyIsulfhyDbenzyI)oxy) 1 C-5445 H H H H H 4-((3-(trifluorom ethyIsulfhyDbenzyI)oxy) 1 C-5446 H H H H H 2-((4-(trifluorom ethyIsulfhyDbenzyI)oxy) 1 C-5447 H H H H H 3-((4-(trifluorom ethyIsulfhyDbenzyI)oxy) 1 C-5448 H H H H H 4-((4-(trifluorom ethyIsulfhyDbenzyI)oxy) 1 C-5449 H H H H H 2-((2-(trifluorom ethylsuIfonyDbenzyDoxy) 1 C-5450 H H H H H 3-((2-(trifluorom ethylsuIfonyDbenzyDoxy) 1 C-5451 H H H H H 4-((2-(trifluorom ethylsulfonyDbenzyDoxy) 1
[0349]
[Table 224]
com pound R R2 R R (R)m P C-5452 H H H H H 2-((3-(trifluorom ethy u fbnyDbenzy Doxy) 1 C-5453 H H H H H 3-((3-(trifluorom ethy u fbnyDbenzy Doxy) 1 C-5454 H H H H H 4-((3-(trifluorom ethy u fbnyDbenzyDoxy) 1 C-5455 H H H H H 2-((4-(trifluorom ethy u fbnyDbenzy Doxy) 1 C-5456 H H H H H 3-((4-(trifluorom ethy su fbnyDbenzyDoxy) 1 C-5457 H H H H H 4-((4-(trifluorom ethy u fbnyDbenzy Doxy) 1 C-5458 H H H H H 2-((2-am inobenzy Doxy) 1 C-5459 H H H H H 3-((2-am inobenzy Doxy) 1 C-5460 H H H H H 4-((2-am inobenzy Doxy) 1 C-5461 H H H H H 2-((3-am inobenzy Doxy) 1 C-5462 H H H H H 3-((3-am inobenzy Doxy) 1 C-5463 H H H H H 4-((3-am inobenzy Doxy) 1 C-5464 H H H H H 2-((4-am inobenzy Doxy) 1 C-5465 H H H H H 3-((4-am inobenzy Doxy) 1 C-5466 H H H H H 4-((4-am inobenzy Doxy) 1 C-5467 H H H H H 2-((2- nethy bm ino)benzy Doxy) 1 C-5468 H H H H H 3-((2- nethy bm ino)benzy Doxy) 1 C-5469 H H H H H 4-((2- nethy bm ino)benzy Doxy) 1 C-5470 H H H H H 2-((3- nethy bm ino)benzy Doxy) 1 C-5471 H H H H H 3-((3- nethy bm ino)benzy Doxy) 1 C-5472 H H H H H 4-((3-n ethy bm ino)benzy Doxy) 1 C-5473 H H H H H 2-((4-n ethy bm ino)benzy Doxy) 1 C-5474 H H H H H 3-((4-n ethy bm ino)benzy Doxy) 1 C-5475 H H H H H 4-((4- nethy bm ino)benzy Doxy) 1 C-5476 H H H H H 2-((2-(d hm ethy bm ino)benzyI)oxy) 1 C-5477 H H H H H 3-((2-(d hm ethy bm ino)benzyI)oxy) 1 C-5478 H H H H H 4-((2-(d hm ethy bm ino)benzyI)oxy) 1 C-5479 H H H H H 2-((3-(d hm ethy bm ino)benzyI)oxy) 1 C-5480 H H H H H 3-((3-(d m ethy bm ino)benzyI)oxy) 1 C-5481 H H H H H 4-((3-(d hm ethy bm ino)benzyI)oxy) 1 C-5482 H H H H H 2-((4-(d ethy bm ino)benzy)oxy) 1 C-5483 H H H H H 3-((4-(d hm ethy bm ino)benzy)oxy) 1 C-5484 H H H H H 4-((4-(d hm ethy bm ino)benzy)oxy) 1 C-5485 H H H H H 2-((2-cyanobenzy Doxy) 1 C-5486 H H H H H 3-((2-cyanobenzy Doxy) 1 C-5487 H H H H H 4-((2-cyanobenzy Doxy) 1 C-5488 H H H H H 2-((3-cyanobenzy Doxy) 1 C-5489 H H H H H 3-((3-cyanobenzy Doxy) 1 C-5490 H H H H H 4-((3-cyanobenzy Doxy) 1 C-5491 H H H H H 2-((4-cyanobenzy Doxy) 1 C-5492 H H H H H 3-((4-cyanobenzy Doxy) 1 C-5493 H H H H H 4-((4-cyanobenzy Doxy) 1 C-5494 H H H H H 2-((2-nitrobenzy Doxy) 1 C-5495 H H H H H 3-((2-nitrobenzy Doxy) 1 C-5496 H H H H H 4-((2-nitrobenzy Doxy) 1 -5497 H H H H H 2-((3-nitrobenzy Doxy) 1 -5498 H H H H H 3-((3-nitrobenzy Doxy) 1 C-5499 H H H H H 4-((3-nitrobenzy Doxy) 1 -5500 H H H H H 2-((4-nitrobenzy Doxy) 1 C-5501 H H H H H 3-((4-nitrobenzyDoxy) 1 -5502 H H H H H 4-((4-nitrobenzy Doxy) 1 C-5503 H H H H H 2-NH 2 1 C-5504 H H H H H 3-NH 2 1 C-5505 H H H H H 4-NH 2 1 C-5506 H H H H H 2-NHM e 1 C-5507 H H H H H 3-NHM e 1 C-5508 H H H H H 4-NHM e 1
[0350]
[Table 225]
com pound R' R2 R- R44 R (Rd)m P C-5509 H H H H H 2-NH Et 1 C-5510 H H H H H 3-NH Et 1 C-5511 H H H H H 4-NH Et 1 C-5512 H H H H H 2-N (M e) 2 C-5513 H H H H H 3-N (M e) 2 C-5514 H H H H H 4-N (M e) 2 C-5515 H H H H H 2-N(Et) 2 C-5516 H H H H H 3-N (Et 2 C-5517 H H H H H 4-N (Et 2 C-5518 H H H H H 2-CHO 1 C-5519 H H H H H 3-CHO 1 C-5520 H H H H H 4-CHO 1 C-5521 H H H H H 2-C (=0)0H 1 C-5522 H H H H H 3-C (=0)0H 1 C-5523 H H H H H 4-C (=0)0H 1 C-5524 H H H H H 2-0,3-dioxolan-2-yD 1 C-5525 H H H H H 3-0,3-dioxolan-2-yD 1 C-5526 H H H H H 4-0,3-dioxolan-2-yD 1 C-5527 H H H H H 2-0,3-dioxan-2-yD 1 C-5528 H H H H H 3-0,3-dioxan-2-yD 1 C-5529 H H H H H 4-0,3-dioxan-2-yD 1 C-5530 H H H H H 2-/(1H-n idazol-2-yD 1 C-5531 H H H H H 3-(1H-in idazol-2-yD 1 C-5532 H H H H H 4-(1H-i idazol-2-yD 1 C-5533 H H H H H 2-(thiazol-2-y) 1 C-5534 H H H H H 3-(thiazol-2-y) 1 C-5535 H H H H H 4-(thiazol-2-yD 1 C-5536 H H H H H 2-(oxazol-2-yl) 1 C-5537 H H H H H 3-(oxazol-2-yl) 1 C-5538 H H H H H 4-(oxazol-2-yl) 1 C-5539 H H H H H 2-CH=N0H 1 C-5540 H H H H H 3-CH=N0H 1 C-5541 H H H H H 4-CH=N0H 1 C-5542 H H H H H 2-CH=NOMe 1 C-5543 H H H H H 3-CH=NOMe 1 C-5544 H H H H H 4-CH=NOMe 1 C-5545 H H H H H 2-(4,5-d hydro-3-isoxazolyl) 1 C-5546 H H H H H 3-(4,5-dhydro-3-isoxazolyl) 1 C-5547 H H H H H 4-(4,5-dhydro-3-isoxazolyl) 1 C-5548 H H H H H 2-CN 1 C-5549 H H H H H 3-CN 1 C-5550 H H H H H 4-CN 1 C-5551 H H H H H 2-N0 2 1 C-5552 H H H H H 3-N0 2 1 C-5553 H H H H H 4-N0 2 1 C-5554 H H H H H 2,3- 2 1 C-5555 H H H H H 2,4-F 2 1 C-5556 H H H H H 2,5-F 2 1 C-5557 H H H H H 2,6-F 2 1 C-5558 H H H H H 3,4- 2 1 C-5559 H H H H H 3,5-F 2 1 C-5560 H H H H H 2-F,3-CI 1 C-5561 H H H H H 2-F,4-CI 1 C-5562 H H H H H 2-F,5-CI 1 C-5563 H H H H H 2-F,6-CI 1 C-5564 H H H H H 3-F,2-CI 1 C-5565 H H H H H 3-F,4-CI 1
[0351]
[Table 226]
com pound R' R2 R R4 R (Rd)m P C-5566 H H H H H 3-F,5-CI 1 C-5567 H H H H H 3-F,6-CI 1 C-5568 H H H H H 4-F,2-CI 1 C-5569 H H H H H 4-F,3-CI 1 C-5570 H H H H H 2-F,3-Ae 1 C-5571 H H H H H 2-F,4-MA e 1 C-5572 H H H H H 2-F,5-MA e 1 C-5573 H H H H H 2-F,6-MA e 1 C-5574 H H H H H 3-F,2-MA e 1 C-5575 H H H H H 3-F,4-MAe 1 C-5576 H H H H H 3-F,5-MA e 1 C-5577 H H H H H 3-F,6-MA e 1 C-5578 H H H H H 4-F,2-M e 1 C-5579 H H H H H 4-F,3-M e 1 C-5580 H H H H H 2-F,3-CF, 1 C-5581 H H H H H 2-F,4-CF, 1 C-5582 H H H H H 2-F,5-CF 1 C-5583 H H H H H 2-F,6- 1 C-5584 H H H H H 3-F,2- 1 C-5585 H H H H H 3-F,4- 1 C-5586 H H H H H 3-F,5-CF3 1 C-5587 H H H H H 3-F,6-CF 1 C-5588 H H H H H 4-F,2-CF 1 C-5589 H H H H H 4-F,3--CF 1 C-5590 H H H H H 2-F,3-0Me 1 C-5591 H H H H H 2-F,4-0Me 1 C-5592 H H H H H 2-F,5-0Me 1 C-5593 H H H H H 2-F,6-0Me 1 C-5594 H H H H H 3-F,2-0Me 1 C-5595 H H H H H 3-F,4-0Me 1 C-5596 H H H H H 3-F,5-0Me 1 C-5597 H H H H H 3-F,6-0Me 1 C-5598 H H H H H 4-F,2-0Me 1 C-5599 H H H H H 4-F,3-0Me 1 C-5600 H H H H H 2,3-C 1 C-5601 H H H H H 2,4-C 1 C-5602 H H H H H 2,b-L 1 C-5603 H H H H H 2,6-C 1 C-5604 H H H H H 3,4-C 1 C-5605 H H H H H 3,5-C 1 C-5606 H H H H H 2-CI,3-Me 1 C-5607 H H H H H 2-CI,4-Me 1 C-5608 H H H H H 2-CI,5-M e 1 C-5609 H H H H H 2-CI,6-Me 1 C-5610 H H H H H 3-CI,2-Me 1 C-5611 H H H H H 3-CI,4-Me 1 C-5612 H H H H H 3-C,5-Me 1 C-5613 H H H H H 3-CI,6-Me 1 C-5614 H H H H H 4-CI,2-Me 1 C-5615 H H H H H 4-CI,3-Me 1 C-5616 H H H H H 2-C1,3-CF 3 1 C-5617 H H H H H 2-CI,4-CF 3 1 C-5618 H H H H H 2-CI,5-CF 3 1 C-5619 H H H H H 2-CI,6-CF 3 1 C-5620 H H H H H 3-CI,2-CF 3 1 C-5621 H H H H H 3-CI,4-CF 3 1 C-5622 H H H H H 3-Cb-CF 3 1
[0352]
[Table 227]
com pound R' R2 R R4 R (Rd)m P C-5623 H H H H H 3-C1,6-CF 1 C-5624 H H H H H 4-C1,2-CF 1 C-5625 H H H H H 4-C1,3- 3 1 C-5626 H H H H H 2-CI,3-0Me 1 C-5627 H H H H H 2-CI,4-0Me 1 C-5628 H H H H H 2-C,5-0Me 1 C-5629 H H H H H 2-C1,6-0Me 1 C-5630 H H H H H 3-CI,2-0Me 1 C-5631 H H H H H 3-CI,4-0Me 1 C-5632 H H H H H 3-CI,5-0Me 1 C-5633 H H H H H 3-C1,6-0Me 1 C-5634 H H H H H 4-CI,2-0Me 1 C-5635 H H H H H 4-CI,3-0Me 1 C-5636 H H H H H 2,3-e 2 1 C-5637 H H H H H 2,4-M e 2 1 C-5638 H H H H H 2,5-MAe 2 C-5639 H H H H H 2,6-MAe 2 C-5640 H H H H H 3,4-M e 2 1 C-5641 H H H H H 3,b-M e 2 1 C-5642 H H H H H 2-M e,3-CF 3 1 C-5643 H H H H H 2-M e,4-CF3 1 C-5644 H H H H H 2-M e,5-CF3 1 C-5645 H H H H H 2-M e,6-CF3 1 C-5646 H H H H H 3-M e,2-F 3 1 C-5647 H H H H H 3-M e,4-CF3 1 C-5648 H H H H H 3-M e,5-CF3 1 C-5649 H H H H H 3-M e,6-CF3 1 C-5650 H H H H H 4-M e,2-CF 3 1 C-5651 H H H H H 4-M e,3-CF 3 1 C-5652 H H H H H 2-M e,3-0Me 1 C-5653 H H H H H 2-M e,4-0Me 1 C-5654 H H H H H 2-Me,5-0Me 1 C-5655 H H H H H 2-M e,6-0Me 1 C-5656 H H H H H 3-M e,2-0Me 1 C-5657 H H H H H 3-M e,4-0Me 1 C-5658 H H H H H 3-Me,5-0 Me 1 C-5659 H H H H H 3-M e,6-0Me 1 C-5660 H H H H H 4-M e,2-0Me 1 C-5661 H H H H H 4-M e,3-0Me 1 C-5662 H H H H H 2,3-0Me 2 1 C-5663 H H H H H 2,4-0M e 2 1 C-5664 H H H H H 2,b-0Me 2 1 C-5665 H H H H H 2,6-0M e 2 1 C-5666 H H H H H 3,4-0Me 2 1 C-5667 H H H H H 3,5-0Me 2 1 C-5668 H H H H H 2-0Me,3-F 3 1 C-5669 H H H H H 2-0Me,4-CF 3 1 C-5670 H H H H H 2-0Me,5-CF 3 1 C-5671 H H H H H 2-0Me,6-CF 3 1 C-5672 H H H H H 3-0Me,2-F 3 1 C-5673 H H H H H 3-0Me,4-CF 3 1 C-5674 H H H H H 3-0Me,5-CF 3 1 C-5675 H H H H H 3-0Me,6-CF 3 1 C-5676 H H H H H 4-0Me,2-CF 3 1 C-5677 H H H H H 4-0Me,3- F3 1 C-5678 H H H H H 2-CH F 2,3-F 1 C-5679 H H H H H 2-CH F 2,4-F 1
[0353]
[Table 228]
com pound R' R2 R R4 R (Rd)m P C-5680 H H H H H 2-CH F 2,5-F 1 C-5681 H H H H H 2-CH F 2,6-F 1 C-5682 H H H H H 2-CH F 2,3-M e 1 C-5683 H H H H H 2-CH F 2,4-ie 1 C-5684 H H H H H 2-CHF 2,b- e C-5685 H H H H H 2-CH F 2,6-4e 1 C-5686 H H H H H 2-cycbpropyl,3-F 1 C-5687 H H H H H 2-cycbpropyl,4-F 1 C-5688 H H H H H 2-cycbpropyl,5-F 1 C-5689 H H H H H 2-cycbpropyl,6-F 1 C-5690 H H H H H 2-cycbpropyl,3-M e 1 C-5691 H H H H H 2-cycbpropyl,4-M e 1 C-5692 H H H H H 2-cycbpropyl,5-Me 1 C-5693 H H H H H 2-cycbpropyl,6-M e 1 C-5694 H H H H H 2-ethenyl,3-F 1 C-5695 H H H H H 2-ethenyl,4-F 1 C-5696 H H H H H 2-ethenyl,5-F 1 C-5697 H H H H H 2-ethenyl,6-F 1 C-5698 H H H H H 2-ethenyl,3-M e 1 C-5699 H H H H H 2-ethenyl,4-M e 1 C-5700 H H H H H 2-ethenyl1,5-Me 1 C-5701 H H H H H 2-ethenyl,6-M e 1 C-5702 H H H H H 2-0 Et,3-F 1 C-5703 H H H H H 2-0 Et4-F 1 C-5704 H H H H H 2-0 Et,5-F 1 C-5705 H H H H H 2-0 Et,6-F 1 C-5706 H H H H H 2-0Et,3-C| 1 C-5707 H H H H H 2-0Et,4-C| 1 C-5708 H H H H H 2-0Et,5-C| 1 C-5709 H H H H H 2-0Et,6-C| 1 C-5710 H H H H H 2-0Et3-Me 1 C-5711 H H H H H 2-0Et4-Me 1 C-5712 H H H H H 2-0Et5-Me 1 C-5713 H H H H H 2-0Et6-Me 1 C-5714 H H H H H 2-0Pr,3-F 1 C-5715 H H H H H 2-0Pr,4-F 1 C-5716 H H H H H 2-0Pr,5-F 1 C-5717 H H H H H 2-0Pr,6-F 1 C-5718 H H H H H 2-0 Pr,3-M e 1 C-5719 H H H H H 2-0 Pr,4-M e 1 C-5720 H H H H H 2-0 Pr,5-M e 1 C-5721 H H H H H 2-0 Pr,6-M e 1 C-5722 H H H H H 2-0 (/-Pr),3-F 1 C-5723 H H H H H 2-0 (/-Pr),4-F 1 C-5724 H H H H H 2-0 (/-Pr),5-F 1 C-5725 H H H H H 2-0 (/-Pr),6-F 1 C-5726 H H H H H 2-0 (/-Pr),3-M e 1 C-5727 H H H H H 2-0 (/-Pr),4-M e 1 C-5728 H H H H H 2-0 (/Pr),5--Me 1 C-5729 H H H H H 2-0 (/-Pr),6-M e 1 C-5730 H H H H H 2-0 CF,3-F 1 C-5731 H H H H H 2-0 CF3,4-F 1 C-5732 H H H H H 2-0 CF3 ,5-F 1 C-5733 H H H H H 2-0 CF3 ,6-F 1 C-5734 H H H H H 2-0 CF 3 ,3-M e 1 C-5735 H H H H H 2-0 CF3 ,4-M e 1 C-5736 H H H H H 2-0 CF 3 ,5-e 1
[0354]
[Table 229]
com pound R' R2 R- R44 R (Rd)m P C-5737 H H H H H 2-O0CF 3 ,6-Me 1 C-5738 H H H H H 2-OCHF 2,3-F 1 C-5739 H H H H H 2-OCHF 2,4-F 1 C-5740 H H H H H 2-OCHF 2,b-F 1 C-5741 H H H H H 2-OCHF 2,6-F C-5742 H H H H H 2-0CHF 2 ,3-Me 1 C-5743 H H H H H 2-0 CH F 2,4-M e 1 C-5744 H H H H H 2-0 CH F 2 ,5-M e 1 C-5745 H H H H H 2-0 CH F 2 ,6-M e 1 C-5746 H H H H H 2-(cycobpropybxy),3-F 1 C-5747 H H H H H 2-(cycobpropybxy),4-F 1 C-5748 H H H H H 2-(cycobpropybxy),5-F 1 C-5749 H H H H H 2-(cycobpropybxy),6-F 1 C-5750 H H H H H 2-(cycbpropybxy),3-M e 1 C-5751 H H H H H 2-(cycbpropybxy),4-M e 1 C-5752 H H H H H 2-(cycbpropybxy),5-M e 1 C-5753 H H H H H 2-(cycbpropybxy),6-Me 1 C-5754 H H H H H 2-(oxiran-2-yl),3-F 1 C-5755 H H H H H 2-(oxiran-2-yl),4-F 1 C-5756 H H H H H 2-(oxiran-2-yl),5-F 1 C-5757 H H H H H 2-(oxiran-2-y),6-F 1 C-5758 H H H H H 2-(oxiran-2-yD,3-Me 1 C-5759 H H H H H 2-(oxiran-2-yD,4-Me 1 C-5760 H H H H H 2-(oxiran-2-yD,5-M e 1 C-5761 H H H H H 2-(oxiran-2-yD,6-Me 1 C-5762 H H H H H 2-(oxiran-2-y IethyD,3-F 1 C-5763 H H H H H 2-(oxiran-2-y IethyD,4-F 1 C-5764 H H H H H 2-(oxiran-2-y IethyD,5-F 1 C-5765 H H H H H 2-(oxiran-2-y IethyD,6-F 1 C-5766 H H H H H 2-(oxiran-2-yh ethyD,3-Me 1 C-5767 H H H H H 2-(oxiran-2-y hethyD,4-Me 1 C-5768 H H H H H 2-(oxiran-2-yh ethyD,5-Me 1 C-5769 H H H H H 2-(oxiran-2-yh ethyD,6-Me 1 C-5770 H H H H H 2-SMe,3-F 1 C-5771 H H H H H 2-SMe,4-F 1 C-5772 H H H H H 2-SMe,5-F 1 C-5773 H H H H H 2-SMe,6-F 1 C-5774 H H H H H 2-SMe,3-M e 1 C-5775 H H H H H 2-SMe,4-M e 1 C-5776 H H H H H 2-SMe,5-Me 1 C-5777 H H H H H 2-SMe,6-M e 1 C-5778 H H H H H 2-SEt,3-F 1 C-5779 H H H H H 2-SEt,4-F 1 C-5780 H H H H H 2-SEt,5-F 1 C-5781 H H H H H 2-SEt,6-F 1 C-5782 H H H H H 2-SEt,3-M e 1 C-5783 H H H H H 2-SEt,4-M e 1 C-5784 H H H H H 2-SEt,5-M e 1 C-5785 H H H H H 2-SEt,6-M e 1 C-5786 H H H H H 2-S (=0)M e,3-F 1 C-5787 H H H H H 2-S (=0)M e,4-F 1 C-5788 H H H H H 2-S (=0)M e,5-F 1 -5789 H H H H H 2-S (=0)M e,6-F 1 C-5790 H H H H H 3-S (=0)M e,2-F 1 -5791 H H H H H 3-S (=0)M e,4-F 1 C-5792 H H H H H 3-S (=0)M e,5-F 1 -5793 H H H H H 3-S (=0)M e,6-F 1
[0355]
[Table 230]
com pound R R2 R R (R)m P C-5794 H H H H H 2-S(=0)Me,3-M e 1 C-5795 H H H H H 2-S(=0)Me,4-M e 1 C-5796 H H H H H 2-S(=0)Me,5-M e 1 C-5797 H H H H H 2-S(=0)Me,6-M e 1 C-5798 H H H H H 3-S(=0)Me,2-Me 1 C-5799 H H H H H 3-S(=0)Me,4-M e 1 C-5800 H H H H H 3-S(=0)Me,5-M e 1 C-5801 H H H H H 3-S(=0)Me,6-M e 1 C-5802 H H H H H 2-S (=0) 2 M e,3-F 1 C-5803 H H H H H 2-S (=0) 2M e,4-F 1 C-5804 H H H H H 2-S (=0) 2 M e,b-F 1 C-5805 H H H H H 2-S (=0) 2 M e,6-F 1 C-5806 H H H H H 2-S(=0) 2Me,3-M e 1 C-5807 H H H H H 2-S (=0) 2M e,4-M e 1 C-5808 H H H H H 2-S(=0) 2Me,5-M e 1 C-5809 H H H H H 2-S(=0) 2Me,6-M e 1 C-5810 H H H H H 2-SCF,,3-F 1 C-5811 H H H H H 2-SGa3,4-F 1 C-5812 H H H H H 2-SCF 3 ,b-F 1 C-5813 H H H H H 2-SCF 3,6-F 1 C-5814 H H H H H 2-SCF 3 ,3-M e 1 C-5815 H H H H H 2-SCF 3 ,4-M e 1 C-5816 H H H H H 2-SCF 3 ,5-M e 1 C-5817 H H H H H 2-SCF 3 ,6-M e 1 C-5818 H H H H H 2-S(=O)CF3 ,3-F 1 C-5819 H H H H H 2-S(=0)CF3 ,4-F 1 C-5820 H H H H H 2-S(=O)CF3 ,5-F 1 C-5821 H H H H H 2-S(=0)0F 3 ,6-F 1 C-5822 H H H H H 2-S(=0)CF 3 ,3-Me 1 C-5823 H H H H H 2-S(=0)CF3 ,4-Me 1 C-5824 H H H H H 2-S(=0)CF 3 5--Me 1 C-5825 H H H H H 2-S(=0)CF 3 ,6-Me 1 C-5826 H H H H H 2-S(=0) 2CF3 ,3-F 1 C-5827 H H H H H 2-S(=0) 2CF3 A,4-F 1 C-5828 H H H H H 2-S(=0) 2CF3 ,5-F 1 C-5829 H H H H H 2-S(=0) 2CF3 ,6-F 1 C-5830 H H H H H 2-S (=0)2CF3 ,3-M e 1 C-5831 H H H H H 2-S (=0)2CF3 .4- e 1 C-5832 H H H H H 2-S (=0)2CF3 ,b-M e 1 C-5833 H H H H H 2-S (=0)2CF3 ,6-M e 1 C-5834 H H H H H 2-(cycbpropylthio),3-F 1 C-5835 H H H H H 2-(cycbpropylthio),4-F 1 C-5836 H H H H H 2-(cycbpropylthio),5-F 1 C-5837 H H H H H 2-(cycbpropylthio),6-F 1 C-5838 H H H H H 2-(cycobpropylthio),3-Me 1 C-5839 H H H H H 2-(cycobpropylthio),4-M e 1 C-5840 H H H H H 2-(cycobpropylthio),5-M e 1 C-5841 H H H H H 2-(cycobpropylthio),6-Me 1 C-5842 H H H H H 2-C(=0)Me,3-F 1 C-5843 H H H H H 2-C(=0)Me,4-F 1 C-5844 H H H H H 2-C(=0)Me,5-F 1 C-5845 H H H H H 2-C(=0)Me,6-F 1 C-5846 H H H H H 2-C(=0)Me,3-M e 1 C-5847 H H H H H 2-C(=0)Me,4-M e 1 C-5848 H H H H H 2-C(=0)Me,5-M e 1 C-5849 H H H H H 2-C(=0)Me,6-M e 1 C-5850 H H H H H 3-C(=0)Me,2-F 1
[0356]
[Table 231]
com pound R R2 R R (R)m P C-5851 H H H H H 3-C(=0)Me,4-F 1 C-5852 H H H H H 3-C(=0)Me,5-F 1 C-5853 H H H H H 3-C(=0)Me,6-F 1 C-5854 H H H H H 3-C(=0)Me,2-M e 1 C-5855 H H H H H 3-C(=0)Me,4-Me 1 C-5856 H H H H H 3-C(=0)Me,5-M e 1 C-5857 H H H H H 3-C(=0)Me,6--M e 1 C-5858 H H H H H 2-C(=0)0Me,3 -F 1 C-5859 H H H H H 2-C(=0)0Me,4-F 1 C-5860 H H H H H 2-C(=0)0Me,5 -F 1 C-5861 H H H H H 2-C(=0)0Me,6 -F 1 C-5862 H H H H H 2-C(=0)0Me,3 -M e 1 C-5863 H H H H H 2-C(=0)0Me,4 -M e 1 C-5864 H H H H H 2-C(=0)0Me,5 -M e 1 C-5865 H H H H H 2-C(=0)0Me,6--M e 1 C-5866 H H H H H 2-C(=0)0Et3-F 1 C-5867 H H H H H 2-C(=0)0Et4-F 1 C-5868 H H H H H 2-C(=0)0Et5-F 1 C-5869 H H H H H 2-C(=0)0Et6-F 1 C-5870 H H H H H 2-C0(=)0Et,3-M e 1 C-5871 H H H H H 2-C0(=)0Et,4-Me 1 C-5872 H H H H H 2-C0(=)0Et,5-M e 1 C-5873 H H H H H 2-C0(=)0Et,6-M e 1 C-5874 H H H H H 2-C(=0)NH 2 ,3-F 1 C-5875 H H H H H 2-C (=0)NH 2 ,4-F 1 C-5876 H H H H H 2-C (=0)NH 2 ,5-F 1 C-5877 H H H H H 2-C (=0)NH 2 ,6-F 1 C-5878 H H H H H 2-C(=0)NH 2,3-M e 1 C-5879 H H H H H 2-C(=0)NH 2 ,4-M e 1 C-5880 H H H H H 2-C(=0)NH 2 ,5-M e 1 C-5881 H H H H H 2-C(=0)NH 2,6-M e 1 C-5882 H H H H H 2-C(=0)NHMe,3-F 1 C-5883 H H H H H 2-C(=0)NHMe,4-F 1 C-5884 H H H H H 2-C(=0)NHMe,5-F 1 C-5885 H H H H H 2-C(=0)NHMe,6-F 1 C-5886 H H H H H 2-C(=0)NHMe,3-M e 1 C-5887 H H H H H 2-C(=0)NHMe,4-M e 1 C-5888 H H H H H 2-C(=0)NHMe,5--M e 1 C-5889 H H H H H 2-C(=0)NHMe,6--M e 1 C-5890 H H H H H 2-C(=0)NMe 2,3-F 1 C-5891 H H H H H 2-C(=0)NMe 2,4-F 1 C-5892 H H H H H 2-C(=0)NMe 2,b- 1 C-5893 H H H H H 2-C(=0)NMe 2,6-F 1 C-5894 H H H H H 2-C(=0)NMe 2,3-Me 1 C-5895 H H H H H 2-C(=0)NMe 2,4-Me 1 C-5896 H H H H H 2-C(=0)NMe 2,b-Me 1 C-5897 H H H H H 2-C(=0)NMe 2 ,6-M e 1 C-5898 H H H H H 2-CH 20H,3-F 1 C-5899 H H H H H 2-CH20H,4-F 1 C-5900 H H H H H 2-CH 20H,5-F 1 C-5901 H H H H H 2-CH 20H,6-F 1 C-5902 H H H H H 2-CH20H,3-M e 1 C-5903 H H H H H 2-CH20H,4-M e 1 C-5904 H H H H H 2-CH20H,5-M e 1 C-5905 H H H H H 2-CH20H,6-M e 1 C-5906 H H H H H 2-CH 20CH 3 ,3-F 1 C-5907 H H H H H 2-CH 200H 3,44-F 1
[0357]
[Table 232]
com pound R' R2 R- R- R (R°)m P 0-5908 H H H H H 2-GH 20H 3,5-F -5909 H H H H H 2-GH 20H 3 ,6-F -5910 H H H H H 2-CH 2UCH 3 ,3-M e -5911 H H H H H 2-CH 2UCH 3 ,4-M e -5912 H H H H H 2-CH 2UCH 3 ,b-M e -5913 H H H H H 2-CH 2UCH 3 ,6- e1 -5914 H H H H H 2-GH 20H 2 CH 3 ,3-F 1 -5915 H H H H H 2-GH 2 0H 2 CH 3 ,4-F 1 -5916 H H H H H 2-GH 2 0H 2 CH 3 ,5-F 1 -5917 H H H H H 2-GH 20H 2CH 3 ,6- 1 -5918 H H H H H 2-GH 2UCH 2CH 3,3-M e 1 -5919 H H H H H 2-GH 2 0H 2CH 3 ,4-M e 1 -5920 H H H H H 2-GH 2UCH 2CH 3,b--M e 1 -5921 H H H H H 2-GH 2UCH 2CH 3,6-M e 1 -5922 H H H H H 2-0(=U)CH 3 ,3-F 1 -5923 H H H H H 2-0(=U)CH 3 ,4-F 1 -5924 H H H H H 2-0(=U)CH 3 ,5-F 1 -5925 H H H H H 2-0(=U)GH 3,6- 1 -5926 H H H H H 2-00(=U)CH 3 ,3-M e 1 -5927 H H H H H 2-0C(=U)CH 3,4-M e 1 -5928 H H H H H 2-00(=0)CH 3 ,5-Me 1 -5929 H H H H H 2-0(=U)CH 3 ,6-M e 1 -5930 H H H H H 2-OS(=U) 2CH 3,3-F 1 -5931 H H H H H 2-OS(=U) 20H 3,4-F 1 -5932 H H H H H 2-OS(=U) 2CH 3,5-F 1 -5933 H H H H H 2-OS(=U) 2CH 3,6-F 1 -5934 H H H H H 2-OS(=U) 2 CH 3 ,3-M e 1 -5935 H H H H H 2-OS(=U) 2CH 3 ,4-M e 1 -5936 H H H H H 2-OS(=U) 2CH 3 ,b-M e 1 -5937 H H H H H 2-OS(=U) 2 CH 3 ,6-M e 1 -5938 H H H H H 2-GH 2SCH 3 3-F 1 -5939 H H H H H 2-GH 2SOH 3,4-F 1 -5940 H H H H H 2-GH 2SOH 3,5-F 1 -5941 H H H H H 2-GH 2SOH 3,6-F 1 -5942 H H H H H 2-OH 2S0H 3,3-M e 1 -5943 H H H H H 2-OH 2S0H e 3,4-M 1 -5944 H H H H H 2-GH 2SCH 3,b-M e 1 -5945 H H H H H 2-GH 2SCH 3,6-M e 1 -5946 H H H H H 2-GH 2SCF 3 ,3-1 -5947 H H H H H 2-GH 2SCF 3 ,4-F -5948 H H H H H 2-GH 2SOF 3 ,5-F -5949 H H H H H 2-GH 2SCF 3 ,6-F -5950 H H H H H 2-OH 2S0F 3 ,3-M e -5951 H H H H H 2-GH 2SCF 3 ,4-M e -5952 H H H H H 2-OH 2 S0F 3 ,5-M e -5953 H H H H H 2-OH 2SCF 3 ,6-M e -5954 H H H H H 2-(benzyloxy),3-F 1 -5955 H H H H H 2-(benzyloxy),4-F 1 -5956 H H H H H 2-(benzyloxy),5-F 1 -5957 H H H H H 2-(benzyloxy),6-F 1 -5958 H H H H H 2-(benzy bxy),3-M e 1 -5959 H H H H H 2-(benzy bxy),4-M e 1 -5960 H H H H H 2-(benzy bxy),5-M e 1 -5961 H H H H H 2-(benzy bxy),6-M e 1 -5962 H H H H H 2-NH 2 ,3-F 1 -5963 H H H H H 2-NH 2 ,44 1 -5964 H H H H H 2-NH 2,b-H1
[0358]
[Table 233]
com pound R R2 R R (R)m P C-5965 H H H H H 2-NH 2 ,6-F 1 C-5966 H H H H H 2-NH 2,3-Me 1 C-5967 H H H H H 2-NH 2,4-Me 1 C-5968 H H H H H 2-NH 2,-Me 1 C-5969 H H H H H 2-NH 2,6-MAe C-5970 H H H H H 2-NHMe,3-F 1 C-5971 H H H H H 2-NHMe,4-F 1 C-5972 H H H H H 2-NHMe,5-F 1 C-5973 H H H H H 2-NHMe,6-F 1 C-5974 H H H H H 2-NHMe,3-M e 1 C-5975 H H H H H 2-NHMe,4-M e 1 C-5976 H H H H H 2-NHMe,5-M e 1 C-5977 H H H H H 2-NHMe,6-M e 1 C-5978 H H H H H 2-NHEt,3-F 1 C-5979 H H H H H 2-NHEt4-F 1 C-5980 H H H H H 2-NHEt,5-F 1 C-5981 H H H H H 2-NHEt,6-F 1 C-5982 H H H H H 2-NHEt,3-M e 1 C-5983 H H H H H 2-NHEt,4-Me 1 C-5984 H H H H H 2-NHEt,5-M e 1 C-5985 H H H H H 2-NHEt,6-M e 1 C-5986 H H H H H 2-NMe 2 ,3-F 1 C-5987 H H H H H 2-NMe 2 ,4-F 1 C-5988 H H H H H 2-NMe 2 ,5-F 1 C-5989 H H H H H 2-NMe 2 ,6-F 1 C-5990 H H H H H 2-NMe 2 ,3-M e 1 C-5991 H H H H H 2-NMe 2 ,4-M e 1 C-5992 H H H H H 2-NMe 2 ,b-M e 1 C-5993 H H H H H 2-NMe 2 ,6-M e 1 C-5994 H H H H H 2-NEt2,3-F 1 C-5995 H H H H H 2-NEt2,4-F 1 C-5996 H H H H H 2-NEt2,5-F 1 C-5997 H H H H H 2-NEt2,6-F 1 C-5998 H H H H H 2-NEt2,3-MAe 1 C-5999 H H H H H 2-NEt2,4-Me 1 C-6000 H H H H H 2-NEt2,5-Me 1 C-6001 H H H H H 2-NEt2,6-M e 1 C-6002 H H H H H 2-CHO,3-F 1 C-6003 H H H H H 2-CH04-F 1 C-6004 H H H H H 2-CHOT5-F 1 C-6005 H H H H H 2-CHO,6-F 1 C-6006 H H H H H 2-CHO,3-M e 1 C-6007 H H H H H 2-CHO,4-Me 1 C-6008 H H H H H 2-CHO,5-M e 1 C-6009 H H H H H 2-CHO,6-M e 1 C-6010 H H H H H 2-C(=0)0H,3-F 1 C-6011 H H H H H 2-C(=0)0H,4-F 1 C-6012 H H H H H 2-C (= )0 H ,5-F 1 C-6013 H H H H H 2-C(=0)0H,6-F 1 C-6014 H H H H H 2-C(=0)0H,3-M e 1 C-6015 H H H H H 2-C(=0)0H,4-M e 1 C-6016 H H H H H 2-C(=0)0H,5-M e 1 C-6017 H H H H H 2-C(=0)0H,6-M e 1 C-6018 H H H H H 2-(1,3-dbxolan-2-y1),3-F 1 C-6019 H H H H H 2-(1,3-dbxolan-2-yl)4-F 1 C-6020 H H H H H 2-(1,3-dbxolan-2-yl),5-F 1 C-6021 H H H H H 2-(1,3-dbxolan-2-y1),6-F 1
[0359]
[Table 234]
com pound R R2 R R (R)m P C-6022 H H H H H 2-0,3-dioxolan-2-yD,3-Me 1 C-6023 H H H H H 2-0,3-dioxolan-2-yD,4-Me 1 C-6024 H H H H H 2-0,3-dioxolan-2-yD,5-M e 1 C-6025 H H H H H 2-0,3-dioxolan-2-yD,6-Me 1 C-6026 H H H H H 2-0,3-dioxan-2-yD,3-F 1 C-6027 H H H H H 2-0,3-dioxan-2-yD,4-F 1 C-6028 H H H H H 2-0,3-dioxan-2-yD,5-F 1 C-6029 H H H H H 2-0,3-dioxan-2-yD,6-F 1 C-6030 H H H H H 2-0,3-dioxan-2-yD,3-Me 1 C-6031 H H H H H 2-(1,3-dioxan-2-yD,4--Me 1 C-6032 H H H H H 2-(1,3-dioxan-2-yD,5-M e 1 C-6033 H H H H H 2-(1,3-dioxan-2-yD,6-Me 1 C-6034 H H H H H 2-(thiazol-2-yD,3-F 1 C-6035 H H H H H 2-(thiazol-2-yD,4-F 1 C-6036 H H H H H 2-(thiazol-2-yD,5-F 1 C-6037 H H H H H 2-(thiazol-2-yD,6-F 1 C-6038 H H H H H 2-(thiazol-2-yD,3-Me 1 C-6039 H H H H H 2-(thiazol-2-yD,4-Me 1 C-6040 H H H H H 2-(thiazol-2-yD,5-Me 1 C-6041 H H H H H 2-(thiazol-2-yD,6-Me 1 C-6042 H H H H H 2-(oxazol-2-y1),3-F 1 C-6043 H H H H H 2-(oxazol-2-yl)4-F 1 C-6044 H H H H H 2-(oxazol-2-y1),5-F 1 C-6045 H H H H H 2-(oxazol-2-y1),6-F 1 C-6046 H H H H H 2-(oxazol-2-yD,3-Me 1 C-6047 H H H H H 2-(oxazol-2-yD,4-Me 1 C-6048 H H H H H 2-(oxazol-2-yD,5-M e 1 C-6049 H H H H H 2-(oxazol-2-yD,6-M e 1 C-6050 H H H H H 2-CH= NOH,3-F 1 C-6051 H H H H H 2-CH= NOH,4-F 1 C-6052 H H H H H 2-CH= NOH,5-F 1 C-6053 H H H H H 2-CH= NOH,6-F 1 C-6054 H H H H H 2-CH=N0H,3-M e 1 C-6055 H H H H H 2-CH=N0H,4-M e 1 C-6056 H H H H H 2-CH=N0H,5-M e 1 C-6057 H H H H H 2-CH=N0H,6-M e 1 C-6058 H H H H H 2-CH=N0Me,3-F 1 C-6059 H H H H H 2-CH=N0Me,4-F 1 C-6060 H H H H H 2-CH=N0Me,5-F 1 C-6061 H H H H H 2-CH=N0Me,6-F 1 C-6062 H H H H H 2-CH=N0Me,3-M e 1 C-6063 H H H H H 2-CH=N0Me,4-M e 1 C-6064 H H H H H 2-CH=N0Me,5-M e 1 C-6065 H H H H H 2-CH=N0Me,6-M e 1 C-6066 H H H H H 2-CN,3-F 1 C-6067 H H H H H 2-CN,4-F 1 C-6068 H H H H H 2-CN,5-F 1 C-6069 H H H H H 2-CN,6-F 1 C-6070 H H H H H 2-CN,3-CI 1 C-6071 H H H H H 2-CN,4-CI 1 C-6072 H H H H H 2-CN,5-CI 1 C-6073 H H H H H 2-CN,6-CI 1 C-6074 H H H H H 2-CN,3-M e 1 C-6075 H H H H H 2-CN,4-M e 1 C-6076 H H H H H 2-CN,5-M e 1 C-6077 H H H H H 2-CN,6-M e 1 C-6078 H H H H H 2-CN,3-0Me 1
[0360]
[Table 235]
com pound R' R2 R- R44 R (Rd)m P C-6079 H H H H H 2-CN,4-0Me 1 C-6080 H H H H H 2-CN,5-0Me 1 C-6081 H H H H H 2-CN,6-0Me 1 C-6082 H H H H H 3-CN,2-F 1 C-6083 H H H H H 3-CN,4-F 1 C-6084 H H H H H 3-CN, 5-F 1 C-6085 H H H H H 3-CN,6 -F 1 C-6086 H H H H H 3-CN,2-CI 1 C-6087 H H H H H 3-CN,4-CI 1 C-6088 H H H H H 3-CN,5-CI 1 C-6089 H H H H H 3-CN,6-CI 1 C-6090 H H H H H 3-CN,2-MA e 1 C-6091 H H H H H 3-CN,4-MAe 1 C-6092 H H H H H 3-CN,-MAe 1 C-6093 H H H H H 3-CN,6-MA e 1 C-6094 H H H H H 3-CN,2-0Me 1 C-6095 H H H H H 3-CN,4-0Me 1 C-6096 H H H H H 3-CN,5-0Me 1 C-6097 H H H H H 3-CN,6-0Me 1 C-6098 H H H H H 4-CN,2-F 1 C-6099 H H H H H 4-CN,3-F 1 C-6100 H H H H H 4-CN,2-CI 1 C-6101 H H H H H 4-CN,3-CI 1 C-6102 H H H H H 4-CN,2-MAe 1 C-6103 H H H H H 4-CN,3-M e 1 C-6104 H H H H H 4-CN,2-0Me 1 C-6105 H H H H H 4-CN,3-0Me 1 C-6106 H H H H H 2-N0 2,3-F 1 C-6107 H H H H H 2-N0 2 ,4- 1 C-6108 H H H H H 2-N0 2 ,5-F 1 C-6109 H H H H H 2-N0 2,6-F 1 C-6110 H H H H H 2-N0 2,3-MAe 1 C-6111 H H H H H 2-N0 2,4-MvAe 1 C-6112 H H H H H 2-N0 2,5 -Me 1 C-6113 H H H H H 2-N0 2,6-MA e 1 C-6114 H H H H H 2-M e,3,4-F2 1 C-6115 H H H H H 2-M e,3,b-F 2 1 C-6116 H H H H H 2-M e,3,6-F 2 1 C-6117 H H H H H 2-M e,4,b-F 2 1 C-6118 H H H H H 2-0Me,3,4-F 2 1 C-6119 H H H H H 2-0Me,3,5-F 2 1 C-6120 H H H H H 2-0Me,3,6-F 2 1 C-6121 H H H H H 2-0Me,4,5-F 2 1 C-6122 H H H H H 2-(CH 2) 3-3 1 C-6123 H H H H H 2-(CH 2) 4-3 1 C-6124 H H H H H 2-(0CH 20H 2)-3 1 C-6125 H H H H H 2-(0CH 2CH 2CH 2)-3 1 C-6126 H H H H H 2-(CH 2 CH 20)-3 1 C-6127 H H H H H 2-(CH 2 CH 2CH 20)-3 1 C-6128 H H H H H 3-(CH 2) 3-4 1 C-6129 H H H H H 3-(CH 2) 4-4 1 C-6130 H H H H H 3-(0CH 2CH 2)-4 1 C-6131 H H H H H 3-(0CH 2CH 2CH 2)-4 1 C-6132 H H H H H 3-(CH 2 CH 20)-4 1 C-6133 H H H H H 3-(CH 20H 2 H 20)-4 1 C-6134 H H H H H 2-(0CH 20)-3 1 C-6135 H H H H H 3-(00H 20)-4
[0361]
[Table 236]
cornpound R' R2 R(RRtR m P 0-61 36 H H H H H 2-(00CH 20H 2 0 )-3 1 0-61 37 H H H H H 3-(00CH 20H 2 0 )-4 1 0-61 38 H H H H H 2-(00CF 20 )-3 1 0-61 39 H H H H H 3-(00CF 20 )-4 1 0-61 40 H H H H H 2-Mvle,6-Et 1 0-61 41 H H H H H 2-Mvle,4,b-F 2 1 0-61 42 H H H H H 2-oycopropyl,6-OM e 1 0-61 43 H H H H H 2-Mvieb-Et 1 0-61 44 H H H H H 2,6-Et 2 1 0-61 45 H H H H H 2-Et,6-F 1 C-61 46 H H H H H 2-0H 2 00CH3 ,6-CI1 1 0-61 47 H H H H H 2-0H 200CH 20H3 ,6-CI1 1 0T-61l4 8 H H H H H 2-C H 2 N Me 2 1
[0362]
[Table 237]
3 2 R R
R4 /'\N N
(O)r R 1 R' cornpound R1 WR Rj R~4 5 D0-0001 H H H H H cI1 0 D0-0002 H H H H H Br 0 -0003 H H H H H 1 0 -0004 H H H H H 0S(=0) 2M e 0 D0-0005 H H H H H 0 S=0 ) 2CF, 0 -0006 H H H H H 0 S(=0 ),C FCF, 0 -0007 H H H H H OS(= 0) 2CF 2CFCF 3 0 -0008 H H H H H S06-U) 2 (;FCF2 CF 2 ;F 1 0 -0009 H H H H H 0 S(= 0) 2 (4-M ePh) 0 -00 10 H H H H H 0 S=0 ) 2 N (M e) 2 0 D0-00 11 H H H H H 0 S=0 ) 2 N(Et) 2 0 D0-00 12 H H H H H naphtha len-1-yI1 0 -0013 H H H H H 2-F-naphtha len- -yI1 0 -0014 H H H H H 2-M e-naphtha len-1-yI1 0 -0015 H H H H H 2-CF 3 -naphtha ln-1-y 1 0 -0016 H H H H H 2-OM e-naphtha len-1-yI1 0 -0017 H H H H H naphtha en-2-yI1 0 -0018 H H H H H 1 -F-naphthalIen-2-yI1 0 -0019 H H H H H I1A e-naphttialen-2-yI1 0 -0020 H H H H H 1 -CF 3 -naphttia In-2-yI1 0 -0021 H H H H H 1 -0M e-naphthalIen-2-yI1 0 -0022 H H H H H 3-F-naphtha In-2-yI1 0 -0023 H H H H H 3-M e-naphtlia In-2-yI1 0 -0024 H H H H H 3-C F3 -naphtha In-2-yI1 0 -0025 H H H H H 3-0 Me-naphtha In-2-yI1 0 -0026 H H H H H pyrid i-2-yI1 0 -0027 H H H H H 3-F-pyri i-2-yI1 0 -0028 H H H H H 4-F-pyridii-2-yI1 0 -0029 H H H H H 5-F-pyrki i-2-yI1 0 -0030 H H H H H 6-F-pyid ii-2-yI1 0 -0031 H H H H H 3 CI-pyrid in-2-yI1 0 -0032 H H H H H 4 CI-pyridin-2-yI1 0 -0033 H H H H H 5-CI -pyriin-2-yI1 0 -0034 H H H H H 6 CI-pyid in-2-yI1 0 -0035 H H H H H 3-M e-pyrkid -2-yI1 0 -0036 H H H H H 4-M e-pyrki i-2-yI1 0 -0037 H H H H H 5-M e-pyri hi-2-yI1 0 -0038 H H H H H 6-M e-pyrkid -2-yI1 0 -0039 H H H H H 3-CF 3-Pyrid in-2-y 1 0 -0040 H H H H H 4--CF 3 -Pyrid n-2-yI1 0 -0041 H H H H H 5-C F 3 -Pyrid n-2-y 1 0 -0042 H H H H H 6-C F 3-Pyid in-2-yI1 0 -0043 H H H H H 3-OM e-pyrid in-2-yI1 0 -0044 H H H H H 4-OM e-pyrid in-2-yI1 0 -0045 H H H H H 5-OM e-pyid in-2-yI1 0 -0046 H H H H H 6-OM e-pyrildn-2-yI1 0 -0047 H H H H H 3,4-F2 -Pyrid ii-2-y 1 0 -0048 H H H H H 3,5-F 2 -Pyri -2-y 1 0 -0049 H H H H H 3,6-F 2 -Pyri i-2-y 1 0 -0050 H H H H H 3,4-C -pyrkid -2-yI1 0 -0051 H H H H H 3,5-C -pyridii-2-yI1 0 -0052 H H H H H 3,6-C -pyriduii-2-y I0
[0363]
[Table 238]
com pound R' R2 R R4 Rbp D-0053 H H H H H 3-F-4-Cl-pyridin-2-y 0 D-0054 H H H H H 3-F-5-Cl-pyridin-2-y 0 D-0055 H H H H H 3-F-6-Cl-pyridin-2-y 0 D-0056 H H H H H 3-F-4-Me-pyridh-2-yI 0 D-0057 H H H H H 3-F-5-Me-pyridh-2-yI 0 D-0058 H H H H H 3-F-6-Me-pyridh-2-yI 0 D-0059 H H H H H 3-F-4-0Me-pyridin-2-yI 0 D-0060 H H H H H 3-F-5-0Me-pyridin-2-yI 0 D-0061 H H H H H 3-F-6-0Me-pyridin-2-yI 0 D-0062 H H H H H 3-CI-4-F-pyridin-2-y 0 D-0063 H H H H H 3-CI-5-F-pyridin-2-y 0 D-0064 H H H H H 3-CI-6-F-pyridin-2-y 0 D-0065 H H H H H 3-CI-4-M Ae-pyridin-2-yI 0 D-0066 H H H H H 3-CI-5-M Ae-pyridin-2-yI 0 D-0067 H H H H H 3-CI-6-M Ae-pyridin-2-yI 0 D-0068 H H H H H 3-M e-4-F-pyridh-2-y 0 D-0069 H H H H H 3-M e-5-F-pyridh-2-y 0 D-0070 H H H H H 3-M e-6-F-pyridh-2-y 0 D-0071 H H H H H 3-MAe-4-Cl-pyridin-2-yI 0 D-0072 H H H H H 3-MAe-5-Cl-pyridin-2-yI 0 D-0073 H H H H H 3-MAe-6-Cl-pyridin-2-yI 0 D-0074 H H H H H 3,4-(Me) 2-pyridin-2-y 0 D-0075 H H H H H 3,5-(Me) 2-pyridin-2-y 0 D-0076 H H H H H 3,6-(Me) 2-pyridin-2-y 0 D-0077 H H H H H 3-M e-4-0Me-pyridh-2-yI 0 D-0078 H H H H H 3-M e-5-0Me-pyridh-2-yI 0 D-0079 H H H H H 3-M e-6-0Me-pyridh-2-yI 0 D-0080 H H H H H 3-0F 3 -4-F-pyrdin-2-yl 0 D-0081 H H H H H 3-0F 3 -5-F-pyrdin-2-yl 0 D-0082 H H H H H 3-CF 3 -6-F-pyridin-2-y 0 D-0083 H H H H H 3-CF 3-4-M e-pyrdn-2-yl 0 D-0084 H H H H H 3-CF 3-5-Me-pyridh-2-y 0 D-0085 H H H H H 3-CF 3-6-Me-pyridh-2-y 0 D-0086 H H H H H 3-0Me-4-F-pyridin-2-yI 0 D-0087 H H H H H 3-0Me-5-F-pyridin-2-yI 0 D-0088 H H H H H 3-0Me-6-F-pyridin-2-yI 0 D-0089 H H H H H 3-0Me-4-Cl-pyridin-2-y 0 D-0090 H H H H H 3-0Me-5-Cl-pyridin-2-y 0 D-0091 H H H H H 3-0Me-6-Cl-pyridin-2-y 0 D-0092 H H H H H 3-0Me-4-M e-pyridh-2-yI 0 D-0093 H H H H H 3-0Me-5-M e-pyridh-2-yI 0 D-0094 H H H H H 3-0Me-6-M e-pyridh-2-yI 0 D-0095 H H H H H 3,4-(OMe) 2-pyridin-2-y 0 D-0096 H H H H H 3,b-(OMe) 2-pyridin-2-y 0 D-0097 H H H H H 3,6-(OMe) 2-pyridin-2-y 0 D-0098 H H H H H pyridh-3-yI 0 D-0099 H H H H H 2-F-pyridin-3-yI 0 D-0100 H H H H H 4-F-pyridin-3-yI 0 D-0101 H H H H H 5-F-pyridin-3-yI 0 D-0102 H H H H H 6-F-pyridin-3-yI 0 D-0103 H H H H H 2-Cl-pyridin-3-yI 0 D-0104 H H H H H 4-Cl-pyridin-3-yI 0 D-0105 H H H H H 5-Cl-pyridin-3-yI 0 D-0106 H H H H H 6-Cl-pyridin-3-yI 0 D-0107 H H H H H 2-M e-pyridh-3-y 0 D-0108 H H H H H 4-M e-pyridh-3-y 0 D-0109 H H H H H 5-M e-pyridh-3-y 0
[0364]
[Table 239]
com pound R' R2 R R4 Rbp D-0110 H H H H H 6-M e-pyridh-3-yI 0 D-0111 H H H H H 2-CF 3 -pyridin-3-yl 0 D-0112 H H H H H 4-CF 3 -pyridin-3-yl 0 D-0113 H H H H H 5-CF 3 -pyridin-3-yl 0 D-0114 H H H H H 6-CF 3 -pyridin-3-yl 0 D-0115 H H H H H 2-0Me-pyridin-3-yI 0 D-0116 H H H H H 4-0Me-pyridin-3-yI 0 D-0117 H H H H H 5-0Me-pyridin-3-yI 0 D-0118 H H H H H 6-0Me-pyridin-3-yI 0 D-0119 H H H H H 2,4-F 2-pyridn-3-yl 0 D-0120 H H H H H 2,b-4 2-pyrdin-3-yl 0 D-0121 H H H H H 2,6-F 2-pyridh-3-y 0 D-0122 H H H H H 4,b- 2-pyrdin-3-yl 0 D-0123 H H H H H 4,6-F 2-pyrdin-3-yl 0 D-0124 H H H H H 2,4-C -pyridin-3-yI 0 D-0125 H H H H H 2,5-C -pyridin-3-yI 0 D-0126 H H H H H 2,6-C -pyridin-3-yI 0 D-0127 H H H H H 4,5-C -pyridin-3-yl 0 D-0128 H H H H H 4,6-C -pyridin-3-yl 0 D-0129 H H H H H 2-F-4-Cl-pyridin-3-y 0 D-0130 H H H H H 2-F-5-Cl-pyridin-3-y 0 D-0131 H H H H H 2-F-6-Cl-pyridin-3-y 0 D-0132 H H H H H 4-F-2-Cl-pyridin-3-y 0 D-0133 H H H H H 4-F-5-Cl-pyridin-3-y 0 D-0134 H H H H H 4-F-6-Cl-pyridin-3-y 0 D-0135 H H H H H 2-F-4-M e-pyridh-3-y 0 D-0136 H H H H H 2-F-5 -M e-pyridh-3-y 0 D-0137 H H H H H 2-F-6 -M e-pyridh-3-y 0 D-0138 H H H H H 4-F-2 -M e-pyridh-3-y 0 D-0139 H H H H H 4-F-5-M e-pyridh-3-y 0 D-0140 H H H H H 4-F-6-M e-pyridh-3-y 0 D-0141 H H H H H 2-F-4-0Me-pyridin-3-yI 0 D-0142 H H H H H 2-F-5-0Me-pyridin-3-yI 0 D-0143 H H H H H 2-F-6-0Me-pyridin-3-yI 0 D-0144 H H H H H 4-F-2-0Me-pyridin-3-yI 0 D-0145 H H H H H 4-F-5-0Me-pyridin-3-yI 0 D-0146 H H H H H 4-F-6-0Me-pyridin-3-yI 0 D-0147 H H H H H 2-CI-5-F-pyridin-3-y 0 D-0148 H H H H H 2-CI-6-F-pyridin-3-y 0 D-0149 H H H H H 4-CI-5-F-pyridin-3-y 0 D-0150 H H H H H 4-CI-6-F-pyridin-3-y 0 D-0151 H H H H H 2-CI-4-iMe-pyridin-3-yI 0 D-0152 H H H H H 2-CI-5-Me-pyridin-3-yI 0 D-0153 H H H H H 2-CI-6-Me-pyridin-3-yI 0 D-0154 H H H H H 4-CI-2-Me-pyridin-3-yI 0 D-0155 H H H H H 4-CI-5-Me-pyridin-3-yI 0 D-0156 H H H H H 4-CI-6-Me-pyridin-3-yI 0 D-0157 H H H H H 2-M e-5-F-pyridh-3-y 0 D-0158 H H H H H 2-M e-6-F-pyridh-3-y 0 D-0159 H H H H H 4-M e-5-F-pyridh-3-y 0 D-0160 H H H H H 4-M e-6-F-pyridh-3-y 0 D-0161 H H H H H 2 -M e-5-Cl-pyridin-3-yI 0 D-0162 H H H H H 2-M e-6-Cl-pyridin-3-yI 0 D-0163 H H H H H 4-M e-5-Cl-pyridin-3-yI 0 D-0164 H H H H H 4-M e-6-Cl-pyridin-3-yI 0 D-0165 H H H H H 2,4-(Me) 2-pyridin-3-y 0 D-0166 H H H H H 2,b-(Me) 2-pyridin-3-y 0
[0365]
[Table 240]
com pound R] R2 Rj R4 0' p D-0167 H H H H H 2,6-(Me) 2-pyridin-3-y 0 D-0168 H H H H H 4,b-(Me) 2-pyridin-3-y 0 D-0169 H H H H H 4,6-(Me) 2-pyridin-3-y 0 D-0170 H H H H H 2-M e-4-0Me-pyridh-3-yI 0 D-0171 H H H H H 2-M e-5-0Me-pyridh-3-yI 0 D-0172 H H H H H 2-M e-6-0Me-pyridh-3-yI 0 D-0173 H H H H H 4-M e-2-0Me-pyridh-3-yI 0 D-0174 H H H H H 4-M e-5-0Me-pyridh-3-yI 0 D-0175 H H H H H 4-M e-6-0Me-pyridh-3-yI 0 D-0176 H H H H H 2-0F 3 -4-F-pyrdin-3-yl 0 D-0177 H H H H H 2-CF 3 -5-F-pyridin-3-y 0 D-0178 H H H H H 2-0F 3 -6-F-pyrdin-3-yl 0 D-0179 H H H H H 4-0F 3 -2-F-pyrdin-3-yl 0 D-0180 H H H H H 4-CF 3 -5-F-pyridin-3-yI 0 D-0181 H H H H H 4-0F 3 -6-F-pyrdin-3-yl 0 D-0182 H H H H H 2-CF 3-4-Me-pyridh-3-y 0 D-0183 H H H H H 2-CF 3-5-Me-pyridh-3-y 0 D-0184 H H H H H 2-CF 3-6-Me-pyridh-3-y 0 D-0185 H H H H H 4-CF 3-2-Me-pyridh-3-y 0 D-0186 H H H H H 4-CF 3-5-Me-pyridh-3-y 0 D-0187 H H H H H 4-CF 3-6-M e-pyrdn-3-yl 0 D-0188 H H H H H 2-0Me-5-F-pyridin-3-yI 0 D-0189 H H H H H 2-0Me-6-F-pyridin-3-yI 0 D-0190 H H H H H 4-0Me-5-F-pyridin-3-yI 0 D-0191 H H H H H 4-0Me-6-F-pyridin-3-yI 0 D-0192 H H H H H 2-0Me-4-Cl-pyridin-3-y 0 D-0193 H H H H H 2-0Me-5-Cl-pyridin-3-y 0 D-0194 H H H H H 2-0Me-6-Cl-pyridin-3-y 0 D-0195 H H H H H 4-0Me-2-Cl-pyridin-3-y 0 D-0196 H H H H H 4-0Me-5-Cl-pyriin-3-y 0 D-0197 H H H H H 4-0Me-6-Cl-pyridin-3-y 0 D-0198 H H H H H 2-0Me-5-M e-pyridh-3-yI 0 D-0199 H H H H H 2-0Me-6-M e-pyridh-3-yI 0 D-0200 H H H H H 4-0Me-5-Me-pyridh-3-y 0 D-0201 H H H H H 4-0Me-6-M e-pyridh-3-yI 0 D-0202 H H H H H 2,4-(OMe) 2-pyridin-3-y 0 D-0203 H H H H H 2,5-(OMe) 2-pyridin-3-y 0 D-0204 H H H H H 2,6-(OMe) 2-pyridin-3-y 0 D-0205 H H H H H 4,b-(OMe) 2-pyridin-3-yl 0 D-0206 H H H H H 4,6-(OMe) 2-pyridin-3-yl 0 D-0207 H H H H H pyridh-4-yI 0 D-0208 H H H H H 2-F-pyridin-4-yI 0 D-0209 H H H H H 3-F-pyridin-4-yI 0 D-0210 H H H H H 2-Cl-pyridin-4-yI 0 D-0211 H H H H H 3-Cl-pyridin-4-yI 0 D-0212 H H H H H 2-M e-pyridh-4-y 0 D-0213 H H H H H 3-M e-pyridh-4-y 0 D-0214 H H H H H 2-GF 3 -pyridin-4-yl 0 D-0215 H H H H H 3-CF 3 -pyridin-4-yI 0 D-0216 H H H H H 2-0Me-pyridin-4-yI 0 D-0217 H H H H H 3-0Me-pyridin-4-yI 0 D-0218 H H H H H 2,3-F 2-Pyrd n-4-y1 0 D-0219 H H H H H 2,5-F 2-pyridh-4-yI 0 D-0220 H H H H H 2,6-F 2-pyrdin-4-yl 0 D-0221 H H H H H 3,5-F 2-pyridh-4-yI 0 D-0222 H H H H H 2,3-C -pyridin-4-yI 0 -0223 H H H H H 2,5-C -pyrdin-4-yI 0
[0366]
[Table 241]
com pound R] R2 Rj R4 0' p D-0224 H H H H H 2,6-C -pyridin-4-yI 0 D-0225 H H H H H 3,5-C -pyridin-4-yI 0 D-0226 H H H H H 3-F-2-Cl-pyridin-4-y 0 D-0227 H H H H H 3-F-5--C-pyridin-4-y 0 D-0228 H H H H H 3-F-6-Cl-pyridin-4-y 0 D-0229 H H H H H 3-F-2-M e-pyridh-4-y 0 D-0230 H H H H H 3-F-5-Me-pyridh-4-yI 0 D-0231 H H H H H 3-F-6-M e-pyridh-4-y 0 D-0232 H H H H H 3-F-2-0Me-pyridin-4-yI 0 D-0233 H H H H H 3-F-5-0Me-pyridin-4-yI 0 D-0234 H H H H H 3-F-6-0Me-pyridin-4-yI 0 D-0235 H H H H H 3-CI-2-F-pyridin-4-y 0 D-0236 H H H H H 3-CI-6-F-pyridin-4-y 0 D-0237 H H H H H 3-CI-2-M e-pyridin-4-yI 0 D-0238 H H H H H 3-CI-5-M e-pyridin-4-y 0 D-0239 H H H H H 3-CI-6-M e-pyridin-4-yI 0 D-0240 H H H H H 3-M e-2-F-pyridh-4-y 0 D-0241 H H H H H 3-Me-6-F-pyridh-4-yI 0 D-0242 H H H H H 3-MAe-2-Cl-pyridin-4-yI 0 D-0243 H H H H H 3-MAe-6-Cl-pyridin-4-yI 0 D-0244 H H H H H 2,3-(Me) 2-pyridin-4-y 0 D-0245 H H H H H 3,5-(Me) 2-pyrdin-4-yl 0 D-0246 H H H H H 3,6-(Me) 2-pyrdin-4-yl 0 D-0247 H H H H H 3-Me-2-0Me-pyridh-4-yI 0 D-0248 H H H H H 3-Me-5-0Me-pyridh-4-yI 0 D-0249 H H H H H 3-Me-6-0Me-pyridh-4-yI 0 D-0250 H H H H H 3-CF 3 -2-F-pyridin-4-y 0 D-0251 H H H H H 3-CF 3-5-F-pyrdin-4-yl 0 D-0252 H H H H H 3-CF 3-6-F-pyrdin-4-yl 0 D-0253 H H H H H 3-CF 3-2-Me-pyridh-4-y 0 D-0254 H H H H H 3-CF 3-5-Me-pyridh-4-y 0 D-0255 H H H H H 3-CF 3-6-Me-pyridh-4-y 0 D-0256 H H H H H 3-0Me-2-F-pyridin-4-yI 0 D-0257 H H H H H 3-0Me-6-F-pyridin-4-yI 0 D-0258 H H H H H 3-0Me-2-Cl-pyridin-4-y 0 D-0259 H H H H H 3-0Me-5-Cl-pyridin-4-y 0 D-0260 H H H H H 3-0Me-6-Cl-pyridin-4-y 0 D-0261 H H H H H 3-0Me-2-Me-pyridh-4-yI 0 D-0262 H H H H H 3-0Me-6-Me-pyridh-4-yI 0 D-0263 H H H H H 2,3-(OMe) 2-pyridin-4-yI 0 D-0264 H H H H H 3,5-(OMe) 2-pyridin-4-yI 0 D-0265 H H H H H 3,6-(OMe) 2-pyridin-4-y 0 D-0266 H H H H H pyrin idin-2-yl 0 D-0267 H H H H H pyrin idin-4-yl 0 D-0268 H H H H H 5-F-pyrin idin-4-yI 0 D-0269 H H H H H 5-Me-pyrin idin-4-yl 0 D-0270 H H H H H b-GF3 -pyrm din-4-yl 0 D-0271 H H H H H 5-0Me-pyrin idin-4-yI 0 D-0272 H H H H H pyrin idin-5-yl 0 D-0273 H H H H H 4-F-pyrin idin-5-yI 0 D-0274 H H H H H 4-Cl-pyrin idn-5-y 0 D-0275 H H H H H 4-Me-pyrin idin-5-yl 0 D-0276 H H H H H 4-CF 3-pyrin idin-5-yl 0 D-0277 H H H H H 4-0Me-pyriniin-5-yI 0 D-0278 H H H H H pyridazn-3-yI 0 D-0279 H H H H H 4-F-pyridazin-3-yl 0 -0280 H H H H H 4-Cl-pyrdiazin-3-yI 0
[0367]
[Table 242]
com pound R' R2 R R4 Rbp D-0281 H H H H H 4-Me-pyridazin-3-yI 0 D-0282 H H H H H 4-CF 3-pyridazh-3-y 0 D-0283 H H H H H 4-0Me-pyridazin-3-yI 0 D-0284 H H H H H pyridazh-4-yI 0 D-0285 H H H H H 3-F-pyridazin-4-y 0 D-0286 H H H H H 3-Cl-pyridazin-4-y 0 D-0287 H H H H H 3-Me-pyridazin-4-yI 0 D-0288 H H H H H 3-CF 3-pyridazh-4-y 0 D-0289 H H H H H 3-0Me-pyridazin-4-yI 0 D-0290 H H H H H 5-F-pyridazin-4-y 0 D-0291 H H H H H 5-Cl-pyridazin-4-y 0 D-0292 H H H H H 5-Me-pyridazin-4-yI 0 D-0293 H H H H H b-CF 3-pyrdiazn-4-yl 0 D-0294 H H H H H 5-OMe-pyridazin-4-yI 0 D-0295 H H H H H thiophen-2-yI 0 D-0296 H H H H H 3-F-thiophen-2-yI 0 D-0297 H H H H H 3-Cl-thiophen-2-yI 0 D-0298 H H H H H 3-M e-thiophen-2-y 0 D-0299 H H H H H 3-GF 3-thiophen-2-yl 0 D-0300 H H H H H 3-0Me-thiophen-2-yI 0 D-0301 H H H H H thiophen-3-yI 0 D-0302 H H H H H 2-F-thiophen-3-yI 0 D-0303 H H H H H 2-Cl-thiophen-3-yI 0 D-0304 H H H H H 2-M e-thiophen-3-y 0 D-0305 H H H H H 2-CF 3-thiophen-3-yI 0 D-0306 H H H H H 2-0Me-thiophen-3-yI 0 D-0307 H H H H H 4-F-thiophen-3-yI 0 D-0308 H H H H H 4-Cl-thiophen-3-yI 0 D-0309 H H H H H 4-M e-thiophen-3-y 0 D-0310 H H H H H 4-CF 3-thiophen-3-y 0 D-0311 H H H H H 4-0Me-thiophen-3-yI 0 D-0312 H H H H H thiazol-2-yI 0 D-0313 H H H H H thiazol-4-yI 0 D-0314 H H H H H 5-F-thiazol-4-yI 0 D-0315 H H H H H 5-M e-thiazol-4-y 0 D-0316 H H H H H 5-CF 3-thibzol-4-yI 0 D-0317 H H H H H 5-OMe-thiazol-4-yI 0 D-0318 H H H H H thiazol-5-yI 0 D-0319 H H H H H 4-F-thiazol-5-y 0 D-0320 H H H H H 4-M e-thiazo-5-y 0 D-0321 H H H H H 4-CF 3-thibzo-5-yI 0 D-0322 H H H H H 4-0Me-thiazol-5-yI 0 D-0323 H H H H H 1 H-pyrrol1-yI 0 D-0324 H H H H H 2-F-1 H-pyrrol1-yI 0 D-0325 H H H H H 2-M e-1 H-pyrrol1-y 0 D-0326 H H H H H 2-0%-1H-pyrrol-yl 0 D-0327 H H H H H 2-0Me-1 H-pyrrol1-y 0 D-0328 H H H H H 1 H-pyrrol-2-yI 0 D-0329 H H H H H 1-M e-1 H-pyrrol-2-y 0 D-0330 H H H H H 3-F-1H-pyrrol-2-yI 0 D-0331 H H H H H 3-M e-1 H-pyrrol-2-yI 0 D-0332 H H H H H 3-CF-i1H-pyrrol-2-y 0 D-0333 H H H H H 3-0Me-1 H-pyrrol-2-yI 0 D-0334 H H H H H 1-M e-3-F-1 H-pyrrol-2-y 0 D-0335 H H H H H 1,3-(Me) 2 -1 H-pyrrol-2-yl 0 D-0336 H H H H H 1-Me-3-CF 3-1H-pyrrol-2-yl 0 D-0337 H H H H H 1-M e-3-0Me-1 H-pyrrol-2-y 0
[0368]
[Table 243]
com pound R' R2 R R4 R p D-0338 H H H H H 1H-pyrrol-3-yI 0 D-0339 H H H H H 1-M e-1H-pyrrol-3-yI 0 D-0340 H H H H H 2-F-1H-pyrrol-3-yI 0 D-0341 H H H H H 2-M e-1H-pyrrol-3-yI 0 D-0342 H H H H H 2-0F-i1H-pyrrol-3-yl 0 D-0343 H H H H H 2-0Me-1H-pyrrol-3-y 0 D-0344 H H H H H 1-M e-2-F-1H-pyrrol-3-yI 0 D-0345 H H H H H 1,2-(Me) 2 -1H-pyrrol-3-yI 0 D-0346 H H H H H 1-Me-2-CF 3 -1H-pyrrol-3-y 0 D-0347 H H H H H 1-M e-2-0Me-1H-pyrrol-3-yI 0 D-0348 H H H H H 4-F-1H-pyrrol-3-yI 0 D-0349 H H H H H 4-M e-1H-pyrrol-3-yI 0 D-0350 H H H H H 4-0%-i1H-pyrrol-3-yl 0 D-0351 H H H H H 4-0Me-1H-pyrrol-3-yI 0 D-0352 H H H H H 1-M e-4-F-1H-pyrrol-3-yI 0 D-0353 H H H H H 1,4-(Me) 2 -1H-pyrrol-3-yI 0 D-0354 H H H H H 1-Me-4-CF 3 -1H-pyrrol-3-y 0 D-0355 H H H H H 1-M e-4-0Me-1H-pyrrol-3-yI 0 D-0356 H H H H H 1H-pyrazol-1-yI 0 D-0357 H H H H H 5-F-1H-pyrazol-1-y 0 D-0358 H H H H H 5-Ci1H-pyrazol-1-yI 0 D-0359 H H H H H 5-M e-1H-pyrazol-1-y 0 D-0360 H H H H H 5-CF 3 -1-pyrazol-1-y 0 D-0361 H H H H H 5-0Me-1H-pyrazol-1-y 0 D-0362 H H H H H 1H-pyrazol-3-yI 0 D-0363 H H H H H 1-M e-1H-pyrazol-3-y 0 D-0364 H H H H H 4-F-1H-pyrazol-3-yI 0 D-0365 H H H H H 4-Ci1H-pyrazol-3-yI 0 D-0366 H H H H H 4-M e-1H-pyrazol-3-y 0 D-0367 H H H H H 4-CF 3-1H-pyrazol-3-yI 0 D-0368 H H H H H 4-0Me-1H-pyrazol-3-y 0 D-0369 H H H H H 1-M e-4-F-1H-pyrazol-3-yl 0 D-0370 H H H H H 1-M e-4-Ci1H-pyrazol-3-y 0 D-0371 H H H H H 1,4-(Me) 2-1H-pyrazol-3-yl 0 D-0372 H H H H H 1-M e-4-CF 3-1H-pyrazol-3-y 0 D-0373 H H H H H 1-M e-4-0Me-1H-pyrazol-3-yI 0 D-0374 H H H H H 1H-pyrazol-4-yI 0 D-0375 H H H H H 1-M e-1H-pyrazol-4-y 0 D-0376 H H H H H 3-F-1H-pyrazol-4-y 0 D-0377 H H H H H 3-CI-1H-pyrazol-4-y 0 D-0378 H H H H H 3-M e-1H-pyrazol-4-y 0 D-0379 H H H H H 3-0F 3 -1-pyrazol-4-yl 0 D-0380 H H H H H 3-0Me-1H-pyrazol-4-y 0 D-0381 H H H H H 1-M e-3-F-1H-pyrazol-4-yl 0 D-0382 H H H H H 1-Me-3-CI-/1H-pyrazol-4-y 0 D-0383 H H H H H 1,3-(Me) 2-1H-pyrazol-4-yl 0 D-0384 H H H H H 1-M e-3-CF 3-1H-pyrazol-4-yI 0 D-0385 H H H H H 1-M e-3-0Me-1H-pyrazol-4-yI 0 D-0386 H H H H H 5-F-1H-pyrazol-4-y 0 D-0387 H H H H H 5-CI-1H-pyrazol-4-y 0 D-0388 H H H H H 5-M e-1H-pyrazol-4-y 0 D-0389 H H H H H 5-CF-1H-pyrazol-4-y 0 D-0390 H H H H H 5-0Me-1H-pyrazol-4-y 0 D-0391 H H H H H 1-M e-5-F-1H-pyrazol-4-yl 0 D-0392 H H H H H 1-M e-5-Ci-1H-pyrazol-4-yl 0 D-0393 H H H H H 1,5-(Me) 2-1H-pyrazol-4-yI 0 D-0394 H H H H H i -M e-5-0F 3 -H1-pyrazol-4-yI 0
[0369]
[Table 244]
com pound R' R2 R R4 R p D-0395 H H H H H 1-M e-5-0Me-1H-pyrazol-4-y 0 D-0396 H H H H H 1H-pyrazol-5-y 0 D-0397 H H H H H 1-M e-1H-pyrazol-5-y 0 D-0398 H H H H H 4-F-1H-pyrazol-5-y 0 D-0399 H H H H H 4-Ci1H-pyrazol-5-y 0 D-0400 H H H H H 4-M e-1H-pyrazol-5-y 0 D-0401 H H H H H 4-CF 3 -1H-pyrazol-5-y 0 D-0402 H H H H H 4-0Me-1H-pyrazol-5-yI 0 D-0403 H H H H H 1-M e-4-F-1H-pyrazol-5-yl 0 D-0404 H H H H H 1-M e-4-Ci1H-pyrazol-5-y 0 D-0405 H H H H H 1,4-(Me) 2 -1H-pyrazol-b-yl 0 D-0406 H H H H H 1-Me-4-CF3 -1 H-pyrazol-5-yI 0 D-0407 H H H H H 1-M e-4-0Me-1H-pyrazol-5-yI 0 D-0408 H H H H H furan-2-yI 0 D-0409 H H H H H 3-F-furan-2-yI 0 D-0410 H H H H H 3-Me-furan-2-yI 0 D-0411 H H H H H 3-CF3- f uran-2-yI 0 D-0412 H H H H H 3-OMe-furan-2-y 0 D-0413 H H H H H furan-3-yI 0 D-0414 H H H H H 2-F-furan-3-yI 0 D-0415 H H H H H 2-Me-furan-3-yI 0 D-0416 H H H H H 2-CF 3 -furan-3-yI 0 D-0417 H H H H H 2-OMe-furan-3-y 0 D-0418 H H H H H 4-F-fu ran-3-yI 0 D-0419 H H H H H 4-M e-furan-3-yI 0 D-0420 H H H H H 4-CF 3 -furan-3-yI 0 D-0421 H H H H H 4-OMe-furan-3-y 0 D-0422 H H H H H isoxazol-3-yI 0 D-0423 H H H H H 4-F-isoxazol-3-yI 0 D-0424 H H H H H 4-Me-isoxazol-3-y 0 D-0425 H H H H H 4-CF 3 -soxazol-3-yl 0 D-0426 H H H H H 4-0Me-isoxazol-3-yI 0 D-0427 H H H H H isoxazol-4-yI 0 D-0428 H H H H H 5-F-isoxazol-4-yI 0 D-0429 H H H H H 5-M e-isoxazol-4-y 0 D-0430 H H H H H 5-CF 3 -isoxazol-4-yI 0 D-0431 H H H H H 5-OMe-isoxazol-4-yI 0 D-0432 H H H H H isoxazol-5-yI 0 D-0433 H H H H H 4-F-isoxazol-5-yl 0 D-0434 H H H H H 4-Me-isoxazo-5-y 0 D-0435 H H H H H 4-CF 3-isoxazol-5-y 0 D-0436 H H H H H 4-0Me-isoxazol-5-y 0 D-0437 H H H H H 1H-1,2,3-triazol-1-y 0 D-0438 H H H H H 5-F-1 H-1,2,3-triazol-1I-y 0 D-0439 H H H H H 5-M e-1 H-1,2,3-triazol-1-yl 0 D-0440 H H H H H b-F 3 -1 H-1,2,3-triazo1l-1-y 0 D-0441 H H H H H 5-0Me-1 H-1,2,3-triazol--y 0 D-0442 H H H H H 1H-1,2,3-triazol-4-y 0 D-0443 H H H H H 5-F-1H-1,2,3-triazo1-4-yl 0 D-0444 H H H H H 5-Me-1H-1,2,3-triazo-4-y 0 D-0445 H H H H H 5-CF 3 -1 H-1,2,3-triazol-4-yl 0 D-0446 H H H H H 5-0Me-1iH-12,3-triazol-4-yl 0 D-0447 H H H H H 1H-1,2,3-triazo[-5-y 0 D-0448 H H H H H 4-F-1H-1,2,3-triazo-5-yl 0 D-0449 H H H H H 4-Me-1H-12,3-triazo-5-y 0 D-0450 H H H H H 4-CF 3 -H -1,2,3-triazol-5-yl 0 D-0451 H H H H H 4-0Me-1H-1,2,3-triazo-S-y 0
[0370]
[Table 245] cornpound R R2 wR R 0 p D0-0452 H H H H H 111-1 2,4-triazo[-1 0 -0453 H H H H H 5-M e-1 H -1,2,4tr az o H -yI1 0 -0454 H H H H H 5-F-1 H -1,2,4-triazo1-1-yI1 0 -0455 H H H H H 5-F,-1H-1,2,4-triazo1-1-yI1 0 -0456 H H H H H 5-OM e-1 H-1 2,4-triazoHl-y1 0 -0457 H H H H H 111-1 2,4-triazo[-3-yI1 0 -0458 H H H H H 1l-M e -l1H-12,4tr ia zo 3 -yI1 0 -0459 H H H H H 111-1 2,4-triazoF-5-yI1 0 -0460 H H H H H 1l-M e-l1H-1,2,4tr ia zo-5-yI1 0 -0461 H H H H H 3,5-(M e) 2 -isoxaZo[-4-yI1 0 -0462 H H H H H 3,5-(Et) 2-LsoxazoF-4-yI1 0 -0463 H H H H H qu ho lin-4-yI1 0 -0464 H H H H H isoqu ho lin-4-yI1 0 -0465 H H H H H 3,6-(OMe) 2 -pyridazni-4-yI1 0 -0466 H H H H H 2,4-(O M e) 2-pyrinl id h-5-yI1 0 -0467 H H H H cI1 OS(=O0) 20F3 0
[0371]
[Table 246]
R3 R2 0 4 R / N'N 0
(0), R 1 R5 cornpound R1 R2 R Tj Q p D0-5001 H H H H H cI 1 D0-5002 H H H H H Br 1 -5003 H H H H H 1 1 -5004 H H H H H OS (=O)2M e 1 -5005 H H H H H S (= 0)2CF, 1 -5006 H H H H H S(= 0) 20F 2CF 3 1 -5007 H H H H H S(= 0) 2CF 2 CF 2 CF 3 1 D0-5008 H H H H H OS(k=-U ) 2 GF 2 GF2 GF 2 GF 3 1 -5009 H H H H H S (= 0) 2 (4-MlePh)1 -5010 H H H H H 0S 0 ) 2 N (M e) 2 1 -5011 H H H H H 0S 0 ) 2 N(Et) 2 1 -5012 H H H H H naphtha len-1 -y~ 1 -5013 H H H H H 2-F-naphtha len-1-yI1 1 -5014 H H H H H 2-Mtle-naphtha len-1 -yI 1 -5015 H H H H H 2-C F3 -naphtha len- -y I 1 -5016 H H H H H 2-OM e-naphtha len-1-yI1 1 -5017 H H H H H naphtha Ien-2-y~ 1 -5018 H H H H H 1 -F-naphthalIen-2-y I 1 -5019 H H H H H 1 AMe-naphthalIen-2-yI1 1 -5020 H H H H H 1 -C F 3 -naphtha In-2-y I 1 -5021 H H H H H 1 -0M e-naphttialen-2-y I 1 -5022 H H H H H 3-F-naphtha In-2-y I 1 -5023 H H H H H 3-M e-naphthalIen-2-y I 1 -5024 H H H H H 3-C F 3-naphtha In-2-y I 1 -5025 H H H H H 3-OM e-naphthalIen-2-yI1 1 -5026 H H H H H pyridii-2-y I 1 -5027 H H H H H 3 -F-p yr iii-2-y I 1 -5028 H H H H H 4-F-pyrid i-2-y I 1 -5029 H H H H H 5 -F-p y r in-2-y I 1 -5030 H H H H H 6 -F-p y r idin-2-yI1 1 -5031 H H H H H 3-C I-pyridin-2-y I 1 -5032 H H H H H 4-C I-pyridin-2-y I 1 -5033 H H H H H 5-CI-pyriin-2-yI1 1 -5034 H H H H H 6-C I--pyriin-2-yI 1 -5035 H H H H H 3-M e-pyrid in-2-y I 1 -5036 H H H H H 4-M e-pyrid in-2-yI1 1 -5037 H H H H H 5-M e-pyrid in-2-y I 1 -5038 H H H H H 6-M e-pyrid in-2-y I 1 -5039 H H H H H 3-0F 3 --Pyrid i-2-y I1 -5040 H H H H H 4-0F 3 -Pyri -2-y I1 -5041 H H H H H 5--0F 3 -Pyri i-2-y I1 -5042 H H H H H 6-0F 3 -Pyri -2-y I1 -5043 H H H H H 3-0 Me-pyridii-2-y I 1 -5044 H H H H H 4-0 Me-pyridii-2-yI1 1 -5045 H H H H H 5-0 Me-pyrkid i-2-y I 1 -5046 H H H H H 6-0 Me-pyrkid i-2-y I 1 -5047 H H H H H 3,4-F 2-Pyri i-2-yI1 1 -5048 H H H H H 3,5-F2 -Pyr~id -2-y I 1 -5049 H H H H H 3,6-F 2-Pyri i-2-y I1 -5050 H H H H H 3,4--C -pyrid ii-2-yI1 -5051 H H H H H 3,5-GC6-pyrki -2-y I1 -5052 H H H H H 3,6-C 6-pyri i-2-y I1
[0372]
[Table 247]
com pound R' R2 R R4 Rb p D-5053 H H H H H 3-F-4-Cl-pyridh-2-y 1 D-5054 H H H H H 3-F-5-Cl-pyridh-2-yI 1 D-5055 H H H H H 3-F-6-Cl-pyridh-2-yI 1 D-5056 H H H H H 3-F-4-M e-pyridin-2-y 1 D-5057 H H H H H 3-F-5-M e-pyridin-2-y 1 D-5058 H H H H H 3-F-6-M e-pyridin-2-y 1 D-5059 H H H H H 3-F-4-0Me-pyridin-2-y 1 D-5060 H H H H H 3-F-5-0Me-pyridin-2-y 1 D-5061 H H H H H 3-F-6-0Me-pyridin-2-y 1 D-5062 H H H H H 3-CI-4-F-pyridh-2-yI 1 D-5063 H H H H H 3-CI-5-F-pyridh-2-y 1 D-5064 H H H H H 3-CI-6-F-pyridh-2-y 1 D-5065 H H H H H 3-CI-4-Me-pyridin-2-y 1 D-5066 H H H H H 3-CI-5-Me-pyridin-2-y 1 D-5067 H H H H H 3-CI-6-Me-pyridin-2-y 1 D-5068 H H H H H 3-M e-4-F-pyridin-2-y 1 D-5069 H H H H H 3-M e-5-F-pyridin-2-y 1 D-5070 H H H H H 3-M e-6-F-pyridin-2-y 1 D-5071 H H H H H 3-M e-4-CI-pyridin-2-yI 1 D-5072 H H H H H 3-M e-5-CI-pyridin-2-yI 1 D-5073 H H H H H 3-M e-6-CI-pyridin-2-yI 1 D-5074 H H H H H 3,4-(Me) 2-pyridin-2-yI 1 D-5075 H H H H H 3,5-(Me) 2-pyridin-2-yI 1 D-5076 H H H H H 3,6-(Me) 2-pyridin-2-yl 1 D-5077 H H H H H 3-M e-4-0Me-pyridin-2-yI 1 D-5078 H H H H H 3-Me-5-0Me-pyridin-2-y 1 D-5079 H H H H H 3-Me-6-0Me-pyridin-2-y 1 D-5080 H H H H H 3-0F 3 -4-F-pyrdn-2-yl 1 D-5081 H H H H H 3-UF 3 -b-F-pyrdn-2-yl 1 D-5082 H H H H H 3-CF 3 -6-F-pyridh-2-yI 1 D-5083 H H H H H 3-CF 3-4-Me-pyrdin-2-yl 1 D-5084 H H H H H 3-CF 3-5-Me-pyridh-2-y 1 D-5085 H H H H H 3-CF 3-6-Me-pyridh-2-y 1 D-5086 H H H H H 3-0Me-4-F-pyridin-2-yI 1 D-5087 H H H H H 3-0Me-5-F-pyridin-2-yI 1 D-5088 H H H H H 3-0Me-6-F-pyridin-2-yI 1 D-5089 H H H H H 3-0Me-4-Cl-pyridh-2-y 1 D-5090 H H H H H 3-0Me-5-Cl-pyridh-2-y 1 D-5091 H H H H H 3-0Me-6-Cl-pyridh-2-yI 1 D-5092 H H H H H 3-0Me-4-Me-pyridin-2-y 1 D-5093 H H H H H 3-0Me-5-Me-pyridin-2-y 1 D-5094 H H H H H 3-0Me-6-Me-pyridin-2-y 1 D-5095 H H H H H 3,4-(0Me) 2 -pyridh-2-yI 1 D-5096 H H H H H 3,b-(0Me) 2 -pyrdn-2-yl 1 D-5097 H H H H H 3,6-(0Me) 2 -pyridh-2-yI 1 D-5098 H H H H H pyridin-3-yI 1 D-5099 H H H H H 2-F-pyridin-3-yI 1 D-5100 H H H H H 4-F-pyridin-3-y 1 D-5101 H H H H H 5-F-pyridin-3-y 1 D-5102 H H H H H 6-F-pyridin-3-y 1 D-5103 H H H H H 2-Cl-pyridin-3-y 1 D-5104 H H H H H 4-Cl-pyridin-3-y 1 D-5105 H H H H H 5-Cl-pyridin-3-y 1 D-5106 H H H H H 6-Cl-pyridin-3-y 1 D-5107 H H H H H 2-Me-pyridin-3-y 1 D-5108 H H H H H 4-Me-pyridin-3-y 1 D-5109 H H H H H 5-Me-pyridin-3-y 1
[0373]
[Table 248]
com pound R' R2 R R4 Rb p D-5110 H H H H H 6-Me-pyridin-3-y 1 D-5111 H H H H H 2-CF 3-pyridh-3-yI 1 D-5112 H H H H H 4-CF 3-pyridn-3-yl 1 D-5113 H H H H H b-CF 3-pyridn-3-yl 1 D-5114 H H H H H 6-CF 3-pyridn-3-yl 1 D-5115 H H H H H 2-0Me-pyridin-3-y 1 D-5116 H H H H H 4-0Me-pyridin-3-yI 1 D-5117 H H H H H 5-0Me-pyridin-3-yI 1 D-5118 H H H H H 6-0Me-pyridin-3-yI 1 D-5119 H H H H H 2,4-F 2-pyrdn-3-yl 1 D-5120 H H H H H 2,b-F2-pyrdn-3-yl 1 D-5121 H H H H H 2,6-F2-pyridh-3-y 1 D-5122 H H H H H 4,b-F 2-pyrdn-3-yl 1 0-5123 H H H H H 4,6-F 2 -pyrdn-3-yl 1 D-5124 H H H H H 2,4-C -pyridin-3-y 1 D-5125 H H H H H 2,5-C -pyridin-3-y 1 D-5126 H H H H H 2,6-C -pyridin-3-y 1 D-5127 H H H H H 4,5-C -pyridin-3-yl 1 D-5128 H H H H H 4,6-C2-pyridin-3-yl 1 D-5129 H H H H H 2-F-4-Cl-pyridh-3-yI 1 D-5130 H H H H H 2-F-5-Cl-pyridh-3-yI 1 D-5131 H H H H H 2-F-6-Cl-pyridh-3-yI 1 D-5132 H H H H H 4-F-2-Cl-pyridh-3-yI 1 D-5133 H H H H H 4-F-5-Cl-pyridh-3-yI 1 D-5134 H H H H H 4-F-6-Cl-pyridh-3-yI 1 D-5135 H H H H H 2-F-4-M e-pyridin-3-y 1 D-5136 H H H H H 2-F-5-M e-pyridin-3-y 1 D-5137 H H H H H 2-F-6-M e-pyridin-3-y 1 D-5138 H H H H H 4-F-2-M e-pyridin-3-y 1 D-5139 H H H H H 4-F-5-M e-pyridin-3-y 1 D-5140 H H H H H 4-F-6-M e-pyridin-3-y 1 D-5141 H H H H H 2-F-4-0Me-pyridin-3-yI 1 D-5142 H H H H H 2-F-5-0Me-pyridin-3-yI 1 D-5143 H H H H H 2-F-6-0Me-pyridin-3-yI 1 D-5144 H H H H H 4-F-2-0Me-pyridin-3-yI 1 D-5145 H H H H H 4-F-5-0Me-pyridin-3-y 1 D-5146 H H H H H 4-F-6-0Me-pyridin-3-yI 1 D-5147 H H H H H 2-CI-5-F-pyridh-3-yI 1 D-5148 H H H H H 2-CI-6-F-pyridh-3-yI 1 D-5149 H H H H H 4-CI-5-F-pyridh-3-yI 1 D-5150 H H H H H 4-CI-6-F-pyridh-3-yI 1 D-5151 H H H H H 2-CI-4-Me-pyridin-3-yI 1 D-5152 H H H H H 2-CI-5-Me-pyridin-3-yI 1 D-5153 H H H H H 2-CI-6-Me-pyridin-3-yI 1 D-5154 H H H H H 4-CI-2-Me-pyridin-3-yI 1 D-5155 H H H H H 4-CI-5-Me-pyridin-3-yI 1 D-5156 H H H H H 4-CI-6-Me-pyridin-3-yI 1 D-5157 H H H H H 2 -M e-5-F-pyridin-3-y 1 D-5158 H H H H H 2 -M e-6-F-pyridin-3-y 1 D-5159 H H H H H 4-M e-5-F-pyridin-3-y 1 D-5160 H H H H H 4-M e-6-F-pyridin-3-y 1 D-5161 H H H H H 2 -M e-5-CI-pyridin-3-yI 1 D-5162 H H H H H 2 -M e-6-CI-pyridin-3-yI 1 D-5163 H H H H H 4 -M e-5-CI-pyridin-3-yI 1 D-5164 H H H H H 4 -M e-6-CI-pyridin-3-yI 1 D-5165 H H H H H 2,4-(Me) 2-pyridin-3-yI 1 D-5166 H H H H H 2,b-(Me) 2-pyridin-3-yI 1
[0374]
[Table 249]
com pound R] R2 Rj R4 R3 0' p D-5167 H H H H H 2,6-(Me) 2-pyridin-3-yI 1 D-5168 H H H H H 4,b-(Me) 2-pyridin-3-yl 1 D-5169 H H H H H 4,6-(Me) 2-pyridin-3-yI 1 D-5170 H H H H H 2-MAe-4-0Me-pyridin-3-y 1 D-5171 H H H H H 2-MAe-5-0Me-pyridin-3-y 1 D-5172 H H H H H 2-MAe-6-0Me-pyridin-3-y 1 D-5173 H H H H H 4-Me-2-0Me-pyridin-3-y 1 D-5174 H H H H H 4-Me-5-0Me-pyridin-3-y 1 D-5175 H H H H H 4-Me-6-0Me-pyridin-3-y 1 D-5176 H H H H H 2-0F 3 -4-F-pyrdn-3-yl 1 D-5177 H H H H H 2-CF 3 -5-F-pyridh-3-yI 1 D-5178 H H H H H 2- F3 -6-F-pyrdn-3-yl 1 D-5179 H H H H H 4-GF 3 -2-F-pyrdn-3-yl 1 D-5180 H H H H H 4-CF 3 -5-F-pyridh-3-yI 1 D-5181 H H H H H 4-0F 3 -6-F-pyrdn-3-yl 1 D-5182 H H H H H 2-CF 3-4-Me-pyridh-3-y 1 D-5183 H H H H H 2-CF 3-5-Me-pyridh-3-y 1 D-5184 H H H H H 2-CF 3-6-Me-pyridh-3-y 1 D-5185 H H H H H 4-CF 3-2-Me-pyridh-3-y 1 D-5186 H H H H H 4-CF 3-5-Me-pyridh-3-y 1 D-5187 H H H H H 4-CF 3-6-M e-pyridn-3-y 1 D-5188 H H H H H 2-0Me-5-F-pyridin-3-yI 1 D-5189 H H H H H 2-0Me-6-F-pyridin-3-yI 1 D-5190 H H H H H 4-0Me-5-F-pyridin-3-yI 1 D-5191 H H H H H 4-0Me-6-F-pyridin-3-yI 1 D-5192 H H H H H 2-0Me-4-Cl-pyridh-3-yI 1 D-5193 H H H H H 2-0Me-5-Cl-pyridh-3-yI 1 D-5194 H H H H H 2-0Me-6-Cl-pyridh-3-yI 1 D-5195 H H H H H 4-0Me-2-Cl-pyridh-3-yI 1 D-5196 H H H H H 4-0Me-5-Cl-pyridh-3-yI 1 D-5197 H H H H H 4-0Me-6-Cl-pyridh-3-yI 1 D-5198 H H H H H 2-0Me-5-Me-pyridin-3-y 1 D-5199 H H H H H 2-0Me-6-Me-pyridin-3-y 1 D-5200 H H H H H 4-0Me-5-Me-pyridin-3-y 1 D-5201 H H H H H 4-0Me-6-Me-pyridin-3-y 1 D-5202 H H H H H 2,4-(0Me) 2 -pyridh-3-yI 1 D-5203 H H H H H 2,5-(0Me) 2 -pyridh-3-yI 1 D-5204 H H H H H 2,6-(0Me) 2 -pyridh-3-yI 1 D-5205 H H H H H 4,b-(0Me) 2 -pyrdn-3-yl 1 D-5206 H H H H H 4,6-(0Me) 2 -pyrdn-3-yl 1 D-5207 H H H H H pyridin-4-yI 1 D-5208 H H H H H 2-F-pyridin-4-yI 1 D-5209 H H H H H 3-F-pyridin-4-yI 1 D-5210 H H H H H 2-Cl-pyridin-4-y 1 D-5211 H H H H H 3-Cl-pyridin-4-y 1 D-5212 H H H H H 2-Me-pyridin-4-y 1 D-5213 H H H H H 3-Me-pyridin-4-y 1 D-5214 H H H H H 2-GF 3 -pyridn-4-yl 1 D-5215 H H H H H 3-CF3 -pyridh-4-y 1 D-5216 H H H H H 2-0Me-pyridin-4-y 1 D-5217 H H H H H 3-0Me-pyridin-4-yI 1 D-5218 H H H H H 2,3-F 2-pyrdn-4-yl 1 D-5219 H H H H H 2,5-F 2-pyridh-4-y 1 D-5220 H H H H H 2,6-F2-pyrdn-4-yl 1 D-5221 H H H H H 3,5-F2-pyridh-4-y 1 D-5222 H H H H H 2,3-C -pyridin-4-y 1 D-5223 H H H H H 2,5-C -pyrdin-4-y 1
[0375]
[Table 250]
com pound R] R2 Rj R4 R3 0' p D-5224 H H H H H 2,6-C -pyridin-4-y 1 D-5225 H H H H H 3,5-C -pyrdin-4-y 1 D-5226 H H H H H 3-F-2-Cl-pyridh-4-yI 1 D-5227 H H H H H 3-F-5--C-pyridh-4-yI 1 D-5228 H H H H H 3-F-6-Cl-pyridh-4-yI 1 D-5229 H H H H H 3-F-2-Me-pyridin-4-y 1 D-5230 H H H H H 3-F-5-Me-pyridin-4-y 1 D-5231 H H H H H 3-F-6-Me-pyridin-4-y 1 D-5232 H H H H H 3-F-2-0Me-pyridin-4-y 1 D-5233 H H H H H 3-F-5-0Me-pyridin-4-yI 1 D-5234 H H H H H 3-F-6-0Me-pyridin-4-yI 1 D-5235 H H H H H 3-CI-2-F-pyridh-4-yI 1 D-5236 H H H H H 3-CI-6-F-pyridh-4-y 1 D-5237 H H H H H 3-CI-2-M e-pyridin-4-y 1 D-5238 H H H H H 3-CI-5-M e-pyridin-4-y 1 D-5239 H H H H H 3-CI-6-M e-pyridin-4-y 1 D-5240 H H H H H 3-Me-2-F-pyridin-4-y 1 D-5241 H H H H H 3-Me-6-F-pyridin-4-y 1 D-5242 H H H H H 3 -M e-2-CI-pyridin-4-yI 1 D-5243 H H H H H 3 -M e-6-CI-pyridin-4-yI 1 D-5244 H H H H H 2,3-(Me) 2-pyridin-4-yI 1 D-5245 H H H H H 3,5-(Me) 2-pyridin-4-yl 1 D-5246 H H H H H 3,6-(Me) 2-pyridin-4-yl 1 D-5247 H H H H H 3-Me-2-0Me-pyridin-4-y 1 D-5248 H H H H H 3-Me-5-0Me-pyridin-4-y 1 D-5249 H H H H H 3-Me-6-0Me-pyridin-4-y 1 D-5250 H H H H H 3-CF 3 -2-F-pyridh-4-yI 1 D-5251 H H H H H 3-GF 3 -b-F-pyrdn-4-yl 1 D-5252 H H H H H 3-0F 3 -6-F-pyrdn-4-yl 1 D-5253 H H H H H 3-CF 3-2-Me-pyridh-4-y 1 D-5254 H H H H H 3-CF 3-5-Me-pyridh-4-y 1 D-5255 H H H H H 3-CF 3-6-Me-pyridh-4-y 1 D-5256 H H H H H 3-0Me-2-F-pyridin-4-yI 1 D-5257 H H H H H 3-0Me-6-F-pyridin-4-y 1 D-5258 H H H H H 3-0Me-2-Cl-pyridh-4-y 1 D-5259 H H H H H 3-0Me-5-Cl-pyridh-4-y 1 D-5260 H H H H H 3-0Me-6-Cl-pyridh-4-y 1 D-5261 H H H H H 3-0Me-2-Me-pyridin-4-y 1 D-5262 H H H H H 3-0Me-6-Me-pyridin-4-y 1 D-5263 H H H H H 2,3-(0Me) 2 -pyrdn-4-yl 1 D-5264 H H H H H 3,5-(0Me) 2 -pyrdn-4-yl 1 D-5265 H H H H H 3,6-(0Me) 2 -pyridh-4-yI 1 D-5266 H H H H H pyril id h-2-yI 1 D-5267 H H H H H pyril idih-4-yI 1 D-5268 H H H H H 5-F-pyrm idin-4-y 1 D-5269 H H H H H 5-Me-pyrikl idh-4-y 1 D-5270 H H H H H 5-CF 3 -pyrm din-4-yl 1 D-5271 H H H H H 5-OMe-pyril idin-4-yl 1 D-5272 H H H H H pyrinl idh-5-y 1 D-5273 H H H H H 4-F-pyrim1 idin-5-yl 1 D-5274 H H H H H 4-CI-pyril idin-5-yl 1 D-5275 H H H H H 4-Me-pyrikl idh-5-y 1 D-5276 H H H H H 4-CF3 -pyril idin-5-yl 1 D-5277 H H H H H 4-0Me-pyril idin-5-yl 1 D-5278 H H H H H pyridazin-3-yl 1 D-5279 H H H H H 4-F-pyridazh-3-yl 1 -5280 H H H H H 4-Cl-pyridazh-3-yI 1
[0376]
[Table 251]
com pound R' R2 R R4 Rb p D-5281 H H H H H 4-M e-pyridazin-3-yI 1 D-5282 H H H H H 4-CF 3-pyridazin-3-y 1 D-5283 H H H H H 4-0Me-pyridazh-3-yI 1 D-5284 H H H H H pyridazin-4-yI 1 D-5285 H H H H H 3-F-pyridazh-4-yI 1 D-5286 H H H H H 3-Cl-pyridazh-4-yI 1 D-5287 H H H H H 3-M e-pyridazin-4-y 1 D-5288 H H H H H 3-CF3 -pyridazin-4-y 1 D-5289 H H H H H 3-0Me-pyridazh-4-yI 1 D-5290 H H H H H 5-F-pyridazh-4-y 1 D-5291 H H H H H 5-Cl-pyridazh-4-yI 1 D-5292 H H H H H 5-M e-pyridazin-4-y 1 D-5293 H H H H H b-F 3--pyrdiazin-4-yl 1 D-5294 H H H H H 5-0Me-pyridazh-4-yI 1 D-5295 H H H H H thiophen-2-yI 1 D-5296 H H H H H 3-F-thiophen-2-y 1 D-5297 H H H H H 3-Cl-thiophen-2-y 1 D-5298 H H H H H 3-Me-thiophen-2-y 1 D-5299 H H H H H 3-0F 3 -thiophen-2-yl 1 D-5300 H H H H H 3-0Me-thiophen-2-y 1 D-5301 H H H H H thiophen-3-yI 1 D-5302 H H H H H 2-F-thiophen-3-y 1 D-5303 H H H H H 2-Cl-thiophen-3-y 1 D-5304 H H H H H 2-Me-thiophen-3-y 1 D-5305 H H H H H 2-CF 3 -thiophen-3-yI 1 D-5306 H H H H H 2-0Me-thiophen-3-y 1 D-5307 H H H H H 4-F-thiophen-3-y 1 D-5308 H H H H H 4-Cl-thiophen-3-y 1 D-5309 H H H H H 4-Me-thiophen-3-y 1 D-5310 H H H H H 4-CF 3 -thiophen-3-yI 1 D-5311 H H H H H 4-0Me-thiophen-3-y 1 D-5312 H H H H H thiazol-2-y 1 D-5313 H H H H H thiazol-4-yI 1 D -5314 H H H H H 5-F-th iazo I-4-y 1 1 D-5315 H H H H H 5-M e-thibzol-4-y 1 D-5316 H H H H H 5-CF3 -thiazol-4-y 1 D-5317 H H H H H 5-0Me-thbzol-4-y 1 D-5318 H H H H H thiazol-5-yI 1 D-5319 H H H H H 4-F-thiazol-5-yI 1 D-5320 H H H H H 4-Me-thbzol-5-yl 1 D-5321 H H H H H 4-CF3 -thiazol-5-y 1 D-5322 H H H H H 4-0Me-thbzol-5-y 1 D-5323 H H H H H 1H-pyrrol1-y 1 D-5324 H H H H H 2-F-1/H-pyrrol-1-y 1 D-5325 H H H H H 2-M e-1H-pyrrol1-y 1 D-5326 H H H H H 2- F3 -1H-pyrrol1-yl 1 D-5327 H H H H H 2-0Me-1 H-pyrrol1-y 1 D-5328 H H H H H 1 H-pyrrol-2-y 1 D-5329 H H H H H 1 -M e-1H-pyrrol-2-y 1 D-5330 H H H H H 3-F-1/H-pyrrol-2-y 1 D-5331 H H H H H 3-M e-1H-pyrrol-2-y 1 D-5332 H H H H H 3-CF3 -1/H-pyrrol-2-y 1 D-5333 H H H H H 3-0Me-1 H-pyrrol-2-y 1 D-5334 H H H H H 1-M e-3-F-1H-pyrrol-2-y 1 D-5335 H H H H H 1,3-(Me) 2 -1 H-pyrrol-2-yl 1 D-5336 H H H H H 1-Me-3-CF 3-1 H-pyrrol-2-y 1 D-5337 H H H H H 1 -M e-3-0Me-1 H-pyrrol-2-y 1
[0377]
[Table 252]
com pound R' R2 R R4 Rb p D-5338 H H H H H 1 H-pyrrol-3-y 1 D-5339 H H H H H 1-M e-1 H-pyrrol-3-y 1 D-5340 H H H H H 2-F-1 H-pyrrol-3-yI 1 D-5341 H H H H H 2-M e-1 H-pyrrol-3-y 1 D-5342 H H H H H 2-0F3 -1H-pyrrol-3-yl 1 D-5343 H H H H H 2-0Me-1 H-pyrrol-3-y 1 D-5344 H H H H H 1 -M e-2-F-1 H-pyrrol-3-yI 1 D-5345 H H H H H 1,2-(Me) 2-1 H-pyrrol-3-y 1 D-5346 H H H H H 1-Me-2-CF 3-1/H-pyrrol-3-y 1 D-5347 H H H H H 1 -M e-2-0Me-1 H-pyrrol-3-y 1 D-5348 H H H H H 4-F-1 H-pyrrol-3-yI 1 D-5349 H H H H H 4-M e-1 H-pyrrol-3-y 1 D-5350 H H H H H 4- F 3 -1 H-pyrrol-3-yl 1 D-5351 H H H H H 4-0Me-1 H-pyrrol-3-yI 1 D-5352 H H H H H 1 -M e-4-F-1 H-pyrrol-3-y 1 D-5353 H H H H H 1,4-(Me) 2-1 H-pyrrol-3-y 1 D-5354 H H H H H 1-Me-4-CF 3 -1/H-pyrrol-3-y 1 D-5355 H H H H H 1 -M e-4-0Me-1 H-pyrrol-3-y 1 D-5356 H H H H H 1 H-pyrazol1-y 1 D-5357 H H H H H 5-F-1 H-pyrazol1-yI 1 D-5358 H H H H H 5-CI-1H-pyrazol1-y 1 D-5359 H H H H H 5-M e-1 H-pyrazol-1-yl 1 D-5360 H H H H H 5-CF 3 -1/H-pyrazol-1-y 1 D-5361 H H H H H 5-0Me-1H-pyrazol1-yI 1 D-5362 H H H H H 1 H-pyrazol-3-yI 1 D-5363 H H H H H 1-M e-1 H-pyrazol-3-yl 1 D-5364 H H H H H 4-F-1 H-pyrazol-3-yI 1 D-5365 H H H H H 4-CI-1H-pyrazol-3-y 1 D-5366 H H H H H 4-M e-1 H-pyrazol-3-yl 1 D-5367 H H H H H 4-CF-1H-pyrazol-3-y 1 D-5368 H H H H H 4-OMe-1 H-pyrazol-3-yI 1 D-5369 H H H H H 1 -M e-4-F-1 H-pyrazol-3-yI 1 D-5370 H H H H H 1 -M e-4-CI1H-pyrazol-3-y 1 D-5371 H H H H H 1,4-(Me) 2-1 H-pyrazol-3-y 1 D-5372 H H H H H 1-Me-4-CF 3-1H-pyrazol-3-yI 1 D-5373 H H H H H 1-Me-4-0Me-1 H-pyrazol-3-y 1 D-5374 H H H H H 1 H-pyrazol-4-yI 1 D-5375 H H H H H 1-M e-1 H-pyrazol-4-yl 1 D-5376 H H H H H 3-F-1 H-pyrazol-4-yI 1 D-5377 H H H H H 3-CI-1 H-pyrazol-4-y 1 D-5378 H H H H H 3-M e-1 H-pyrazol-4-yl 1 D-5379 H H H H H 3-%-F1H-pyrazo-4-y 1 D-5380 H H H H H 3-0Me-1 H-pyrazol-4-y 1 D-5381 H H H H H 1 -M e-3-F-1 H-pyrazol-4-yI 1 D-5382 H H H H H 1 -M e-3-CI1HH-pyrazol-4-y 1 D-5383 H H H H H 1,3-(Me) 2-1/H-pyrazol-4-yl 1 D-5384 H H H H H 1 -M e-3-CF 3-1 H-pyrazol-4-y 1 D-5385 H H H H H 1-Me-3-0Me-1 H-pyrazol-4-y 1 D-5386 H H H H H 5-F-1 H-pyrazol-4-yI 1 D-5387 H H H H H 5-CI-1 H-pyrazol-4-yI 1 D-5388 H H H H H 5-Me-1/H-pyrazol-4-y 1 D-5389 H H H H H 5-CF-1H-pyrazo-4-y 1 D-5390 H H H H H 5-0Me-1 H-pyrazol-4-y 1 D-5391 H H H H H 1 -M e-5-F-1 H-pyrazol-4-yI 1 D-5392 H H H H H 1 -M e-5-CI1HH-pyrazol-4-y 1 D-5393 H H H H H 1,5-(Me) 2-1 H-pyrazol-4-yl 1 -5394 H H H H H 1-M e-5-0F 3-1 H-pyrazol-4-yl 1
[0378]
[Table 253]
cornpound - R R2 3 R-iR 4-R b p -5395 H H H H H 1-M e-5-OM e-/-pyrazok4A-yI 1 -5396 H H H H H 1 H-pyrazo F-5-y 1 1 -5397 H H H H H 1 -M e-1 H -pyrazo -5-y 1 1 -5398 H H H H H 4-F-1 H-pyrazoF-5-y 1 1 -5399 H H H H H 4-CF11 -pyrazok--I 1 -5400 H H H H H 4-M e-1 H -pyrazo -5-y 1 1 -5401 H H H H H 4-0F 3 1/H-pyrazo[1-5-y1 1 -5402 H H H H H 4-OM e-1 H-pyrazok--I 1 -5403 H H H H H 1 -Mve-4-F-1 H -pyrazok 5-y 1 1 -5404 H H H H H 1 -Mve-4--C H1H-pyrazok 5-y 1 1 -5405 H H H H H 1,4-(M e) 2 -1 H -pvrazoI1-5-yvI 1 -5406 H H H H H 1 -Mve-4-0F 3 -1 H-pyrazok--I 1 -5407 H H H H H 1-AMe-4-OM e-1 H -pyrazok--I 1 -5408 H H H H H furan-2-vI1 1 -5409 H H H H H 3-F-turan-2-vI1 1 -5410 H H H H H 3-M e -tura n-2-yvI 1 -5411 H H H H H 3 -0F 3 -fu ra n-2 -yI 1 -5412 H H H H H 3-OM e-tu ran-2-vI1 1 -5413 H H H H H fu ran-3-vI1 1 -5414 H H H H H 2-F-tu ran-3-vI1 1 -5415 H H H H H 2 -Mve -tura n-3 -yI 1 -5416 H H H H H 2-0F3 -fu ran-3-vI1 1 -5417 H H H H H 2-OM e-tu ran-3-vI1 1 -5418 H H H H H 4-F-tu ran-3-vI1 1 -5419 H H H H H 4-Mvle-turan-3-vI1 1 -5420 H H H H H 4-0F3 -fu ran-3-vI1 1 -5421 H H H H H 4-OM e-tu ran-3-vI1 1 -5422 H H H H H Loxazok3-vI1 1 -5423 H H H H H 4-F-isoxazo[-3-vI1 1 -5424 H H H H H 4-Mvle-isoxazok 3-vI1 1 -5425 H H H H H 4-,uF3 -Esoxazo--vI 1 -5426 H H H H H 4-OM e-isoxazok 3-vI1 1 -5427 H H H H H Loxazok4-vI1 1 -5428 H H H H H 5-F-isoxazo[-4-vI1 1 -5429 H H H H H 5-Mvle-isoxazok 4-vI1 1 -5430 H H H H H 5-C F 3 Loxazo[ --v1 1 -5431 H H H H H 5-OM e-isoxazo4A-vI1 1 -5432 H H H H H Loxazok5-vI1 1 -5433 H H H H H 4-F-isoxazo-5-vI1 1 -5434 H H H H H 4-M e-isoxazo-S-vi1 1 -5435 H H H H H 4-C F 3 Loxazo-S-vI1 1 -5436 H H H H H 4-OM e-isoxazok-viy 1 -5437 H H H H H 1 H -1,2,3-tr ia zok1-vyl 1 -5438 H H H H H 5-F-1 H-1,2,3-trbzoHl-I1 1 -5439 H H H H H 5-M e-1 H-1 2,3-triazo[-1 1 -5440 H H H H H b-0%-ilH-i,2,3-trbzo[-vI 1 -5441 H H H H H 5-OM e-1lHl-1,2,3-trbzo[-1 1 -5442 H H H H H 1lHl-1,2,3tr ia zol1-4 -y1 1 -5443 H H H H H S-F-ill-,2,3-trbzo-4-vI1 1 -5444 H H H H H 5-M e-1 H-1 2,3-triazo[ --v1 1 -5445 H H H H H S-0%-ill-1,2,3-trbzo --vI 1 -5446 H H H H H 5-OM e-1lll-1,2,3-trbzo --v1 1 -5447 H H H H H 1lHl-1,2,3tr ia zo1-5 -yI 1 -5448 H H H H H 4-F-ilH-,2,3-trbzo -5-vI1 1 -5449 H H H H H 4-M e-1ll-1 2,3-triazoP-S-vi 1 -5450 H H H H H 4-0%3-il-,2,3-trbzo-S-vI 1 -S4S1 H H H H I H 4-OMe-ill-i,2,3-trbzo-S-vi 1
[0379]
[Table 254] cornpound R R2 wR RT4 R p -5452 H H H H H 1 H -1,2,4-triazo1-1-yI1 1 -5453 H H H H H 5-M e-1 H-1 2,4-triazo-1 1 -5454 H H H H H 5-F-1 H-1,2,4-trbzoHl-vI1 1 -5455 H H H H H b-0%-ilH-1,2,4-trbzo[Hl-yI1 1 -5456 H H H H H 5-OM e-1H -1,2,4-trbzokP1-yI1 1 -5457 H H H H H 1 H -1,2,4-triazok13 -yI1 1 -5458 H H H H H 1 -M e-1 H-1 2,4-triazoF-3-yI1 1 -5459 H H H H H 1 H -1,2,4tria zol1-5 -y I1 -5460 H H H H H 1 -M e-1 H-1 2,4-triazoF-5-yi 1 -5461 H H H H H 3,5-(M e) 2 -iSoxazo[-4-v I1 -5462 H H H H H 3,5-(Et) 2 Lsxazo[-4-vI1 1 -5463 H H H H H 1,3,5-(M e) 3 -1 1-pvrazo[-4-vI1 1 -5464 H H H H H qu ino lin-4-y 1 1 -5465 H H H H H isoqu ino lin-4-y 1 1 -5466 H H H H H 3,6-(O M e) 2 -pyrbdazih-4-v I 1 -5467 H H H H H 2,4-( M e) 2 -pvrinl id h-b-v I 1
[0380]
[Table 255]
3 2 R R O
R4 N
1 5 (O)p R R
com pound R' R RT R4 R5 (R), p E-0001 H H H H H H 0 E-0002 H H H H H 2-F 0 E-0003 H H H H H 3-F 0 E-0004 H H H H H 4-F 0 E-0005 H H H H H 2-Cl 0 E-0006 H H H H H 3-Cl 0 E-0007 H H H H H 4-Cl 0 E-0008 H H H H H 2-Br 0 E-0009 H H H H H 3-Br 0 E-0010 H H H H H 4-Br 0 E-0011 H H H H H 2-I 0 E-0012 H H H H H 3-I 0 E-0013 H H H H H 4-I 0 E-0014 H H H H H 2-OH 0 E-0015 H H H H H 3-OH 0 E-0016 H H H H H 4-OH 0 E-0017 H H H H H 2-SH 0 E-0018 H H H H H 3-SH 0 E-0019 H H H H H 4-SH 0 E-0020 H H H H H 2-M e 0 E-0021 H H H H H 3-M e 0 E-0022 H H H H H 4-M e 0 E-0023 H H H H H 2-Et 0 E-0024 H H H H H 3-Et 0 E-0025 H H H H H 4-Et 0 E-0026 H H H H H 2-Pr 0 E-0027 H H H H H 3-Pr 0 E-0028 H H H H H 4-Pr 0 E-0029 H H H H H 2-i-Pr 0 E-0030 H H H H H 3-i-Pr 0 E-0031 H H H H H 4-i-Pr 0 E-0032 H H H H H 2-Bu 0 E-0033 H H H H H 3-Bu 0 E-0034 H H H H H 4-Bu 0 E-0035 H H H H H 2-s-Bu 0 E-0036 H H H H H 3-s-Bu 0 E-0037 H H H H H 4-s-Bu 0 E-0038 H H H H H 2-i-Bu 0 E-039 H H H H H 3-i-Bu 0 E-0040 H H H H H 4-i-Bu 0 E-0041 H H H H H 2-t-Bu 0 E-0042 H H H H H 3-t-Bu 0 E-0043 H H H H H 4-t-Bu 0 E-0044 H H H H H 2-CF 3 0 E-0045 H H H H H 3-CF 3 0 E-0046 H H H H H 4-CF3 0 E-0047 H H H H H 2-CHF 2 0 E-0048 H H H H H 3-CHF 2 0 E-0049 H H H H H 4-CHF 2 0 E-0050 H H H H H 2-CH 2F 0 E-0051 H H H H H 3-CH 2F 0 E-0052 H H H H H 4-CH 2F 0
[0381]
[Table 256]
com pound R' R2 R R4 R (Rd)m P E-0053 H H H H H 2-CF 2C 1 0 E-0054 H H H H H 3-CF 2C1 0 E-0055 H H H H H 4-CF 2C1 0 E-0056 H H H H H 2-CF(F 3 ) 2 0 E-0057 H H H H H 3-CF(F 3 ) 2 0 E-0058 H H H H H 4-C -(0 3 ) 2 0 E-0059 H H H H H 2-cycobpropy 0 E-0060 H H H H H 3-cycobpropy 0 E-0061 H H H H H 4-cycobpropy 0 E-0062 H H H H H 2-cyclobutyl 0 E-0063 H H H H H 3-cyclobutyl 0 E-0064 H H H H H 4-cyclobutyl 0 E-0065 H H H H H 2-cycbpentyl 0 E-0066 H H H H H 3-cycbpentyl 0 E-0067 H H H H H 4-cycbpentyl 0 E-0068 H H H H H 2-(cyclopropyImethyD 0 E-0069 H H H H H 3-(cyclopropyImethyD 0 E-0070 H H H H H 4-(cyclopropyImethyD 0 E-0071 H H H H H 2-(cycobbuty IethyD 0 E-0072 H H H H H 3-(cycobbuty IethyD 0 E-0073 H H H H H 4-(cycobbuty IethyD 0 E-0074 H H H H H 2-(cycbpentyh ethyD 0 E-0075 H H H H H 3-(cycbpentyh ethyD 0 E-0076 H H H H H 4-(cycbpentyh ethyD 0 E-0077 H H H H H 2-(cyclopropylethyD 0 E-0078 H H H H H 3-(cyclopropylethyD 0 E-0079 H H H H H 4-(cyclopropylethyD 0 E-0080 H H H H H 2-(2,2-difluorocycbpropyD 0 E-0081 H H H H H 3-(2,2-difluorocycbpropyD 0 E-0082 H H H H H 4-(2,2-difluorocycbpropyD 0 E-0083 H H H H H 2-(2,2-dichbrocycbpropyD 0 E-0084 H H H H H 3-(2,2-dichbrocycbpropyD 0 E-0085 H H H H H 4-(2,2-dichbrocycbpropyD 0 E-0086 H H H H H 2-ethenyl 0 E-0087 H H H H H 3-ethenyl 0 E-0088 H H H H H 4-ethenyl 0 E-0089 H H H H H 2-allyl 0 E-0090 H H H H H 3-allyl 0 E-0091 H H H H H 4-allyl 0 E-0092 H H H H H 2-(prop-1-en-1-y D 0 E-0093 H H H H H 3-(prop-1-en-1-y D 0 E-0094 H H H H H 4-(prop-1-en-1-y D 0 E-0095 H H H H H 2-(trifluoroethenyD 0 E-0096 H H H H H 3-(trifluoroethenyD 0 E-0097 H H H H H 4-(trifluoroethenyD 0 E-0098 H H H H H 2-(2,2-dichbroethenyD 0 E-0099 H H H H H 3-(2,2-dichbroethenyD 0 E-0100 H H H H H 4-(2,2-dichbroethenyD 0 E-0101 H H H H H 2-ethynyl 0 E-0102 H H H H H 3-ethynyl 0 E-0103 H H H H H 4-ethynyl 0 E-0104 H H H H H 2-(1-propyn-1-yD 0 E-0105 H H H H H 3-(1-propyn-1-yD 0 E-0106 H H H H H 4-(1-propyn-1-yD 0 E-0107 H H H H H 2-(2-propyn-1-yD 0 E-0108 H H H H H 3-(2-propyn-1-y D 0 E-0109 H H H H H 4-(2-propyn-1-yl 0
[0382]
[Table 257]
com pound R R2 R R (R)m P E-0110 H H H H H 2-(2-cycobpropylethynyD 0 E-0111 H H H H H 3-(2-cycobpropylethynyD 0 E-0112 H H H H H 4-(2-cycobpropylethynyD 0 E-0113 H H H H H 2-(2-chbroethynyD 0 E-0114 H H H H H 3-(2-chbroethynyD 0 E-0115 H H H H H 4-(2-chbroethynyD 0 E-0116 H H H H H 2-(2-brom oethynyl) 0 E-0117 H H H H H 3-(2-brom oethynyl) 0 E-0118 H H H H H 4-(2-brom oethynyl) 0 E-0119 H H H H H 2-0M e 0 E-0120 H H H H H 3-0M e 0 E-0121 H H H H H 4-0M e 0 E-0122 H H H H H 2-0Et 0 E-0123 H H H H H 3-0Et 0 E-0124 H H H H H 4-0Et 0 E-0125 H H H H H 2-0Pr 0 E-0126 H H H H H 3-0Pr 0 E-0127 H H H H H 4-0Pr 0 E-0128 H H H H H 2-0 (/-Pr) 0 E-0129 H H H H H 3-0 (/-Pr) 0 E-0130 H H H H H 4-0 (/-Pr) 0 E-0131 H H H H H 2-0Bu 0 E-0132 H H H H H 3-0Bu 0 E-0133 H H H H H 4-0Bu 0 E-0134 H H H H H 2-0 (s-Bu) 0 E-0135 H H H H H 3-0 (s-Bu) 0 E-0136 H H H H H 4-0 (s-Bu) 0 E-0137 H H H H H 2-0 (/-Bu) 0 E-0138 H H H H H 3-0 (/-Bu) 0 E-0139 H H H H H 4-0 (/-Bu) 0 E-0140 H H H H H 2-0 (t-Bu) 0 E-0141 H H H H H 3-0 (t-Bu) 0 E-0142 H H H H H 4-0 (t-Bu) 0 E-0143 H H H H H 2-0CF 0 E-0144 H H H H H 3-0CF 0 E-0145 H H H H H 4-0CF 0 E-0146 H H H H H 2-0CHF 2 0 E-0147 H H H H H 3-0CHF 2 0 E-0148 H H H H H 4-0CHF 2 0 E-0149 H H H H H 2-0CH 20F 3 0 E-0150 H H H H H 3-0CH 2 CF3 0 E-0151 H H H H H 4-0CH 20F 3 0 E-0152 H H H H H 2-(cycbpropy bxy) 0 E-0153 H H H H H 3-(cycbpropy bxy) 0 E-0154 H H H H H 4-(cycbpropy bxy) 0 E-0155 H H H H H 2-(cyclobutybxy) 0 E-0156 H H H H H 3-(cyclobutybxy) 0 E-0157 H H H H H 4-(cyclobutybxy) 0 E-0158 H H H H H 2-(cyclopentybxy) 0 E-0159 H H H H H 3-(cyclopentybxy) 0 E-0160 H H H H H 4-(cyclopentybxy) 0 E-0161 H H H H H 2-((2,2-dichbrocycbpropyDoxy) 0 E-0162 H H H H H 3-((2,2-dichbrocycbpropyDoxy) 0 E-0163 H H H H H 4-((2,2-dichbrocycbpropyDoxy) 0 E-0164 H H H H H 2-(cycbpropyhiethoxy) 0 E-0165 H H H H H 3-(cycbpropyhiethoxy) 0 E-0166 H H H H H 4-(cycbpropyhiethoxy) 0
[0383]
[Table 258]
com pound R R2 R R (R)m P E-0167 H H H H H 2-((2,2-difluorocycbpropyDm ethoxy) 0 E-0168 H H H H H 3-((2,2-difluorocycbpropyDm ethoxy) 0 E-0169 H H H H H 4-((2,2-difluorocycbpropyDm ethoxy) 0 E-0170 H H H H H 2-(oxiran-2-y) 0 E-0171 H H H H H 3-(oxiran-2-yl) 0 E-0172 H H H H H 4-(oxiran-2-y) 0 E-0173 H H H H H 2-(oxiran-2-yh ethyD 0 E-0174 H H H H H 3-(oxiran-2-yh ethyD 0 E-0175 H H H H H 4-(oxiran-2-yh ethyD 0 E-0176 H H H H H 2-SMe 0 E-0177 H H H H H 3-SMe 0 E-0178 H H H H H 4-SMe 0 E-0179 H H H H H 2-SEt 0 E-0180 H H H H H 3-SEt 0 E-0181 H H H H H 4-SEt 0 E-0182 H H H H H 2-S(=0)Me 0 E-0183 H H H H H 3-S(=0)Me 0 E-0184 H H H H H 4-S(=0)Me 0 E-0185 H H H H H 2-S(=O) 2Me 0 E-0186 H H H H H 3-S(=O) 2Me 0 E-0187 H H H H H 4-S (=0) 2M e 0 E-0188 H H H H H 2-SCF, 0 E-0189 H H H H H 3-SCF, 0 E-0190 H H H H H 4-SCF, 0 E-0191 H H H H H 2-S(=0)CF 3 0 E-0192 H H H H H 3-S(=0)CF 3 0 E-0193 H H H H H 4-S(=0)CF3 0 E-0194 H H H H H 2-S(=0) 20F 3 0 E-0195 H H H H H 3-S(=0) 2CF 3 0 E-0196 H H H H H 4-S(=0) 2CF3 0 E-0197 H H H H H 2-SCF(F 3 ) 2 0 E-0198 H H H H H 3-SCF (CF 3) 2 0 E-0199 H H H H H 4-SCF (CF3) 2 0 E-0200 H H H H H 2-(cycbpropylthio) 0 E-0201 H H H H H 3-(cycbpropylthio) 0 E-0202 H H H H H 4-(cycbpropylthio) 0 E-0203 H H H H H 2-(cycbpropysulfinyD 0 E-0204 H H H H H 3-(cycbpropysulfinyD 0 E-0205 H H H H H 4-(cycbpropysulfiny D 0 E-0206 H H H H H 2-(cycbpropyIsulfonyD 0 E-0207 H H H H H 3-(cycbpropyIsulfonyD 0 E-0208 H H H H H 4-(cycbpropyIsulfonyD 0 E-0209 H H H H H 2-((cycbpropyI ethyI)thio) 0 E-0210 H H H H H 3-((cycbpropyI ethyl)thio) 0 E-0211 H H H H H 4-((cycbpropyI ethyl)thio) 0 E-0212 H H H H H 2-((cycbpropy ethylsulfinyD 0 E-0213 H H H H H 3-((cycbpropy ethylsulfinyD 0 E-0214 H H H H H 4-((cycobpropy IethyDsulfinyD 0 E-0215 H H H H H 2-((cycbpropy ethyDsulfonyD 0 E-0216 H H H H H 3-((cycbpropy ethyDsulfonyD 0 E-0217 H H H H H 4-((cycbpropy IethylsulfonyD 0 E-0218 H H H H H 2-(((2,2-difluorocycbpropyDm ethylDthio) 0 E-0219 H H H H H 3-(((2,2-difluorocycbpropyDm ethyDthio) 0 E-0220 H H H H H 4-(((2,2-difluorocycbpropyDm ethylDthio) 0 E-0221 H H H H H 2-(((2,2-diflorocycbpropylDm ethylsulfinyD 0 E-0222 H H H H H 3-(((2,2-diflorocycbpropyDm ethyDsulfinyD 0 E-0223 H H H H H 4-(((2,2-dfLiorocycbpropyDm ethylsulfinyD 0
[0384]
[Table 259]
com pound R R2 R R (R)m P E-0224 H H H H H 2-(((2,2-difluorocycobpropyl)m ethyl)sulfonyD 0 E-0225 H H H H H 3-(((2,2-difluorocycobpropyl)m ethyl)sulfonyD 0 E-0226 H H H H H 4-(((2,2-difluorocycobpropyl)m ethyl)sulfonyD 0 E-0227 H H H H H 2-C(=0)Me 0 E-0228 H H H H H 3-C(=0)Me 0 E-0229 H H H H H 4-C(=0)Me 0 E-0230 H H H H H 2-C(=0)Et 0 E-0231 H H H H H 3-C(=0)Et 0 E-0232 H H H H H 4-C(=0)Et 0 E-0233 H H H H H 2-0(=0)0%, 0 E-0234 H H H H H 3-0(=0)F 3 0 E-0235 H H H H H 4-C (=0)CF3 0 E-0236 H H H H H 2-C(=0)0Me 0 E-0237 H H H H H 3-C(=0)0Me 0 E-0238 H H H H H 4-C(=0)0Me 0 E-0239 H H H H H 2-C(=0)0Et 0 E-0240 H H H H H 3-C(=0)0Et 0 E-0241 H H H H H 4-C(=0)0Et 0 E-0242 H H H H H 2-0(=0)NH 2 0 E-0243 H H H H H 3-0(=0)NH 2 0 E-0244 H H H H H 4-C (=0)NH 2 0 E-0245 H H H H H 2-C(=0)NHMe 0 E-0246 H H H H H 3-C(=0)NHMe 0 E-0247 H H H H H 4-C(=0)NHMe 0 E-0248 H H H H H 2-C(=0)NMe 2 0 E-0249 H H H H H 3-C(=0)NMe 2 0 E-0250 H H H H H 4-C(=0)NMe 2 0 E-0251 H H H H H 2-CH 2 0(=0)CH 3 0 E-0252 H H H H H 3-CH 2 0(=0)CH 3 0 E-0253 H H H H H 4-CH 2 C(=0)CH 3 0 E-0254 H H H H H 2-CH 2 0(=0)0%3 0 E-0255 H H H H H 3-CH 2C(=0)CF 0 E-0256 H H H H H 4-CH 2C(=0)CF 0 E-0257 H H H H H 2-CH 2C(=0)0CH 3 0 E-0258 H H H H H 3-CH 2C(=0)0CH 3 0 E-0259 H H H H H 4-CH 2C(=0)0CH3 0 E-0260 H H H H H 2-CH 2 0H 0 E-0261 H H H H H 3-CH 2 0H 0 E-0262 H H H H H 4-CH 2 0H 0 E-0263 H H H H H 2-CH 200H 3 0 E-0264 H H H H H 3-CH 20CH 3 0 E-0265 H H H H H 4-CH 200H 3 0 E-0266 H H H H H 2-CH 2 0CH 2CH 3 0 E-0267 H H H H H 3-CH 2 00H 2CH 3 0 E-0268 H H H H H 4-CH 2 0CH 2CH 3 0 E-0269 H H H H H 2-CH(CH 3)0CH 3 0 E-0270 H H H H H 3-CH(CH 3)0CH 3 0 E-0271 H H H H H 4-CH(CH 3)0CH 3 0 E-0272 H H H H H 2-CH 2 CH 20CH 3 0 E-0273 H H H H H 3-CH 2 CH 200H 3 0 E-0274 H H H H H 4-CH 2 CH 20CH 3 0 E-0275 H H H H H 2-CH 20CF3 0 E-0276 H H H H H 3-CH 20CF3 0 E-0277 H H H H H 4-CH 20CF3 0 E-0278 H H H H H 2-CF 200H 3 0 E-0279 H H H H H 3-CF 20CH 3 0 E-0280 H H H H H 4-GF 200H 3 0
[0385]
[Table 260]
com pound R' R2 R R R (R°)m P E-0281 H H H H H 2-0FGF 2 2 0F 3 0 E-0282 H H H H H 3-0FGF 2 2 0F 3 0 E-0283 H H H H H 4-GF 2 F 2 0F 3 0 E-0284 H H H H H 2-0C(=0)GH 3 0 E-0285 H H H H H 3-0C(=0)GH 3 0 E-0286 H H H H H 4-0(=U)GH 3 0 E-0287 H H H H H 2-U0(=U)GF 3 0 E-0288 H H H H H 3-U0(=U)0F 3 0 E-0289 H H H H H 4-U0(=U)CF 3 0 E-0290 H H H H H 2-00(=0)NH2 0 E-0291 H H H H H 3-0C(=0)NH 2 0 E-0292 H H H H H 4-U0(=U)NH 2 0 E-0293 H H H H H 2-0C(=0)NHCH 3 0 E-0294 H H H H H 3-0C(=0)NHCH 3 0 E-0295 H H H H H 4-U0(=U)NHOH 3 0 E-0296 H H H H H 2-U0(=U)N (H 3) 2 0 E-0297 H H H H H 3-0(=U)N (H 3) 2 0 E-0298 H H H H H 4-0C(=0)N (H 3) 2 0 E-0299 H H H H H 2-GH 2 00(=0)NH 2 0 E-0300 H H H H H 3-GH 2 00(=0)NH 2 0 E-0301 H H H H H 4-CH 200(=)NH2 0 E-0302 H H H H H 2-CH 20(=U)NHOH 3 0 E-0303 H H H H H 3-GH 20(=O)NHCH 3 0 E-0304 H H H H H 4-GH 200(=0)NHCH 3 0 E-0305 H H H H H 2-CH 20(=O)N (H 3) 2 0 E-0306 H H H H H 3-CH 20(=O)N (H 3) 2 0 E-0307 H H H H H 4-CH 20(=O)N (H 3) 2 0 E-0308 H H H H H 2-0C(=0)0GH 3 0 E-0309 H H H H H 3-0C(=0)0GH 3 0 E-0310 H H H H H 4-UC(=U)UGH 3 0 E-0311 H H H H H 2-GH 2 0(=0)0GH 3 0 E-0312 H H H H H 3-CH 20(=O)OH 3 0 E-0313 H H H H H 4-CH 20G(=O)OGH 3 0 E-0314 H H H H H 2-CH 20(=U)CH 3 0 E-0315 H H H H H 3-CH 20(=U)GH 3 0 E-0316 H H H H H 4-CH 20(=U)GH 3 0 E-0317 H H H H H 2-U S=0) 2CH 3 0 E-0318 H H H H H 3-U S=0) 20H3 0 E-0319 H H H H H 4-USt=0) 20H 3 0 E-0320 H H H H H 2-CH 2SCH 3 0 E-0321 H H H H H 3-CH 2SOH 3 0 E-0322 H H H H H 4-CH 2SCH 3 0 E-0323 H H H H H 2-CH 2 S(=U)CH 3 0 E-0324 H H H H H 3-CH 2 S(=0)GH 3 0 E-0325 H H H H H 4-CH 2 S(=U)CH 3 0 E-0326 H H H H H 2-CH 2S(=0) 20H 3 0 E-0327 H H H H H 3-CH 2S(=U) 2 H 3 0 E-0328 H H H H H 4-CH 2S(=U) 2 H3 0 E-0329 H H H H H 2-CH 2SGF 3 0 E-0330 H H H H H 3-GH 2SCF 3 0 E-0331 H H H H H 4-CH 2SGF 3 0 E-0332 H H H H H 2-CH 2 S(=U)GF 3 0 E-0333 H H H H H 3-CH 2 S(=U)GF 3 0 E-0334 H H H H H 4-CH 2 S(=0)OF 3 0 E-0335 H H H H H 2-CH 2 S=0) 20F 3 0 E-0336 H H H H H 3-CH 2 S(=U) 2GF 3 0 E-0337 H H H H H 4-CH 2 S=0) 0 2 3 0
[0386]
[Table 261]
com pound R R2 R R (R)m P E-0338 H H H H H 2-pheny 1 0 E-0339 H H H H H 3-pheny 1 0 E-0340 H H H H H 4-pheny 1 0 E-0341 H H H H H 2-(pheny bxy) 0 E-0342 H H H H H 3-(pheny bxy) 0 E-0343 H H H H H 4-(pheny bxy) 0 E-0344 H H H H H 2-benzy 1 0 E-0345 H H H H H 3-benzy 1 0 E-0346 H H H H H 4-benzy 1 0 E-0347 H H H H H 2-(benzybxy) 0 E-0348 H H H H H 3-(benzybxy) 0 E-0349 H H H H H 4-(benzybxy) 0 E-0350 H H H H H 2-((2-fluorobenzyDoxy) 0 E-0351 H H H H H 3-((2-fluorobenzyDoxy) 0 E-0352 H H H H H 4-((2-fluorobenzyDoxy) 0 E-0353 H H H H H 2-((3-fluorobenzyDoxy) 0 E-0354 H H H H H 3-((3-fluorobenzyDoxy) 0 E-0355 H H H H H 4-((3-fluorobenzyDoxy) 0 E-0356 H H H H H 2-((4-fluorobenzyDoxy) 0 E-0357 H H H H H 3-((4-fluorobenzyDoxy) 0 E-0358 H H H H H 4-((4-fluorobenzyDoxy) 0 E-0359 H H H H H 2-((2-ch brobenzy Doxy) 0 E-0360 H H H H H 3-((2-ch brobenzy Doxy) 0 E-0361 H H H H H 4-((2-ch brobenzy Doxy) 0 E-0362 H H H H H 2-((3-ch brobenzy Doxy) 0 E-0363 H H H H H 3-((3-ch brobenzy Doxy) 0 E-0364 H H H H H 4-((3-ch brobenzy Doxy) 0 E-0365 H H H H H 2-((4-ch brobenzy Doxy) 0 E-0366 H H H H H 3-((4-ch brobenzy Doxy) 0 E-0367 H H H H H 4-((4-ch brobenzy Doxy) 0 E-0368 H H H H H 2-((2-methylbenzyDoxy) 0 E-0369 H H H H H 3-((2-methylbenzyDoxy) 0 E-0370 H H H H H 4-((2-methylbenzyDoxy) 0 E-0371 H H H H H 2-((3-methylbenzyDoxy) 0 E-0372 H H H H H 3-((3-methylbenzyDoxy) 0 E-0373 H H H H H 4-((3-methylbenzyDoxy) 0 E-0374 H H H H H 2-((4-methylbenzyDoxy) 0 E-0375 H H H H H 3-((4-methylbenzyDoxy) 0 E-0376 H H H H H 4-((4-methylbenzyDoxy) 0 E-0377 H H H H H 2-((2-(trifluorom ethyDbenzyDoxy) 0 E-0378 H H H H H 3-((2-(trifluorom ethyDbenzyDoxy) 0 E-0379 H H H H H 4-((2-(trifluorom ethyDbenzyDoxy) 0 E-0380 H H H H H 2-((3-(trifluorom ethyDbenzyDoxy) 0 E-0381 H H H H H 3-((3-(trifluorom ethyDbenzyDoxy) 0 E-0382 H H H H H 4-((3-(trifluorom ethyDbenzyDoxy) 0 E-0383 H H H H H 2-((4-(trifluorom ethyDbenzyDoxy) 0 E-0384 H H H H H 3-((4-(trifluorom ethyDbenzyDoxy) 0 E-0385 H H H H H 4-((4-(trifluorom ethyDbenzyDoxy) 0 E-0386 H H H H H 2-((2-m ethoxybenzyDoxy) 0 E-0387 H H H H H 3-((2-m ethoxybenzyloxy) 0 E-0388 H H H H H 4-((2-m ethoxybenzyDoxy) 0 E-0389 H H H H H 2-((3-m ethoxybenzyDoxy) 0 E-0390 H H H H H 3-((3-m ethoxybenzyDoxy) 0 E-0391 H H H H H 4-((3-m ethoxybenzyDoxy) 0 E-0392 H H H H H 2-((4-m ethoxybenzyDoxy) 0 E-0393 H H H H H 3-((4-m ethoxybenzyDoxy) 0 E-0394 H H H H H 4-((4-m ethoxybenzyDoxy) 0
[0387]
[Table 262]
cornpound R] R2 Rj R4 R p E-0395 H H H H H 2-((2-(trifluorom ethoxy)benzy Doxy) 0 E-0396 H H H H H 3-((2-(trifluorom ethoxy)benzy Doxy) 0 E-0397~7 H -(-trifluorom ethoxy)benzy Doxy) 0 E-0397 H H H H H 4-2--Trfoomtoyb yo)0 E-0398 H H H H H 3-((3-(trifluorom ethoxy)benzy Doxy) 0 E-0399 H H H H H -(3-(-trifluorom ethoxy)benzy Doxy) 0 E-0400 H H H H H 4-((4-(trifluorom ethoxy)benzy Doxy) 0 E-0401 H H H H H 3-((4-(trifluorom ethoxy)benzy Doxy) 0 E-0402 H H H H H 4-((4-(trifluorom ethoxy)benzy Doxy) 0 E-0403 H H H H H 4-((-(rfum e tho)benzy Doxy) 0 E-0404 H H H H H 2-((2-(m eth y th i)benzy Doxy) 0 E-0405 H H H H H 34-T(2-(m eth y thbi)benzy Doxy) 0 E-0406 H H H H H 4-((2-(m eth y th i)benzy Doxy) 0 E-0407 H H H H H 23-3 -(m eth y th i)benzy Doxy) 0 E-0408 H H H H H 3-((3-(m eth y th i)benzy Doxy) 0 E-0409 H H H H H -4-3-(m eth y th i)benzy Doxy) 0 E-04110 H H H H H 23-74- (m ethy Ithbi)benzy Doxy) 0 E-04121 H H H H H 3-((4-(m eth y th i)benzy Doxy) 0 E-04132 H H H H H -72- (methy Iufiybenzy Doxy) 0 E-04143 H H H H H 23- 2- (inethy Isu finyDbenzy Doxy) 0 E-04154 H H H H H 34-(2- (inethy Isu finyDbenzy Doxy) 0 E-04165 H H H H H 4 -((2- (ine th yIs u finy Db e nzyDoxy) 0 E -04 16 H H H H H 23-(M- (ine th yIs u finy Db e nzyDoxy) 0 E -04 17 H H H H H 43M- (ine th yIs u finy Db e nzyDoxy) 0 E-04198 H H H H H 4 -3-(ine th yIs u finy Db e nzyDoxy) 0 E-041 9 H H H H H 23-((4- (ine th yIs u finyD b e nzyDoxy) 0 E -0 42 0 H H H H H 3 -((4- (ine th yIs u finy Db e nzyDoxy) 0 E -0 42 1 H H H H H 4 - - (ine th yIsufiny Db e nzyDoxy) 0 E -0 4232 H H H H H 23-((2- (inethy Isu fo ny Db e nzy Do xy) 0 E -0 4243 H H H H H 34-((2- (inethy Isufo n y Db e nzy Do xy) 0 E -0 42 4 H H H H H 4 -((2- (inethy Isu fo n yDb e nzy D oxy) 0 E -0 4265 H H H H H 23-T3- (inethy Isufo n y Db e nzy Do xy) 0 E -0 42 6 H H H H H 43M- (inethy Isu fo n yDb e nzy Do xy) 0 E -0 42 7 H H H H H 4 -(M- (inethy Isufo n y Db e nzy Do xy) 0 E -0 4298 H H H H H 23-((4- (inethy Isu fo n yDb e nzy Do xy) 0 E -0 4320 H H H H H 34-((4- (inethy Isu fo n yDb e nzy Doxy) 0 E -0 43 0 H H H H H -((-(ilurethyt o nyDb e nzy D oxy) 0 E-0431 H H H H H 2-(2-rifluorom ethy thio)benzyDoxy) 0 E-0432 H H H H H 4-((2-(-trifluorom ethy thio)benzyDoxy) 0 E-0433 H H H H H 4-((3-(trifluorom ethy thio)benzyDoxy) 0 E-0434 H H H H H 2-(3-rifluorom ethy thio)benzyDoxy) 0 E-0435 H H H H H 3-((3-(trifluorom ethy thio)benzyDoxy) 0 E-0436 H H H H H 24-(t7rifluorom ethythio)benzyDoxy) 0 E-0437 H H H H H 3-((4-(trifluorom ethythio)benzyDoxy) 0 E-0438 H H H H H 4-((4-(trifluorom ethythio)benzyDoxy) 0 E-0439 H H H H H -((-(trifluorom ethysuthyobenzyI~oxy) 0 E-0440 H H H H H 2-((2-trifluorom ethy Isu filyDbenzy I)oxy) 0 E-0441 H H H H H 3-((2-(trifluorom ethy Isu filyDbenzy I)oxy) 0 E-0442 H H H H H 4-((3-(trifluorom ethy Isu filyDbenzy I)oxy) 0 E-0443 H H H H H 3-((3-(trifluorom ethy Isu filyDbenzy I)oxy) 0 E-0444 H H H H H 3-((3-trifluorom ethy Isu filyDbenzy I)oxy) 0 E-0445 H H H H H 4-((4-(trifluorom ethy Isu filyDbenzy I)oxy) 0 E-0446 H H H H H 3-((4-(trifluorom ethy Isu filyDbenzy I)oxy) 0 E-0447 H H H H H 3-((4-(trifluorom ethy Isu filyDbenzy I)oxy) 0 E-0449 H H H H H 2-((2-trifluorom ethysu Ifony Dbenzy Doxy) 0 E-0450 H H H H H 3-((2-(trifluorom ethysu Ifony Dbenzy Doxy) 0 E-0451 H H H H H 4-((Z-(triluorom ethy sufony Dbenzy Doxy) 0
[0388]
[Table 263]
cornpound R] R2 Rj R4 R p E-0452 H H H H H 2-((3-(trifluorom ethysu Ifony Dbenzy Doxy) 0 E-0453 H H H H H 3-((3-(trifluorom ethysu Ifony Dbenzy Doxy) 0 E-0454 H H H H H 4-((3-rifluorom ethysu Ifony Dbenzy Doxy) 0 E-0455 H H H H H 2-((4-(trifluorom ethysu Ifony Dbenzy Doxy) 0 E-0456 H H H H H 3 -((4-(triflu orom ethy su fony Dbenzy Doxy) 0 E-0457 H H H H H 4-((4-(trifluorom ethysu Ifony Dbenzy Doxy) 0 E-0458 H H H H H 2-((2-am inobenzy Doxy) 0 E-0459 H H H H H 3-((2-am inobenzy Doxy) 0 E-0460 H H H H H 4-((2-am inobenzy Doxy) 0 E-0461 H H H H H 2 - M3-amin o be nzy Do xy) 0 E -0 4 62 H H H H H 3 - M3-am in o be nzy Do xy) 0 E -0 4 63 H H H H H 4 -(M3-am in ob e nzy Do xy) 0 E -0 4 64 H H H H H 2 -((4 -am in o be nzy Do xy) 0 E -0 4 65 H H H H H 3 -((4 -am in o be nzy Do xy) 0 E -0 4 66 H H H H H 4 -((4 -am in o be nzy Do xy) 0 E -0 4 67 H H H H H 2 -T2- (inethyam ino)benzy Doxy) 0 E-0468 H H H H H 3 -((2- (inethyam ino)benzy Doxy) 0 E-0469 H H H H H 4 -T2- (inethyam ino)benzy Doxy) 0 E-0470 H H H H H 2-((3-(mnethyam ino)benzy Doxy) 0 E-0471 H H H H H 3 -T3- (inethyam ino)benzy Doxy) 0 E-0472 H H H H H 4-((3-(mnethyam ino)benzy Doxy) 0 E-0473 H H H H H 2-((4-(mnethyam ino)benzy Doxy) 0 E-0474 H H H H H 3-((4-(mnethyam ino)benzy Doxy) 0 E-0475 H H H H H 4 -74-(inethyam ino)benzy Doxy) 0 E-0476 H H H H H 2-((2-(dhiethy lam ino)benzy I)oxy) 0 E-0477 H H H H H 3-((2-(dhiethy lam ino)benzy I)oxy) 0 E-0478 H H H H H 4-((2-(dhiethy lam ino)benzy I)oxy) 0 E-0479 H H H H H 2-((3-(dhiethy lam ino)benzy I)oxy) 0 E-0480 H H H H H 3-777-(dhiethy lam ino)benzy I)oxy) 0 E-0481 H H H H H 4-((3-(dhiethy lam ino)benzy I)oxy) 0 E-0482 H H H H H 2-(4---(dhiethy lam ino)benzyDoxy) 0 E-0483 H H H H H 3-((4-(dhiethy lam ino)benzy I)oxy) 0 E-0484 H H H H H 4-((4-(dhiethy lam ino)benzy I)oxy) 0 E-0485 H H H H H 2-((2-cyanobenzy Doxy) 0 E-0486 H H H H H 3-((2-cyanobenzy Doxy) 0 E-0487 H H H H H 4-((2-cyanobenzy Doxy) 0 E-0488 H H H H H 2-((3-cyanobenzy Doxy) 0 E-0489 H H H H H 3-((3-cyanobenzy Doxy) 0 E-0490 H H H H H 4-((3-cyanobenzy Doxy) 0 E-0491 H H H H H 2-((4-cyanobenzy Doxy) 0 E-0492 H H H H H 3-((4-cyanobenzy Doxy) 0 E-0493 H H H H H 4-((4-cyanobenzy Doxy) 0 E-0494 H H H H H 2-((2-n itrobenzy Doxy) 0 E-0495 H H H H H 3-((2-n itrobenzy Doxy) 0 E-0496 H H H H H 4-((2-n itrobenzy Doxy) 0 E-0497 H H H H H 2-((3-n itrobenzy Doxy) 0 E-0498 H H H H H 3-((3-n itrobenzy Doxy) 0 E-0499 H H H H H 4-((3-n itrobenzy Doxy) 0 E-0500 H H H H H 2-((4-n itrobenzy Doxy) 0 E-0501 H H H H H 3-((4-n itrobenzy Doxy) 0 E-0502 H H H H H 4-((4-n itrobenzy Doxy) 0 E-0503 H H H H H 2-N H2 0 E-0504 H H H H H 3-N H 2 0 E-0505 H H H H H 4-N H 2 0 E-0506 H H H H H 2-N HM e 0 E-0507 H H H H H 3-N HM e 0 E-0508 H H H H H 4-N HM e 0
[0389]
[Table 264]
com pound R' R2 R- R44 R (Rd)m P E-0509 H H H H H 2-NH Et 0 E-0510 H H H H H 3-NH Et 0 E-0511 H H H H H 4-NH Et 0 E-0512 H H H H H 2-N (M e) 2 0 E-0513 H H H H H 3-N (M e) 2 0 E-0514 H H H H H 4-N (M e) 2 0 E-0515 H H H H H 2-N(Et) 2 0 E-0516 H H H H H 3-N (EV 2 0 E-0517 H H H H H 4-N (EV 2 0 E-0518 H H H H H 2-CHO 0 E-0519 H H H H H 3-CHO 0 E-0520 H H H H H 4-CHO 0 E-0521 H H H H H 2-C (=0)0H 0 E-0522 H H H H H 3-C (=0)0H 0 E-0523 H H H H H 4-C (=0)0H 0 E-0524 H H H H H 2-(1,3-dioxolan-2-yD 0 E-0525 H H H H H 3-(1,3-dioxolan-2-yD 0 E-0526 H H H H H 4-(1,3-dioxolan-2-yD 0 E-0527 H H H H H 2-(1,3-dioxan-2-yD 0 E-0528 H H H H H 3-(1,3-dioxan-2-yD 0 E-0529 H H H H H 4-(1,3-dioxan-2-yD 0 E-0530 H H H H H 2-(1H-in idazol-2-yD 0 E-0531 H H H H H 3-(1H-in idazol-2-yD 0 E-0532 H H H H H 4-(1H-i idazol-2-yD 0 E-0533 H H H H H 2-(thiazol-2-yD 0 E-0534 H H H H H 3-(thiazol-2-yD 0 E-0535 H H H H H 4-(thiazol-2-yD 0 E-0536 H H H H H 2-(oxazol-2-yl) 0 E-0537 H H H H H 3-(oxazol-2-yl) 0 E-0538 H H H H H 4-(oxazol-2-yl) 0 E-0539 H H H H H 2-CH=N0H 0 E-0540 H H H H H 3-CH=N0H 0 E-0541 H H H H H 4-CH=N0H 0 E-0542 H H H H H 2-CH=NOMe 0 E-0543 H H H H H 3-CH=NOMe 0 E-0544 H H H H H 4-CH=NOMe 0 E-0545 H H H H H 2-(4,5-dhydro-3-isoxazolyl) 0 E-0546 H H H H H 3-(4,5-dhydro-3-isoxazolyl) 0 E-0547 H H H H H 4-(4,5-dhydro-3-isoxazolyl) 0 E-0548 H H H H H 2-CN 0 E-0549 H H H H H 3-CN 0 E-0550 H H H H H 4-CN 0 E-0551 H H H H H 2-N0 2 0 E-0552 H H H H H 3-N0 2 0 E-0553 H H H H H 4-N0 2 0 E-0554 H H H H H 2,3- 2 0 E-0555 H H H H H 2,4-F 2 0 E-0556 H H H H H 2,5-F 2 0 E-0557 H H H H H 2,6-F 2 0 E-0558 H H H H H 3,4- 2 0 E-0559 H H H H H 3,5-F 2 0 E-0560 H H H H H 2-F,3-CI 0 E-0561 H H H H H 2-F,4-CI 0 E-0562 H H H H H 2-F,5-CI 0 E-0563 H H H H H 2-F,6-CI 0 E-0564 H H H H H 3-F,2-CI 0 E-0565 H H H H H 3-F,4-CI 0
[0390]
[Table 265]
com pound R' R2 R R4 R (Rd)m P E-0566 H H H H H 3-F,5-CI 0 E-0567 H H H H H 3-F,6-CI 0 E-0568 H H H H H 4-F,2-CI 0 E-0569 H H H H H 4-F,3-CI 0 E-0570 H H H H H 2-F,3-MA e 0 E-0571 H H H H H 2-F,4-MA e 0 E-0572 H H H H H 2-F,5-MvAe 0 E-0573 H H H H H 2-F,6-MAe 0 E-0574 H H H H H 3-F,2-MA e 0 E-0575 H H H H H 3-F,4-MA e 0 E-0576 H H H H H 3-F,5-MvAe 0 E-0577 H H H H H 3-F,6-MA e 0 E-0578 H H H H H 4-F,2-M e 0 E-0579 H H H H H 4-F,3-M e 0 E-0580 H H H H H 2-F,3-CF, 0 E-0581 H H H H H 2-F,4-CF, 0 E-0582 H H H H H 2-F,5-CF, 0 E-0583 H H H H H 2-F,6- F 3 0 E-0584 H H H H H 3-F,2- F 3 0 E-0585 H H H H H 3-F,4- F 3 0 E-0586 H H H H H 3-F,5-CF3 0 E-0587 H H H H H 3-F,6-CF3 0 E-0588 H H H H H 4-F,2-CF3 0 E-0589 H H H H H 4-F,3-CF 3 0 E-0590 H H H H H 2-F,3-0Me 0 E-0591 H H H H H 2-F,4-0Me 0 E-0592 H H H H H 2-F,5-0Me 0 E-0593 H H H H H 2-F,6-0Me 0 E-0594 H H H H H 3-F,2-0Me 0 E-0595 H H H H H 3-F,4-0Me 0 E-0596 H H H H H 3-F,5-0Me 0 E-0597 H H H H H 3-F,6-0Me 0 E-0598 H H H H H 4-F,2-0Me 0 E-0599 H H H H H 4-F,3-0Me 0 E-0600 H H H H H 2,3-C 0 E-0601 H H H H H 2,4-C 0 E-0602 H H H H H 2,b-L 0 E-0603 H H H H H 2,6-C 0 E-0604 H H H H H 3,4-C 0 E-0605 H H H H H 3,5-C 0 E-0606 H H H H H 2-CI,3-Me 0 E-0607 H H H H H 2-CI,4-Me 0 E-0608 H H H H H 2-CI,5-M e 0 E-0609 H H H H H 2-CI,6-Me 0 E-0610 H H H H H 3-CI,2-Me 0 E-0611 H H H H H 3-CI,4-Me 0 E-0612 H H H H H 3-CI,5-Me 0 E-0613 H H H H H 3-CI,6-Me 0 E-0614 H H H H H 4-CI,2-Me 0 E-0615 H H H H H 4-CI,3-Me 0 E-0616 H H H H H 2-C1,3-CF 3 0 E-0617 H H H H H 2-CI,4-CF 3 0 E-0618 H H H H H 2-CI,5-CF 3 0 E-0619 H H H H H 2-C1,6-CF 3 0 E-0620 H H H H H 3-CI,2-CF 3 0 E-0621 H H H H H 3-CI,4-CF 3 0 E-0622 H H H H H 3-C,5-CF 3 0
[0391]
[Table 266]
com pound R' R2 R R4 R (Rd)m P E-0623 H H H H H 3-C1,6-CF, 0 E-0624 H H H H H 4-C1,2-CF, 0 E-0625 H H H H H 4-C1,3-F, 0 E-0626 H H H H H 2-C,3-0Me 0 E-0627 H H H H H 2-C,4-0Me 0 E-0628 H H H H H 2-C1,5-0Me 0 E-0629 H H H H H 2-C1,6-0Me 0 E-0630 H H H H H 3-C,2-0Me 0 E-0631 H H H H H 3-CI,4-0Me 0 E-0632 H H H H H 3-C1,5-0Me 0 E-0633 H H H H H 3-C1,6-0Me 0 E-0634 H H H H H 4-C,2-0Me 0 E-0635 H H H H H 4-C,3-0Me 0 E-0636 H H H H H 2,3-M e 2 0 E-0637 H H H H H 2,4-M e 2 0 E-0638 H H H H H 2,5-Me 2 0 E-0639 H H H H H 2,6-M e 2 0 E-0640 H H H H H 3,4-M e 2 0 E-0641 H H H H H 3,b-M e 2 0 E-0642 H H H H H 2-M e,3-CF 3 0 E-0643 H H H H H 2-M e,4-CF3 0 E-0644 H H H H H 2-M e,5-CF3 0 E-0645 H H H H H 2-M e,6-CF3 0 E-0646 H H H H H 3-M e,2-F 3 0 E-0647 H H H H H 3-M e,4-CF3 0 E-0648 H H H H H 3-M e,5-CF3 0 E-0649 H H H H H 3-M e,6-CF3 0 E-0650 H H H H H 4-M e,2-CF3 0 E-0651 H H H H H 4-M e,3-CF 3 0 E-0652 H H H H H 2-M e,3-0Me 0 E-0653 H H H H H 2-M e,4-0Me 0 E-0654 H H H H H 2-Me,5-0 Me 0 E-0655 H H H H H 2-M e,6-0Me 0 E-0656 H H H H H 3-M e,2-0Me 0 E-0657 H H H H H 3-M e,4-0Me 0 E-0658 H H H H H 3-Me,5-0 Me 0 E-0659 H H H H H 3-M e,6-0Me 0 E-0660 H H H H H 4-M e,2-0Me 0 E-0661 H H H H H 4-Me,3-0Me 0 E-0662 H H H H H 2,3-0Me 2 0 E-0663 H H H H H 2,4-0Me 2 0 E-0664 H H H H H 2,b-0Me 2 0 E-0665 H H H H H 2,6-0Me 2 0 E-0666 H H H H H 3,4-0Me 2 0 E-0667 H H H H H 3,5-0Me 2 0 E-0668 H H H H H 2-0Me,3-F 3 0 E-0669 H H H H H 2-0Me,4-CF 3 0 E-0670 H H H H H 2-0Me,5-CF 3 0 E-0671 H H H H H 2-0Me,6-CF 3 0 E-0672 H H H H H 3-0Me,2-F 3 0 E-0673 H H H H H 3-0Me,4-CF 3 0 E-0674 H H H H H 3-0Me,5-CF 3 0 E-0675 H H H H H 3-0Me,6-CF 3 0 E-0676 H H H H H 4-0Me,2-CF 3 0 E-0677 H H H H H 4-0Me,3- F 3 0 E-0678 H H H H H 2-CH F 2,3-F 0 E-0679 H H H H H 2-CH F 2,4-F 0
[0392]
[Table 267]
com pound R' R2 R R4 R (Rd)m P E-0680 H H H H H 2-CH F 2,5-F 0 E-0681 H H H H H 2-CH F 2,6-F 0 E-0682 H H H H H 2-CHF 2,3-M e 0 E-0683 H H H H H 2-CHF 2,4-M e 0 E-0684 H H H H H 2-CHF 2,b-M e 0 E-0685 H H H H H 2-CHF 2,6-M e 0 E-0686 H H H H H 2-cycbpropyl,3-F 0 E-0687 H H H H H 2-cycbpropyl,4-F 0 E-0688 H H H H H 2-cycbpropyl,5-F 0 E-0689 H H H H H 2-cycbpropyl,6-F 0 E-0690 H H H H H 2-cycbpropyl,3-M e 0 E-0691 H H H H H 2-cycbpropyl,4-M e 0 E-0692 H H H H H 2-cycbpropyl,5-Me 0 E-0693 H H H H H 2-cycbpropyl,6-M e 0 E-0694 H H H H H 2-ethenyl,3-F 0 E-0695 H H H H H 2-ethenyl,4-F 0 E-0696 H H H H H 2-ethenyl,5-F 0 E-0697 H H H H H 2-ethenyl,6-F 0 E-0698 H H H H H 2-ethenyl,3-Me 0 E-0699 H H H H H 2-ethenyl,4-Me 0 E-0700 H H H H H 2-ethenyl1,5-Me 0 E-0701 H H H H H 2-ethenyl,6-M e 0 E-0702 H H H H H 2-0 Et,3-F 0 E-0703 H H H H H 2-0 Et4-F 0 E-0704 H H H H H 2-0 Et,5-F 0 E-0705 H H H H H 2-0 Et,6-F 0 E-0706 H H H H H 2-0 Et,3-CI 0 E-0707 H H H H H 2-0 Et4-CI 0 E-0708 H H H H H 2-0 Et,5-CI 0 E-0709 H H H H H 2-0 Et,6-CI 0 E-0710 H H H H H 2-0 Et3-M e 0 E-0711 H H H H H 2-0 Et4-M e 0 E-0712 H H H H H 2-0 Et5-M e 0 E-0713 H H H H H 2-0 Et6-M e 0 E-0714 H H H H H 2-0 Pr,3-F 0 E-0715 H H H H H 2-0 Pr,4-F 0 E-0716 H H H H H 2-0 Pr,5-F 0 E-0717 H H H H H 2-0 Pr,6-F 0 E-0718 H H H H H 2-0 Pr,3-M e 0 E-0719 H H H H H 2-0 Pr,4-M e 0 E-0720 H H H H H 2-0 Pr,5-M e 0 E-0721 H H H H H 2-0 Pr,6-M e 0 E-0722 H H H H H 2-0 (/-Pr),3-F 0 E-0723 H H H H H 2-0 (/-Pr),4-F 0 E-0724 H H H H H 2-0 (/-Pr),5-F 0 E-0725 H H H H H 2-0 (/-Pr),6-F 0 E-0726 H H H H H 2-0 (/-Pr),3-M e 0 E-0727 H H H H H 2-0 (/-Pr),4-M e 0 E-0728 H H H H H 2-0 (-Pr),5--Me 0 E-0729 H H H H H 2-0 (/-Pr),6-M e 0 E-0730 H H H H H 2-0 CF,,3-F 0 E-0731 H H H H H 2-0 CF3,4-F 0 E-0732 H H H H H 2-0 CF3 ,5-F 0 E-0733 H H H H H 2-0 CF3 ,6-F 0 E-0734 H H H H H 2-0 CF 3 ,3-M e 0 E-0735 H H H H H 2-0 CF3 ,4-M e 0 E-0736 H H H H H 2-0 CF 3,b- e 0
[0393]
[Table 268]
com pound R' R2 R R4 R (Rd)m P E-0737 H H H H H 2-0CF 3 ,6-M e 0 E-0738 H H H H H 2-OCHF 2,3-F 0 E-0739 H H H H H 2-OCHF 2,4-F 0 E-0740 H H H H H 2-OCHF 2,b-F 0 E-0741 H H H H H 2-OCHF 2,6-F 0 E-0742 H H H H H 2-0CHF 2 ,3-M e 0 E-0743 H H H H H 2-0 CH F 2,4-M e 0 E-0744 H H H H H 2-0 CH F 2 ,5-M e 0 E-0745 H H H H H 2-0 CH F 2 ,6-M e 0 E-0746 H H H H H 2-(cycbpropybxy),3-F 0 E-0747 H H H H H 2-(cycbpropybxy),4-F 0 E-0748 H H H H H 2-(cycbpropybxy),5-F 0 E-0749 H H H H H 2-(cycbpropybxy),6-F 0 E-0750 H H H H H 2-(cycbpropybxy),3-M e 0 E-0751 H H H H H 2-(cycbpropybxy),4-M e 0 E-0752 H H H H H 2-(cycbpropybxy),5-M e 0 E-0753 H H H H H 2-(cycbpropybxy),6-Me 0 E-0754 H H H H H 2-(oxiran-2-yl),3-F 0 E-0755 H H H H H 2-(oxiran-2-yl),4-F 0 E-0756 H H H H H 2-(oxiran-2-yl),5-F 0 E-0757 H H H H H 2-(oxiran-2-y),6-F 0 E-0758 H H H H H 2-(oxiran-2-yD,3-Me 0 E-0759 H H H H H 2-(oxiran-2-yD,4-Me 0 E-0760 H H H H H 2-(oxiran-2-yD,5-M e 0 E-0761 H H H H H 2-(oxiran-2-yD,6-Me 0 E-0762 H H H H H 2-(oxiran-2-y IethyD,3-F 0 E-0763 H H H H H 2-(oxiran-2-y IethyD,4-F 0 E-0764 H H H H H 2-(oxiran-2-y IethyD,5-F 0 E-0765 H H H H H 2-(oxiran-2-y IethyD,6-F 0 E-0766 H H H H H 2-(oxiran-2-yh ethyD,3-Me 0 E-0767 H H H H H 2-(oxiran-2-yh ethyD,4-Me 0 E-0768 H H H H H 2-(oxiran-2-yh ethyD,5-M e 0 E-0769 H H H H H 2-(oxiran-2-yh ethyD,6-Me 0 E-0770 H H H H H 2-SMe,3-F 0 E-0771 H H H H H 2-SMe,4-F 0 E-0772 H H H H H 2-SMe,5-F 0 E-0773 H H H H H 2-SMe,6-F 0 E-0774 H H H H H 2-SMe,3-M e 0 E-0775 H H H H H 2-SMe,4-M e 0 E-0776 H H H H H 2-SMe,5-Me 0 E-0777 H H H H H 2-SMe,6-M e 0 E-0778 H H H H H 2-SEt,3-F 0 E-0779 H H H H H 2-SEt,4-F 0 E-0780 H H H H H 2-SEt,5-F 0 E-0781 H H H H H 2-SEt,6-F 0 E-0782 H H H H H 2-SEt,3-M e 0 E-0783 H H H H H 2-SEt,4-M e 0 E-0784 H H H H H 2-SEt,5-M e 0 E-0785 H H H H H 2-SEt,6-M e 0 E-0786 H H H H H 2-S (=0)M e,3-F 0 E-0787 H H H H H 2-S (=0)M e,4-F 0 E-0788 H H H H H 2-S (=0)M e,5-F 0 E-0789 H H H H H 2-S (=0)M e,6-F 0 E-0790 H H H H H 3-S (=0)M e,2-F 0 E-0791 H H H H H 3-S (=0)M e,4-F 0 E-0792 H H H H H 3-S (=0)M e,5-F 0 E-0793 H H H H H 3-S (=0)M e,6-F 0
[0394]
[Table 269]
com pound R R2 R R (R)m P E-0794 H H H H H 2-S(=0)Me,3-M e 0 E-0795 H H H H H 2-S(=0)Me,4-M e 0 E-0796 H H H H H 2-S(=0)Me,5-M e 0 E-0797 H H H H H 2-S(=0)Me,6-M e 0 E-0798 H H H H H 3-S(=0)Me,2-M e 0 E-0799 H H H H H 3-S(=0)Me,4-M e 0 E-0800 H H H H H 3-S(=0)Me,5-M e 0 E-0801 H H H H H 3-S(=0)Me,6-M e 0 E-0802 H H H H H 2-S (=0) 2 M e,3-F 0 E-0803 H H H H H 2-S (=0) 2M e,4-F 0 E-0804 H H H H H 2-S (=0) 2 M e,b-F 0 E-0805 H H H H H 2-S (=0) 2 M e,6-F 0 E-0806 H H H H H 2-S(=0) 2Me,3-M e 0 E-0807 H H H H H 2-S (=0) 2M e,4-M e 0 E-0808 H H H H H 2-S(=0) 2Me,5-M e 0 E-0809 H H H H H 2-S(=0) 2Me,6-M e 0 E-0810 H H H H H 2-SCF,,3-F 0 E-0811 H H H H H 2-SGa3 ,4-F 0 E-0812 H H H H H 2-SCF 3 ,b-F 0 E-0813 H H H H H 2-SCF 3 ,6-F 0 E-0814 H H H H H 2-SCF 3 ,3-M e 0 E-0815 H H H H H 2-SCF 3 ,4-M e 0 E-0816 H H H H H 2-SCF 3 ,5-M e 0 E-0817 H H H H H 2-SCF 3 ,6-M e 0 E-0818 H H H H H 2-S(=O)CF 3 ,3-F 0 E-0819 H H H H H 2-S(=0)CF 3 ,4-F 0 E-0820 H H H H H 2-S(=O)CF 3 ,5-F 0 E-0821 H H H H H 2-S(=O)0F 3 ,6-F 0 E-0822 H H H H H 2-S(=0)CF 3 ,3-M e 0 E-0823 H H H H H 2-S(=0)CF 3 ,4-M e 0 E-0824 H H H H H 2-S(=0)C F 3 ,-M e 0 E-0825 H H H H H 2-S(=0)CF 3 ,6-M e 0 E-0826 H H H H H 2-S (=0) 2CF3 ,3-F 0 E-0827 H H H H H 2-S (=0) 2CF3A,4-F 0 E-0828 H H H H H 2-S (=0) 2CF3 ,5-F 0 E-0829 H H H H H 2-S (=0) 2CF3 ,6-F 0 E-0830 H H H H H 2-S (=0) 2CF 3 ,3-M e 0 E-0831 H H H H H 2-S (=0) 2CF 3,4-M e 0 E-0832 H H H H H 2-S (=0) 2CF 3 ,b- e 0 E-0833 H H H H H 2-S (=0) 2CF 3 ,6- e 0 E-0834 H H H H H 2-(cycbpropylthio),3-F 0 E-0835 H H H H H 2-(cycbpropylthio),4-F 0 E-0836 H H H H H 2-(cycbpropylthio),5-F 0 E-0837 H H H H H 2-(cycbpropylthio),6-F 0 E-0838 H H H H H 2-(cycobpropylthio),3-Me 0 E-0839 H H H H H 2-(cycobpropylthio),4-M e 0 E-0840 H H H H H 2-(cycobpropylthio),5-M e 0 E-0841 H H H H H 2-(cycobpropylthio),6-Me 0 E-0842 H H H H H 2-C(=0)Me,3-F 0 E-0843 H H H H H 2-C(=0)Me,4-F 0 E-0844 H H H H H 2-C(=0)Me,5-F 0 E-0845 H H H H H 2-C(=0)Me,6-F 0 E-0846 H H H H H 2-C(=0)Me,3-M e 0 E-0847 H H H H H 2-C(=0)Me,4-M e 0 E-0848 H H H H H 2-C(=0)Me,5-M e 0 E-0849 H H H H H 2-C(=0)Me,6-M e 0 E-0850 H H H H H 3-C(=0)Me,2-F 0
[0395]
[Table 270]
com pound R R2 R R (R)m P E-0851 H H H H H 3-C(=0)Me,4-F 0 E-0852 H H H H H 3-C(=0)Me,5-F 0 E-0853 H H H H H 3-C(=0)Me,6-F 0 E-0854 H H H H H 3-C(=0)Me,2-M e 0 E-0855 H H H H H 3-C(=0)Me,4-M e 0 E-0856 H H H H H 3-C(=0)Me,5-M e 0 E-0857 H H H H H 3-C(=0)Me,6--M e 0 E-0858 H H H H H 2-C(=0)0Me,3-F 0 E-0859 H H H H H 2-C(=0)0Me,4-F 0 E-0860 H H H H H 2-C(=0)0Me,5-F 0 E-0861 H H H H H 2-C(=0)0Me,6-F 0 E-0862 H H H H H 2-C(=0)0Me,3 -M e 0 E-0863 H H H H H 2-C(=0)0Me,4 -M e 0 E-0864 H H H H H 2-C(=0)0Me,5-M e 0 E-0865 H H H H H 2-C(=0)0Me,6--M e 0 E-0866 H H H H H 2-C(=0)0Et3-F 0 E-0867 H H H H H 2-C(=0)0Et4-F 0 E-0868 H H H H H 2-C(=0)0Et5-F 0 E-0869 H H H H H 2-C(=0)0Et6-F 0 E-0870 H H H H H 2-C(=0)0Et,3-M e 0 E-0871 H H H H H 2-C(=0)0Et,4-Me 0 E-0872 H H H H H 2-C(=0)0Et,5-M e 0 E-0873 H H H H H 2-C(=0)0Et,6-M e 0 E-0874 H H H H H 2-C(=0)NH 2 ,3-F 0 E-0875 H H H H H 2-C (=0)NH 2 ,4-F 0 E-0876 H H H H H 2-C (=0)NH 2 ,5-F 0 E-0877 H H H H H 2-C (=0)NH 2 ,6-F 0 E-0878 H H H H H 2-C(=0)NH 2,3-M e 0 E-0879 H H H H H 2-C(=0)NH 2 ,4-M e 0 E-0880 H H H H H 2-C(=0)NH 2 ,5-M e 0 E-0881 H H H H H 2-C(=0)NH 2,6-M e 0 E-0882 H H H H H 2-C(=0)NHMe,3-F 0 E-0883 H H H H H 2-C(=0)NHMe,4-F 0 E-0884 H H H H H 2-C(=0)NHMe,5-F 0 E-0885 H H H H H 2-C(=0)NHMe,6-F 0 E-0886 H H H H H 2-C(=0)NHMe,3-M e 0 E-0887 H H H H H 2-C(=0)NHMe,4-M e 0 E-0888 H H H H H 2-C(=0)NHMe,5 -Me 0 E-0889 H H H H H 2-C(=0)NHMe,6--M e 0 E-0890 H H H H H 2-C(=0)NMe 2,3-F 0 E-0891 H H H H H 2-C(=0)NMe 2,4-F 0 E-0892 H H H H H 2-C(=0)NMe 2,b- 0 E-0893 H H H H H 2-C(=0)NMe 2,6-F 0 E-0894 H H H H H 2-C(=0)NMe 2,3-M e 0 E-0895 H H H H H 2-C(=0)NMe 2,4-M e 0 E-0896 H H H H H 2-C(=0)NMe 2,b-M e 0 E-0897 H H H H H 2-C(=0)NMe 2 ,6-M e 0 E-0898 H H H H H 2-CH 20H,3-F 0 E-0899 H H H H H 2-CH20H,4-F 0 E-0900 H H H H H 2-CH 20H,5-F 0 E-0901 H H H H H 2-CH 20H,6-F 0 E-0902 H H H H H 2-CH20H,3-M e 0 E-0903 H H H H H 2-CH20H,4--M e 0 E-0904 H H H H H 2-CH20H,b5-M e 0 E-0905 H H H H H 2-CH20H,6-M e 0 E-0906 H H H H H 2-CH 20CH 3 ,3-F 0 E-0907 H H H H H 2-CH 200H 3,44-F 0
[0396]
[Table 271]
com pound R' R R R (R°)m P E-0908 H H H H H 2-GH 20H 3,b-F 0 E-0909 H H H H H 2-GH 20H 3 ,6-F 0 E-0910 H H H H H 2-CH 2UCH 3 ,3-M e 0 E-0911 H H H H H 2-CH 2UCH 3 ,4-M e 0 E-0912 H H H H H 2-CH 2UCH 3 ,b-M e 0 E-0913 H H H H H 2-CH 2UCH 3 ,6-M e 0 E-0914 H H H H H 2-GH 20H CH 3 ,3-F 2 0 E-0915 H H H H H 2-GH 20H 2CH 3 ,4-F 0 E-0916 H H H H H 2-GH 20H 2CH 3 ,b-F 0 E-0917 H H H H H 2-GH 20H 2CH 3 ,6- 0 E-0918 H H H H H 2-GH 2UCH 2 CH 3 ,3-M e 0 E-0919 H H H H H 2-GH 2 CH 2CH 3 ,4-M e 0 E-0920 H H H H H 2-GH 2UCH 2 CH 3 ,b-M e 0 E-0921 H H H H H 2-GH 2UCH 2 CH 3 ,6-M e 0 E-0922 H H H H H 2-UC(=U)CH 3 ,3-F 0 E-0923 H H H H H 2-UC(=U)CH 3 ,4-F 0 E-0924 H H H H H 2-UC(=U)CH 3 ,b-F 0 E-0925 H H H H H 2-C(=U)GH 3,6-F 0 E-0926 H H H H H 2-00(=U)CH 3 ,3-M e 0 E-0927 H H H H H 2-0(=U)CH 3,4-M e 0 E-0928 H H H H H 2-00(=0)CH 3 ,b-Me 0 E-0929 H H H H H 2-0(=U)CH 3 ,6-M e 0 E-0930 H H H H H 2-OS(=U) 2CH 3,3-F 0 E-0931 H H H H H 2-OS(=U) 20H 3,4-F 0 E-0932 H H H H H 2-OS(=U) 2CH 3,b-F 0 E-0933 H H H H H 2-OS(=U) 20H 3,6-F 0 E-0934 H H H H H 2-OS(=U) 2CH 3 ,3-M e 0 E-0935 H H H H H 2-OS(=U) 2CH 3 ,4-M e 0 E-0936 H H H H H 2-OS(=U) 2CH 3 ,b-M e 0 E-0937 H H H H H 2-OS(=U) 2 CH 3 ,6-M e 0 E-0938 H H H H H 2-GH 2SCH 3,3-F 0 E-0939 H H H H H 2-GH 2SCH 3,4-F 0 E-0940 H H H H H 2-GH 2SCH 3,5-F 0 E-0941 H H H H H 2-GH 2SCH 3,6-F 0 E-0942 H H H H H 2-OH 2S0H 3,3-M e 0 E-0943 H H H H H 2-OH 2S0H 3,4-M e 0 E-0944 H H H H H 2-GH 2SCH 3,b-M e 0 E-0945 H H H H H 2-GH 2SCH 3,6-M e 0 E-0946 H H H H H 2-GH 2SCF 3 ,3-F 0 E-0947 H H H H H 2-GH 2SCF 3 ,4-F 0 E-0948 H H H H H 2-GH 2SCF 3 ,b-F 0 E-0949 H H H H H 2-GH 2SCF 3 ,6-F 0 E-0950 H H H H H 2-OH 2S0F 3 ,3-M e 0 E-0951 H H H H H 2-GH 2SCF 3 ,4-M e 0 E-0952 H H H H H 2-OH 2S0F 3 ,5-M e 0 E-0953 H H H H H 2-OH 2SCF 3 ,6-M e 0 E-0954 H H H H H 2-(benzy loxy),3-F 0 E-0955 H H H H H 2-(benzy loxy),4-F 0 E-0956 H H H H H 2-(benzy loxy),b-F 0 E-0957 H H H H H 2-(benzyloxy),6-F 0 E-0958 H H H H H 2-(benzy bxy),3-M e 0 E-0959 H H H H H 2-(benzy bxy),4-M e 0 E-0960 H H H H H 2-(benzy bxy),b-M e 0 E-0961 H H H H H 2-(benzy bxy),6-M e 0 E-0962 H H H H H 2-NH 2 ,3-F 0 E-0963 H H H H H 2-NH 2 ,44 0 E-0964 H H H H H 2-NH 2,b-H 0
[0397]
[Table 272]
com pound R' R2 R R4 R (Rd)m P E-0965 H H H H H 2-NH 2 ,6-F 0 E-0966 H H H H H 2-NH 2,3-MAe 0 E-0967 H H H H H 2-NH 2,4-MAe 0 E-0968 H H H H H 2-NH 2,-MAe 0 E-0969 H H H H H 2-NH 2,6-MAe 0 E-0970 H H H H H 2-NHMe,3-F 0 E-0971 H H H H H 2-NHMe,4-F 0 E-0972 H H H H H 2-NHMe,5-F 0 E-0973 H H H H H 2-NHMe,6-F 0 E-0974 H H H H H 2-NHMe,3-M e 0 E-0975 H H H H H 2-NHMe,4-M e 0 E-0976 H H H H H 2-NHMe,5-M e 0 E-0977 H H H H H 2-NHMe,6-M e 0 E-0978 H H H H H 2-NHEt,3-F 0 E-0979 H H H H H 2-NHEt4-F 0 E-0980 H H H H H 2-NHEt,5-F 0 E-0981 H H H H H 2-NHEt,6-F 0 E-0982 H H H H H 2-NHEt,3-M e 0 E-0983 H H H H H 2-NHEt,4-Me 0 E-0984 H H H H H 2-NHEt,5-M e 0 E-0985 H H H H H 2-NHEt,6-M e 0 E-0986 H H H H H 2-NMe 2 ,3-F 0 E-0987 H H H H H 2-NMe 2 ,4-F 0 E-0988 H H H H H 2-NMe 2 ,5-F 0 E-0989 H H H H H 2-NMe 2 ,6-F 0 E-0990 H H H H H 2-NMe 2 ,3-M e 0 E-0991 H H H H H 2-NMe 2 ,4-M e 0 E-0992 H H H H H 2-NMe 2 ,b-M e 0 E-0993 H H H H H 2-NMe 2 ,6-M e 0 E-0994 H H H H H 2-NEt2,3-F 0 E-0995 H H H H H 2-NEt2,4-F 0 E-0996 H H H H H 2-NEt2,5-F 0 E-0997 H H H H H 2-NEt2,6-F 0 E-0998 H H H H H 2-NEt2,3-MAe 0 E-0999 H H H H H 2-NEt2,4-Me 0 E-1000 H H H H H 2-NEt2,5-MAe 0 E-1001 H H H H H 2-NEt2,6-M e 0 E-1002 H H H H H 2-CHO,3-F 0 E-1003 H H H H H 2-CH04-F 0 E-1004 H H H H H 2-CHO,5-F 0 E-1005 H H H H H 2-CHO,6-F 0 E-1006 H H H H H 2-CHO,3-M e 0 E-1007 H H H H H 2-CHO,4-Me 0 E-1008 H H H H H 2-CHO,5-M e 0 E-1009 H H H H H 2-CHO,6-M e 0 E-1010 H H H H H 2-C(=0)0H,3-F 0 E-1011 H H H H H 2-C(=0)0H,4-F 0 E-1012 H H H H H 2-C(=0)0H,5-F 0 E-1013 H H H H H 2-C(=0)0H,6-F 0 E-1014 H H H H H 2-C(=0)0H,3-M e 0 E-1015 H H H H H 2-C(=0)0H,4-M e 0 E-1016 H H H H H 2-C(=0)0H,b5-M e 0 E-1017 H H H H H 2-C(=0)0H,6-M e 0 E-1018 H H H H H 2-(1,3-dbxolan-2-yD,3-F 0 E-1019 H H H H H 2-(1,3-dbxolan-2-yD,4-F 0 E-1020 H H H H H 2-(1,3-dbxolan-2-yD,5-F 0 E-1021 H H H H H 2-0,3-dbxolan-2-yD,6-F 0
[0398]
[Table 273]
com pound R R2 R R (R)m P E-1022 H H H H H 2-0,3-dioxolan-2-yD,3-Me 0 E-1023 H H H H H 2-0,3-dioxolan-2-yD,4-Me 0 E-1024 H H H H H 2-0,3-dioxolan-2-yD,5-M e 0 E-1025 H H H H H 2-0,3-dioxolan-2-yD,6-Me 0 E-1026 H H H H H 2-0,3-dioxan-2-yD,3-F 0 E-1027 H H H H H 2-0,3-dioxan-2-yD,4-F 0 E-1028 H H H H H 2-0,3-dioxan-2-yD,5-F 0 E-1029 H H H H H 2-0,3-dioxan-2-yD,6-F 0 E-1030 H H H H H 2-(1,3-dioxan-2-yD,3-Me 0 E-1031 H H H H H 2-(1,3-dioxan-2-yD,4-Me 0 E-1032 H H H H H 2-(1,3-dioxan-2-yD,5-Me 0 E-1033 H H H H H 2-0,3-dioxan-2-yD,6-Me 0 E-1034 H H H H H 2-(thiazol-2-yD,3-F 0 E-1035 H H H H H 2-(thiazol-2-yD,4-F 0 E-1036 H H H H H 2-(thiazol-2-yD,5-F 0 E-1037 H H H H H 2-(thiazol-2-yD,6-F 0 E-1038 H H H H H 2-(thiazol-2-yD,3-M e 0 E-1039 H H H H H 2-(thiazol-2-yD,4-M e 0 E-1040 H H H H H 2-(thiazol-2-yD,5-M e 0 E-1041 H H H H H 2-(thiazol-2-yD,6-M e 0 E-1042 H H H H H 2-(oxazol--2-yl),3-F 0 E-1043 H H H H H 2-(oxazol--2-yl),4-F 0 E-1044 H H H H H 2-(oxazol-2-yl),5-F 0 E-1045 H H H H H 2-(oxazol-2-yl),6-F 0 E-1046 H H H H H 2-(oxazol-2-yD,3-Me 0 E-1047 H H H H H 2-(oxazol-2-yD,4-Me 0 E-1048 H H H H H 2-(oxazol-2-yD,5-M e 0 E-1049 H H H H H 2-(oxazol-2-yD,6-M e 0 E-1050 H H H H H 2-CH= NOH,3-F 0 E-1051 H H H H H 2-CH= NOH,4-F 0 E-1052 H H H H H 2-CH= NOH,5-F 0 E-1053 H H H H H 2-CH= NOH,6-F 0 E-1054 H H H H H 2-CH=N0H,3-M e 0 E-1055 H H H H H 2-CH=N0H,4-M e 0 E-1056 H H H H H 2-CH=N0H, 5-M e 0 E-1057 H H H H H 2-CH=N0H,6-M e 0 E-1058 H H H H H 2-CH=N0Me,3-F 0 E-1059 H H H H H 2-CH=N0Me,4-F 0 E-1060 H H H H H 2-CH=N0Me,5-F 0 E-1061 H H H H H 2-CH=N0Me,6-F 0 E-1062 H H H H H 2-CH=N0Me,3-M e 0 E-1063 H H H H H 2-CH=N0Me,4-M e 0 E-1064 H H H H H 2-CH=N0Me,5-M e 0 E-1065 H H H H H 2-CH=N0Me,6-M e 0 E-1066 H H H H H 2-CN,3-F 0 E-1067 H H H H H 2-CN,4-F 0 E-1068 H H H H H 2-CN,5-F 0 E-1069 H H H H H 2-CN,6-F 0 E-1070 H H H H H 2-CN,3-CI 0 E-1071 H H H H H 2-CN,4-CI 0 E-1072 H H H H H 2-CN,5-CI 0 E-1073 H H H H H 2-CN,6-CI 0 E-1074 H H H H H 2-CN,3-M e 0 E-1075 H H H H H 2-CN,4-M e 0 E-1076 H H H H H 2-CN,5-Me 0 E-1077 H H H H H 2-CN,6-M e 0 E-1078 H H H H H 2-CN,3-0Me 0
[0399]
[Table 274]
cornpound R] R2 T R~4 ~ (R)m p E-1079 H H H H H 2-CNA-OM e 0 E-1 080 H H H H H 2-CN 5-OM e 0 E-1 081 H H H H H 2-CN,6-OM e 0 E-1 082 H H H H H 3-CN,2 -F 0 E-1 083 H H H H H 3-CNA4-F 0 E-1 084 H H H H H 3-CN 5b-F 0 E-1 085 H H H H H 3-CN,6 -F 0 E-1 086 H H H H H 3-ON 2 -C1 0 E-1 087 H H H H H 3-CNA4-C1 0 E-1 088 H H H H H 3-CN 5b-C1 0 E-1 089 H H H H H 3-CN,6 -C1 0 E -10 90 H H H H H 3-ON,2-Mvle 0 E -10 91 H H H H H 3-CN,4-vle 0 E-1 092 H H H H H 3-CN 5-iAle 0 E -10 93 H H H H H 3 -CN,6-iAle 0 E -10 94 H H H H H 3-ON 2-0 Me 0 E -10 95 H H H H H 3-CNA-0 Me 0 E-1 096 H H H H H 3-CN 5b-0M e 0 E-1 097 H H H H H 3-CN,6-0 Me 0 E-1 098 H H H H H 4-ON,2-F 0 E-1 099 H H H H H 4-ON 3-F 0 E-1 100 H H H H H 4-CN,2-C 1 0 E-1 101 H H H H H 4-CN,3-C 1 0 E-1 102 H H H H H 4-ON,2-M e 0 E-1 103 H H H H H 4-ON,3-Mvle 0 E-1 104 H H H H H 4- N,2 -0M e 0 E-1 105 H H H H H 4- N,3 -0M e 0 E-1 106 H H H H H 2-N 0 2,3-F 0 E-1 107 H H H H H 2A 0 2 ,440 E-1 108 H H H H H 2-N 0 2 ,b-4 0 E-1 109 H H H H H 2-N 0 2,6-F 0 E-1 110 H H H H H 2-NO0 2 ,3-A e 0 E-1 111 H H H H H 2AN0 2 A4-A e 0 E-1 112 H H H H H 2AN0 2 ,b -Mve 0 E-1 113 H H H H H 2-AN0 2,6-iAe 0 E-1 114 H H H H H 2-Mvle,3,4-F 2 0 E-11 15 H H H H H 2-M e,3,5-F 2 0 E-1 116 H H H H H 2-M e,3,6-F 2 0 E-1 117 H H H H H 2-M e,4,5-F 2 0 E-1 118 H H H H H 2-0 Me,3,4-F2 0 E-1 119 H H H H H 2 -0 Me, 3,5-42 0 E-1 120 H H H H H 2-0 Me,3,6-F2 0 E-1 121 H H H H H 2 -0 Me,4,5-42 0 E-1 122 H H H H H 2-(0H 2 ) 3 -3 0 E-1 123 H H H H H 2-(0H 2 ) 4 -3 0 E-1 124 H H H H H 2-(00CH 20H 2 )-3 0 E-1 125 H H H H H 2-(0CH 20H 20H 2)-3 0 E-1 126 H H H H H 2-(0H 20H 2 0 )-3 0 E-1 127 H H H H H 2-(0H 2 0H 20H 2 0 )-3 0 E-1 128 H H H H H 3-(0H 2) 3-4 0 E-1 129 H H H H H 3-(0H 2 4 -4 0 E-1 130 H H H H H 3-(00CH 20H 2)-4 0 E-1 131 H H H H H 3-(0CH 20H 20H 2 )-4 0 E-1 132 H H H H H 3-(0H 20H 20 )-4 0 E-1 133 H H H H H 3-(0H 2 0H 20H 2 0 )-4 0 E-1 134 H H I H H H 2-(0CH 20 )-3 0 E-1 135 H H I H H H 3-(0CH 20 )-40
[0400]
[Table 275] com pound R' R R (R)m P E-1136 H H H H H 2-(0CH 2 H2 0)-3 0 E-1137 H H H H H 3-(0CH 2CH 20)-4 0 E-1138 H H H H H 2-(00F 20)-3 0 E-1139 H H H H H 3-(0CF 20)-4 0 E-1140 H H H H H 2-M e,6-Et 0 E-1141 H H H H H 2-CH20TBS 0 E-1142 H H H H H 2-cycbpropyl,3-0Me 0 E-1143 H H H H H 2-cycbpropyl,4-0Me 0 E-1144 H H H H H 2-cycbpropyl,5-0Me 0 E-1145 H H H H H 2-cycbpropyl,6-0Me 0 E-1146 H H H H H 2-M e,3-OMe,6-M e 0 E-1147 H H H H H 2-M e,4-OMe,6-M e 0 E-1148 H H H H H 2-OMe,3-M e,6-M e 0 E-1149 H H H H H 2-OMe,5-M e,6-M e 0 E-1150 H H H H H 2-OMe,3-F,6-M e 0 E-1151 H H H H H 2-OMe,5-F,6-M e 0 E-1152 H H H H H 2-OMe,5-M e,6-F 0 E-1153 H H H H H 2-CI,3-M e,6-F 0 E-1154 H H H H H 2-C1,5-M e,6-F 0 E-1155 H H H H H 2-C ,3-OM e,6-F 0 E-1156 H H H H H 2-C I,5-OM e,6-F 0 E-1157 H H H H H 2-M e,5-Et 0 E-1158 H H H H H 2,6-Et2 0 E-1159 H H H H H 2-Et,6-F 0 E-1160 H H H H H 2-CH 2 00H 3,6-CI 0 E-1161 H H H H H 2-CH 2 00H 20H 3,6-CI 0 E-1162 H H H H H 2-0M e,5-CH= NOM e 0 E-1163 H H H H H 2-CH 2NMe 2 0 E-1164 H H H H H 2-CH 20CH 3 ,6-CF 3 0 E-1165 H H F H H 2-M e 0
[0401]
[Table 276]
3 2 R R 0
~ NNOH
1 (O)p R R'
cornpound R1 ~ R2 Rj R4 R (R%) p E-5001 H H H H H H 1 E-5002 H H H H H 2-F 1 E-5003 H H H H H 3-F 1 E-5004 H H H H H 4-F 1 E-5005 H H H H H 2-Cl1 E-5006 H H H H H 3-Cl1 1 E-5007 H H H H H 4-Cl1 1 E-5008 H H H H H 2-B r 1 E-5009 H H H H H 3-B r 1 E-501 0 H H H H H 4-B r 1 E-501 1 H H H H H 2-1 1 E-501 2 H H H H H 3-1 1 E-501 3 H H H H H 4-1 1 E-501 4 H H H H H 2-0OH 1 E-501 5 H H H H H 3-O H 1 E-50 16 H H H H H 4-0OH 1 E-501 7 H H H H H 2-SH 1 E-501 8 H H H H H 3-SH 1 E-501 9 H H H H H 4-SH 1 E-5020 H H H H H 2-M e 1 E-5021 H H H H H 3-M e 1 E-5022 H H H H H 4-M e 1 E-5023 H H H H H 2-Et 1 E-5024 H H H H H 3-Et 1 E-5025 H H H H H 4-Et 1 E-5026 H H H H H 2-Pr 1 E-5027 H H H H H 3-Pr 1 E-5028 H H H H H 4-Pr 1 E-5029 H H H H H 2-i-Pr 1 E-5030 H H H H H 3-i-Pr 1 E-5031 H H H H H 4-i-Pr 1 E-5032 H H H H H 2-Bu 1 E-5033 H H H H H 3-Eu 1 E-5034 H H H H H 4-B u 1 E-5035 H H H H H 2-s-B u 1 E-503 6 H H H H H 3-s-E u 1 E-503 7 H H H H H 4-s-E u 1 E-5038 H H H H H 2-/-B u 1 E-503 9 H H H H H 3-i-B u 1 E-5040 H H H H H 4-/-B u 1 E-5041 H H H H H 2-t-B u 1 E-5042 H H H H H 3-t-B u 1 E-5043 H H H H H 4-t-B u 1 E-5044 H H H H H 2-C F, 1 E-5045 H H H H H 3-CUF, 1 E-5046 H H H H H 4--C F, 1 E-5047 H H H H H 2 -UCHF 2 1 E-5048 H H H H H 3 -CHF 2 1 E-5049 H H H H H 4 -UHF2 1 E-5050 H H H H H 2--C H2F 1 E-5051 H H H H H 3-C H2F 1 E-5052 H H H H H 4-CH 2 F
[0402]
[Table 277]
com pound R' R2 R R4 R (Rd)m P E-5053 H H H H H 2-CF 2C 1 1 E-5054 H H H H H 3-CF 2C 1 1 E-5055 H H H H H 4-CF 201 1 E-5056 H H H H H 2-CF(F 3 ) 2 1 E-5057 H H H H H 3-CF(F 3 ) 2 1 E-5058 H H H H H 4-C -(0 3 ) 2 1 E-5059 H H H H H 2-cycobpropyl 1 E-5060 H H H H H 3-cycobpropyl 1 E-5061 H H H H H 4-cycobpropyl 1 E-5062 H H H H H 2-cyclobutyl 1 E-5063 H H H H H 3-cyclobutyl 1 E-5064 H H H H H 4-cyclobutyl 1 E-5065 H H H H H 2-cycbpentyl 1 E-5066 H H H H H 3-cycbpentyl 1 E-5067 H H H H H 4-cycbpentyl 1 E-5068 H H H H H 2-(cyclopropyhiethyD 1 E-5069 H H H H H 3-(cyclopropyhiethyD 1 E-5070 H H H H H 4-(cyclopropyhiethyD 1 E-5071 H H H H H 2-(cycobbutyhiethyD 1 E-5072 H H H H H 3-(cycobbutyhi ethyD 1 E-5073 H H H H H 4-(cycobbutyhi ethyD 1 E-5074 H H H H H 2-(cycbpentyhi ethyD 1 E-5075 H H H H H 3-(cycbpentyhi ethyD 1 E-5076 H H H H H 4-(cycbpentyhi ethyD 1 E-5077 H H H H H 2-(cyclopropylethyD 1 E-5078 H H H H H 3-(cyclopropylethyD 1 E-5079 H H H H H 4-(cyclopropylethyD 1 E-5080 H H H H H 2-(2,2-difluorocycbpropyD 1 E-5081 H H H H H 3-(2,2-difluorocycbpropyD 1 E-5082 H H H H H 4-(2,2-difluorocycbpropyD 1 E-5083 H H H H H 2-(2,2-dichbrocycbpropyD 1 E-5084 H H H H H 3-(2,2-dichbrocycbpropyD 1 E-5085 H H H H H 4-(2,2-dichbrocycbpropyD 1 E-5086 H H H H H 2-ethenyl 1 E-5087 H H H H H 3-ethenyl 1 E-5088 H H H H H 4-ethenyl 1 E-5089 H H H H H 2-allyl 1 E-5090 H H H H H 3-allyl 1 E-5091 H H H H H 4-allyl 1 E-5092 H H H H H 2-(prop-1-en-1-yD 1 E-5093 H H H H H 3-(prop-1-en-1-yD 1 E-5094 H H H H H 4-(prop-1-en-1-yD 1 E-5095 H H H H H 2-(trifluoroethenyD 1 E-5096 H H H H H 3-(trifluoroethenyD 1 E-5097 H H H H H 4-(trifluoroethenyD 1 E-5098 H H H H H 2-(2,2-dichbroethenyD 1 E-5099 H H H H H 3-(2,2-dichbroethenyD 1 E-5100 H H H H H 4-(2,2-dichbroethenyD 1 E-5101 H H H H H 2-ethynyl 1 E-5102 H H H H H 3-ethynyl 1 E-5103 H H H H H 4-ethynyl 1 E-5104 H H H H H 2-(1-propyn-1-yD 1 E-5105 H H H H H 3-(1-propyn-1-yD 1 E-5106 H H H H H 4-(1-propyn-1-yD 1 E-5107 H H H H H 2-(2-propyn-1-yD 1 E-5108 H H H H H 3-(2-propyn-1-yD 1 E-5109 H H H H H 4-(2-propyn-1-yl 1
[0403]
[Table 278]
com pound R R2 R R (R)m P E-5110 H H H H H 2-(2-cycobpropylethynyD 1 E-5111 H H H H H 3-(2-cycobpropylethynyD 1 E-5112 H H H H H 4-(2-cycobpropylethynyD 1 E-5113 H H H H H 2-(2-chbroethynyD 1 E-5114 H H H H H 3-(2-chbroethynyD 1 E-5115 H H H H H 4-(2-chbroethynyD 1 E-5116 H H H H H 2-(2-brom oethynyl) 1 E-5117 H H H H H 3-(2-brom oethynyl) 1 E-5118 H H H H H 4-(2-brom oethynyl) 1 E-5119 H H H H H 2-0M e 1 E-5120 H H H H H 3-0M e 1 E-5121 H H H H H 4-0M e 1 E-5122 H H H H H 2-0Et 1 E-5123 H H H H H 3-0Et 1 E-5124 H H H H H 4-0Et 1 E-5125 H H H H H 2-0Pr 1 E-5126 H H H H H 3-0Pr 1 E-5127 H H H H H 4-0Pr 1 E-5128 H H H H H 2-0 (/-Pr) 1 E-5129 H H H H H 3-0 (/-Pr) 1 E-5130 H H H H H 4-0 (/-Pr) 1 E-5131 H H H H H 2-0Bu 1 E-5132 H H H H H 3-0Bu 1 E-5133 H H H H H 4-0Bu 1 E-5134 H H H H H 2-0 (s-Bu) 1 E-5135 H H H H H 3-0 (s-Bu) 1 E-5136 H H H H H 4-0 (s-Bu) 1 E-5137 H H H H H 2-0 (/-Bu) 1 E-5138 H H H H H 3-0 (/-Bu) 1 E-5139 H H H H H 4-0 (/-Bu) 1 E-5140 H H H H H 2-0 (t-Bu) 1 E-5141 H H H H H 3-0 (t-Bu) 1 E-5142 H H H H H 4-0 (t-Bu) 1 E-5143 H H H H H 2-0CF 1 E-5144 H H H H H 3-0CF 1 E-5145 H H H H H 4-0CF 1 E-5146 H H H H H 2-0CHF 2 1 E-5147 H H H H H 3-0CHF 2 1 E-5148 H H H H H 4-0CHF 2 1 E-5149 H H H H H 2-0CH 20F 3 1 E-5150 H H H H H 3-0CH 2 CF3 1 E-5151 H H H H H 4-0CH 20F 3 1 E-5152 H H H H H 2-(cycbpropy bxy) 1 E-5153 H H H H H 3-(cycbpropy bxy) 1 E-5154 H H H H H 4-(cycbpropy bxy) 1 E-5155 H H H H H 2-(cyclobutybxy) 1 E-5156 H H H H H 3-(cyclobutybxy) 1 E-5157 H H H H H 4-(cyclobutybxy) 1 E-5158 H H H H H 2-(cyclopentybxy) 1 E-5159 H H H H H 3-(cyclopentybxy) 1 E-5160 H H H H H 4-(cyclopentybxy) 1 E-5161 H H H H H 2-((2,2-dichbrocycbpropyDoxy) 1 E-5162 H H H H H 3-((2,2-dichbrocycbpropyDoxy) 1 E-5163 H H H H H 4-((2,2-dichbrocycbpropyDoxy) 1 E-5164 H H H H H 2-(cycbpropyhiethoxy) 1 E-5165 H H H H H 3-(cycbpropyhiethoxy) 1 E-5166 H H H H H 4-(cycbpropyhiethoxy) 1
[0404]
[Table 279]
com pound R' R2 R- R44 R (Rd)m P E-5167 H H H H H 2-((2,2-difluorocycbpropyDm ethoxy) 1 E-5168 H H H H H 3-((2,2-difluorocycbpropyDm ethoxy) 1 E-5169 H H H H H 4-((2,2-difluorocycbpropyDm ethoxy) 1 E-5170 H H H H H 2-(oxiran-2-y) 1 E-5171 H H H H H 3-(oxiran-2-yl) 1 E-5172 H H H H H 4-(oxiran-2-y) 1 E-5173 H H H H H 2-(oxiran-2-yh ethyl) 1 E-5174 H H H H H 3-(oxiran-2-yh ethyl) 1 E-5175 H H H H H 4-(oxiran-2-yh ethyl) 1 E-5176 H H H H H 2-SMe 1 E-5177 H H H H H 3-SMe 1 E-5178 H H H H H 4-SMe 1 E-5179 H H H H H 2-SEt 1 E-5180 H H H H H 3-SEt 1 E-5181 H H H H H 4-SEt 1 E-5182 H H H H H 2-S(=0)Me 1 E-5183 H H H H H 3-S(=0)Me 1 E-5184 H H H H H 4-S(=0)Me 1 E-5185 H H H H H 2-S (=0) 2M e 1 E-5186 H H H H H 3-S (=0) 2M e 1 E-5187 H H H H H 4-S (=0) 2M e 1 E-5188 H H H H H 2-SCF, 1 E-5189 H H H H H 3-SCF, 1 E-5190 H H H H H 4-SCF, 1 E-5191 H H H H H 2-S (=0)CF3 1 E-5192 H H H H H 3-S (=0)CF3 1 E-5193 H H H H H 4-S (=0)CF3 1 E-5194 H H H H H 2-S (=0) 20F 3 1 E-5195 H H H H H 3-S (=0) 2CF 3 1 E-5196 H H H H H 4-S (=0) 2CF3 1 E-5197 H H H H H 2-SCF ( F 3 ) 2 1 E-5198 H H H H H 3-SCF (CF 3) 2 1 E-5199 H H H H H 4-SCF (CF3) 2 1 E-5200 H H H H H 2-(cycbpropylthio) 1 E-5201 H H H H H 3-(cycbpropylthio) 1 E-5202 H H H H H 4-(cycbpropylthio) 1 E-5203 H H H H H 2-(cycbpropysulfinyD 1 E-5204 H H H H H 3-(cycbpropysulfinyD 1 E-5205 H H H H H 4-(cycbpropysulfinyl) 1 E-5206 H H H H H 2-(cycbpropyIsulfonyD 1 E-5207 H H H H H 3-(cycbpropyIsulfonyl) 1 E-5208 H H H H H 4-(cycbpropyIsulfonyD 1 E-5209 H H H H H 2-((cycbpropyI ethyI)thio) 1 E-5210 H H H H H 3-((cycbpropyI ethyl)thio) 1 E-5211 H H H H H 4-((cycbpropyI ethyl)thio) 1 E-5212 H H H H H 2-((cycbpropy ethylsulfinyD 1 E-5213 H H H H H 3-((cycbpropy ethylsulfinyD 1 E-5214 H H H H H 4-((cycobpropy Iethyl)sulfinyD 1 E-5215 H H H H H 2-((cycbpropy ethyDsulfonyD 1 E-5216 H H H H H 3-((cycbpropy ethyDsulfonyD 1 E-5217 H H H H H 4-((cycbpropy IethylsulfonyD 1 E-5218 H H H H H 2-(((2,2-difluorocycbpropyl)m ethyl)thio) 1 E-5219 H H H H H 3-(((2,2-difluorocycbpropyDm ethyDthio) 1 E-5220 H H H H H 4-(((2,2-difluorocycbpropyl)m ethyl)thio) 1 E-5221 H H H H H 2-(((2,2-diflorocycbpropylDm ethylsulfinyD 1 E-5222 H H H H H 3-(((2,2-diflorocycbpropyl)m ethyl)sulfinyl) 1 E-5223 H H H H H 4-(((2,2-dfLiorocycbpropyDm ethylsulfinyD 1
[0405]
[Table 280]
com pound R' R2 R- R44 R (Rd)m P E-5224 H H H H H 2-(((2,2-d fluorocycobpropy )m ethyl)suiony D 1 E-5225 H H H H H 3-(((2,2-d fluorocycobpropy )m ethyl)su fony D 1 E-5226 H H H H H 4-(((2,2-d fluorocycobpropyl)m ethyl)su fonyD 1 E-5227 H H H H H 2-C (=0)M e 1 E-5228 H H H H H 3-C (=0)M e 1 E-5229 H H H H H 4-C (=0)M e 1 E-5230 H H H H H 2-C(=0)Et 1 E-5231 H H H H H 3-C(=0)Et 1 E-5232 H H H H H 4-C(=0)Et 1 E-5233 H H H H H 2-0 (= 0)0% 1 E-5234 H H H H H 3-0 (=0)F3 1 E-5235 H H H H H 4-C (=0)CF3 1 E-5236 H H H H H 2-C (= 0)0Me 1 E-5237 H H H H H 3-C (= 0)0Me 1 E-5238 H H H H H 4-C (= 0)0Me 1 E-5239 H H H H H 2-C (=0)0Et 1 E-5240 H H H H H 3-C (=0)0Et 1 E-5241 H H H H H 4-C 0(= 0)0Et 1 E-5242 H H H H H 2-0 (=0)NH 2 1 E-5243 H H H H H 3-0 (=0)NH 2 1 E-5244 H H H H H 4-C (=0)NH 2 1 E-5245 H H H H H 2-C 0(= 0)NHM e 1 E-5246 H H H H H 3-C 0(= 0)NHM e 1 E-5247 H H H H H 4-C 0(= 0)NHM e 1 E-5248 H H H H H 2-C (=0)N M e 2 1 E-5249 H H H H H 3-C 0(= 0)NM e 2 1 E-5250 H H H H H 4-C (=0)NM e 2 1 E-5251 H H H H H 2-CH20 (=00 31 E-5252 H H H H H 3-CH20 (=00 31 E-5253 H H H H H 4-CH 2 C 0(= 0)CH 3 1 E-5254 H H H H H 2-CH 2 0 (=0)0 1 E-5255 H H H H H 3-CH 2C (=0)CF 1 E-5256 H H H H H 4-CH 2C (=0)CF 1 E-5257 H H H H H 2-CH 2C(=0)0CH 3 1 E-5258 H H H H H 3-CH 2C 0(= 0)0CH 3 1 E-5259 H H H H H 4-CH 2C(=0)0CH3 1 E-5260 H H H H H 2-CH 2 0H 1 E-5261 H H H H H 3-CH 2 0H 1 E-5262 H H H H H 4-CH 2 0H 1 E-5263 H H H H H 2-CH 200H 3 1 E-5264 H H H H H 3-CH 20CH 3 1 E-5265 H H H H H 4-CH 200H 3 1 E-5266 H H H H H 2-CH 2 0CH 2CH 3 1 E-5267 H H H H H 3-CH 2 00H 20H 3 1 E-5268 H H H H H 4-CH 2 0CH 2CH 3 1 E-5269 H H H H H 2-CH (CH 3)0CH 3 1 E-5270 H H H H H 3-CH (CH 3)0CH 3 1 E-5271 H H H H H 4-CH (CH 3)0CH 3 1 E-5272 H H H H H 2-CH 2 CH 20CH 3 1 E-5273 H H H H H 3-CH 2 CH2 00CH 3 1 E-5274 H H H H H 4-CH 2 CH 20CH 3 1 E-5275 H H H H H 2-CH 20 CF3 1 E-5276 H H H H H 3-CH 20 CF3 1 E-5277 H H H H H 4-CH 20 CF3 1 E-5278 H H H H H 2-CF 200H 3 1 E-5279 H H H H H 3-CF 20CH 3 1 E-5280 H H H H H 4-GF 200H 3
[0406]
[Table 281]
com pound R' R R R (R°)m P E-5281 H H H H H 2-0FGF 2 2 0F 1 E-5282 H H H H H 3-0FGF 2 2 0F 1 E-5283 H H H H H 4-GF 2 F 2 0F 1 E-5284 H H H H H 2-0C(=0)GH 3 1 E-5285 H H H H H 3-0C(=0)GH 3 1 E-5286 H H H H H 4-0(=U)GH 3 1 E-5287 H H H H H 2-U0(=U)GF 3 1 E-5288 H H H H H 3-U0(=U)0F 3 1 E-5289 H H H H H 4-U0(=U)CF 3 1 E-5290 H H H H H 2-00(=0)NH2 1 E-5291 H H H H H 3-0C(=0)NH 2 1 E-5292 H H H H H 4-U0(=U)NH 2 1 E-5293 H H H H H 2-0C(=0)NHCH 3 1 E-5294 H H H H H 3-0C(=0)NHCH 3 1 E-5295 H H H H H 4-U0(=U)NHOH 3 1 E-5296 H H H H H 2-0(=U)N (H 3) 2 1 E-5297 H H H H H 3-0(=U)N (H 3) 2 1 E-5298 H H H H H 4-0C(=0)N (H 3) 2 1 E-5299 H H H H H 2-GH 2 00(=0)NH 2 1 E-5300 H H H H H 3-GH 2 00(=0)NH 2 1 E-5301 H H H H H 4-CH 200(=)NH 2 1 E-5302 H H H H H 2-CH 20(=U)NHOH 3 1 E-5303 H H H H H 3-GH 20(=O)NHCH 3 1 E-5304 H H H H H 4-GH 200(=0)NHCH 3 1 E-5305 H H H H H 2-CH 20(=O)N (H 3) 2 1 E-5306 H H H H H 3-CH 20(=O)N (H 3) 2 1 E-5307 H H H H H 4-CH 20(=O)N (H 3) 2 1 E-5308 H H H H H 2-0C(=0)0H 3 1 E-5309 H H H H H 3-0C(=0)0H 3 1 E-5310 H H H H H 4-UC(=U)UGH 3 1 E-5311 H H H H H 2-GH 2 0(=0)0H 3 1 E-5312 H H H H H 3-CH 20(=O)OH 3 1 E-5313 H H H H H 4-CH 20G(=O)OGH 3 1 E-5314 H H H H H 2-CH 20(=U)CH 3 1 E-5315 H H H H H 3-CH 20(=U)GH 3 1 E-5316 H H H H H 4-CH 20(=U)GH 3 1 E-5317 H H H H H 2-U S=0) 2CH 3 1 E-5318 H H H H H 3-U S=0) 20H 3 E-5319 H H H H H 4-U S=0) 20H 3 1 E-5320 H H H H H 2-CH 2SCH 3 1 E-5321 H H H H H 3-CH 2SOH 3 1 E-5322 H H H H H 4-CH 2SCH 3 1 E-5323 H H H H H 2-CH 2S(=U)CH 3 1 E-5324 H H H H H 3-CH 2 S(=0)GH 3 1 E-5325 H H H H H 4-CH 2 S(=U)CH 3 1 E-5326 H H H H H 2-CH 2S=0) 20H 3 1 E-5327 H H H H H 3-CH 2S(=U) 2 H 3 1 E-5328 H H H H H 4-CH 2S(=U) 2 H 3 1 E-5329 H H H H H 2-CH 2SGF 3 1 E-5330 H H H H H 3-GH 2SCF 3 1 E-5331 H H H H H 4-CH 2SGF 3 1 E-5332 H H H H H 2-CH 2 S(=U)GF 3 1 E-5333 H H H H H 3-CH 2 S(=U)GF 3 1 E-5334 H H H H H 4-CH 2 S(=0)OF 3 1 E-5335 H H H H H 2-CH 2 S=0) 2CF 3 1 E-5336 H H H H H 3-CH 2 S(=U) 2GF 3 1 E-5337 H H H H H 4-CH 2 S=0) 0F 3
[0407]
[Table 282]
com pound R' R2 R R4 R (Rd)m P E-5338 H H H H H 2-phenyl 1 E-5339 H H H H H 3-phenyl 1 E-5340 H H H H H 4-phenyl 1 E-5341 H H H H H 2-(pheny bxy) 1 E-5342 H H H H H 3-(pheny bxy) 1 E-5343 H H H H H 4-(pheny bxy) 1 E-5344 H H H H H 2-benzyl 1 E-5345 H H H H H 3-benzyl 1 E-5346 H H H H H 4-benzyl 1 E-5347 H H H H H 2-(benzybxy) 1 E-5348 H H H H H 3-(benzybxy) 1 E-5349 H H H H H 4-(benzybxy) 1 E-5350 H H H H H 2-((2-fluorobenzyDoxy) 1 E-5351 H H H H H 3-((2-fluorobenzyDoxy) 1 E-5352 H H H H H 4-((2-fluorobenzyDoxy) 1 E-5353 H H H H H 2-((3-fluorobenzyDoxy) 1 E-5354 H H H H H 3-((3-fluorobenzyDoxy) 1 E-5355 H H H H H 4-((3-fluorobenzyDoxy) 1 E-5356 H H H H H 2-((4-fluorobenzyDoxy) 1 E-5357 H H H H H 3-((4-fluorobenzyDoxy) 1 E-5358 H H H H H 4-((4-fluorobenzyDoxy) 1 E-5359 H H H H H 2-((2-ch brobenzy Doxy) 1 E-5360 H H H H H 3-((2-ch brobenzy Doxy) 1 E-5361 H H H H H 4-((2-ch brobenzy Doxy) 1 E-5362 H H H H H 2-((3-ch brobenzy Doxy) 1 E-5363 H H H H H 3-((3-ch brobenzy Doxy) 1 E-5364 H H H H H 4-((3-ch brobenzy Doxy) 1 E-5365 H H H H H 2-((4-ch brobenzy Doxy) 1 E-5366 H H H H H 3-((4-ch brobenzy Doxy) 1 E-5367 H H H H H 4-((4-ch brobenzy Doxy) 1 E-5368 H H H H H 2-((2-methylbenzyDoxy) 1 E-5369 H H H H H 3-((2-methylbenzyDoxy) 1 E-5370 H H H H H 4-((2-methylbenzyDoxy) 1 E-5371 H H H H H 2-((3-methylbenzyDoxy) 1 E-5372 H H H H H 3-((3-methylbenzyDoxy) 1 E-5373 H H H H H 4-((3-methylbenzyDoxy) 1 E-5374 H H H H H 2-((4-methylbenzyDoxy) 1 E-5375 H H H H H 3-((4-methylbenzyDoxy) 1 E-5376 H H H H H 4-((4-methylbenzyDoxy) 1 E-5377 H H H H H 2-((2-(trifluorom ethyDbenzyDoxy) 1 E-5378 H H H H H 3-((2-(trifluorom ethyDbenzyDoxy) 1 E-5379 H H H H H 4-((2-(trifluorom ethyDbenzyDoxy) 1 E-5380 H H H H H 2-((3-(trifluorom ethyDbenzyDoxy) 1 E-5381 H H H H H 3-((3-(trifluorom ethyDbenzyDoxy) 1 E-5382 H H H H H 4-((3-(trifluorom ethyDbenzyDoxy) 1 E-5383 H H H H H 2-((4-(trifluorom ethyDbenzyDoxy) 1 E-5384 H H H H H 3-((4-(trifluorom ethyDbenzyDoxy) 1 E-5385 H H H H H 4-((4-(trifluorom ethyDbenzyDoxy) 1 E-5386 H H H H H 2-((2-m ethoxybenzyDoxy) 1 E-5387 H H H H H 3-((2-m ethoxybenzyloxy) 1 E-5388 H H H H H 4-((2-m ethoxybenzyDoxy) 1 E-5389 H H H H H 2-((3-m ethoxybenzyDoxy) 1 E-5390 H H H H H 3-((3-m ethoxybenzyDoxy) 1 E-5391 H H H H H 4-((3-m ethoxybenzyDoxy) 1 E-5392 H H H H H 2-((4-m ethoxybenzyDoxy) 1 E-5393 H H H H H 3-((4-m ethoxybenzyDoxy) 1 E-5394 H H H H H 4-((4-m ethoxybenzyDoxy) 1
[0408]
[Table 283]
cornpound R] R2 Rj R4 R p E-5395 H H H H H 2-((2-(trifluorom ethoxy)benzy Doxy) 1 E-5396 H H H H H 3-((2-(trifluorom ethoxy)benzy Doxy) 1 E-5397~7 H -(-trifluorom ethoxy)benzy Doxy) 1 E-5397 H H H H H 4-2--Trfoomtoyb yo)1 E-5398 H H H H H 3-((3-(trifluorom ethoxy)benzy Doxy) 1 E-5399 H H H H H -(3-(-trifluorom ethoxy)benzy Doxy) 1 E-5400 H H H H H 4-((4-(trifluorom ethoxy)benzy Doxy) 1 E-5401 H H H H H 3-((4-(trifluorom ethoxy)benzy Doxy) 1 E-5402 H H H H H 4-((4-(trifluorom ethoxy)benzy Doxy) 1 E-5403 H H H H H 4-((-tilum e tho)benzy Doxy) 1 E-5404 H H H H H 2-((2-(m eth y th i)benzy Doxy) 1 E-5405 H H H H H 34-T(2-(m eth y thbi)benzy Doxy) 1 E-5406 H H H H H 4-((2-(m eth y th i)benzy Doxy) 1 E-5407 H H H H H 23-3 -(m eth y th i)benzy Doxy) 1 E-5408 H H H H H 3-((3-(m eth y th i)benzy Doxy) 1 E-5409 H H H H H -4-3-(m eth y th i)benzy Doxy) 1 E-54110 H H H H H 23-74- (m ethy Ithbi)benzy Doxy) 1 E-54121 H H H H H 3-((4-(m ethy Ith i)benzy Doxy) 1 E-54132 H H H H H -72- (methy Iufiybenzy Doxy) 1 E-54143 H H H H H 23- 2- (inethy Isu finyDbenzy Doxy) 1 E-54154 H H H H H 34-( 2- (inethy Isu finyDbenzy Doxy) 1 E-54165 H H H H H 4 -((2- (ine th yIs u finy Db e nzyDoxy) 1 E -54 16 H H H H H 23 - (in e th yIs u finy Db e nzyDoxy) 1 E -54 17 H H H H H 34- (in e th yIs u finy Db e nzyDoxy) 1 E-54198 H H H H H 4 -3-(ine th yIs u finy Db e nzyDoxy) 1 E-541 9 H H H H H 23-((4- (ine th yIs u finyD b e nzyDoxy) 1 E -5 4210 H H H H H 3 -((4- (ine th yIs u finy Db e nzyDoxy) 1 E -5 42 1 H H H H H 4 27- (in e th yIs ufiny Db e nzyDoxy) 1 E -5 4232 H H H H H 2 - ((2-(inethy Isu fo ny Db e nzy Do xy) 1 E -5 4243 H H H H H 34-((2- (inethy Isufo n y Db e nzy Do xy) 1 E -5 42 4 H H H H H 4 -((2- (inethy Isu fo n yDb e nzy D oxy) 1 E -5 4265 H H H H H 23-T3- (inethy Isufo n y Db e nzy Do xy) 1 E -5 42 6 H H H H H 43M- (inethy Isu fo n yDb e nzy Do xy) 1 E -5 42 7 H H H H H 4 -(M- (inethy Isufo n y Db e nzy Do xy) 1 E -5 4298 H H H H H 23-((4- (inethy Isu fo n yDb e nzy Do xy) 1 E -5 4320 H H H H H 34-((4- (inethy Isu fo n yDb e nzy Doxy) 1 E -5 4310 H H H H H -((-(trfnurethy t o nyDb e nzy D oxy) 1 E-5431 H H H H H 2- 2-trifluorom ethy thio)benzyDoxy) 1 E-5432 H H H H H 4-((2-(-trifluorom ethy thio)benzyDoxy) 1 E-5433 H H H H H 4-((3-(trifluorom ethy thio)benzyDoxy) 1 E-5434 H H H H H 2-(3-rifluorom ethy thio)benzyDoxy) 1 E-5435 H H H H H 3-((3-(trifluorom ethy thio)benzyDoxy) 1 E-5436 H H H H H 24-(t7rifluorom ethythio)benzyDoxy) 1 E-5437 H H H H H 3-((4-(trifluorom ethythio)benzyDoxy) 1 E-5438 H H H H H 4-((4-(trifluorom ethythio)benzyDoxy) 1 E-5439 H H H H H -((-(trifluorom ethysuthyobenzyI~oxy) 1 E-5440 H H H H H 2-((2-trifluorom ethy Isu filyDbenzy I)oxy) 1 E-5441 H H H H H 3-((2-(trifluorom ethy Isu filyDbenzy I)oxy) 1 E-5442 H H H H H 4-((3-(trifluorom ethy Isu filyDbenzy I)oxy) 1 E-5443 H H H H H 3-((3-(trifluorom ethy Isu filyDbenzy I)oxy) 1 E-5444 H H H H H 3-((3-trifluorom ethy Isu filyDbenzy I)oxy) 1 E-5445 H H H H H 4-((4-(trifluorom ethy Isu filyDbenzy I)oxy) 1 E-5446 H H H H H 3-((4-(trifluorom ethy Isu filyDbenzy I)oxy) 1 E-5447 H H H H H 3-((4-(trifluorom ethy Isu filyDbenzy I)oxy) 1 E-5449 H H H H H 2-((2-trifluorom ethysu Ifony Dbenzy Doxy) 1 E-5450 H H H H H 3-((2-(trifluorom ethysu Ifony Dbenzy Doxy) 1 E-5451 H H H H H 4-((Z-(triluorom ethy sufony Dbenzy Doxy) 1
[0409]
[Table 284]
cornpound R] R2 Rj R4 R p E-5452 H H H H H 2-((3-(trifluorom ethysu Ifony Dbenzy Doxy) 1 E-5453 H H H H H 3-((3-(trifluorom ethysu Ifony Dbenzy Doxy) 1 E-5454 H H H H H 4-((3-rifluorom ethysu Ifony Dbenzy Doxy) 1 E-5455 H H H H H 2-((4-(trifluorom ethysu Ifony Dbenzy Doxy) 1 E-5456 H H H H H 3 -((4-(triflu orom ethy su fony Dbenzy Doxy) 1 E-5457 H H H H H 4-((4-(trifluorom ethysu Ifony Dbenzy Doxy) 1 E-5458 H H H H H 2 -((2 -am in ob e nzy Do xy)1 E -5 4 59 H H H H H 3 -((2 -am in ob e nzy Do xy)1 E -5 4 60 H H H H H 4 -((2-am inob e nzy D o xy)1 E -5 4 61 H H H H H 2 - M3-am in o be nzy Do xy)1 E -5 4 62 H H H H H 3 - M3-am in o be nzy Do xy)1 E -5 4 63 H H H H H 4 -(M3-am in ob e nzy Do xy)1 E -5 4 64 H H H H H 2 -((4 -am in o be nzy Do xy)1 E -5 4 65 H H H H H 3 -((4 -am in o be nzy Do xy)1 E -5 4 66 H H H H H 4 -((4 -am in o be nzy Do xy)1 E -5 4 67 H H H H H 2 -T2- (inethyam ino)benzy Doxy) 1 E-5468 H H H H H 3 -((2- (inethyam ino)benzy Doxy) 1 E-5469 H H H H H 4 -T2- (inethyam ino)benzy Doxy) 1 E-5470 H H H H H 2-((3-(mnethyam ino)benzy Doxy) 1 E-5471 H H H H H 3 -T3- (inethyam ino)benzy Doxy) 1 E-5472 H H H H H 4-((3-(mnethyam ino)benzy Doxy) 1 E-5473 H H H H H 2-((4-(mnethyam ino)benzy Doxy) 1 E-5474 H H H H H 3-((4-(jmethyam ino)benzy Doxy) 1 E-5475 H H H H H 4 -74- inethyam ino)benzy Doxy) 1 E-5476 H H H H H 2-((2-(dhiethy lam ino)benzy I)oxy) 1 E-5477 H H H H H 3-((2-(dhiethy lam ino)benzy I)oxy) 1 E-5478 H H H H H 4-((2-(dhiethy lam ino)benzy I)oxy) 1 E-5479 H H H H H 2-((3-(dhiethy lam ino)benzy I)oxy) 1 E-5480 H H H H H 3-777-(dhiethy lam ino)benzy I)oxy) 1 E-5481 H H H H H 4-((3-(dhiethy lam ino)benzy I)oxy) 1 E-5482 H H H H H 2-(4---(dhiethy lam ino)benzyDoxy) 1 E-5483 H H H H H 3-((4-(dhiethy lam ino)benzy I)oxy) 1 E-5484 H H H H H 4-((4-(dhiethy lam ino)benzy I)oxy) 1 E-5485 H H H H H 2-((2-cyanobenzy Doxy) 1 E-5486 H H H H H 3-((2-cyanobenzy Doxy) 1 E-5487 H H H H H 4-((2-cyanobenzy Doxy) 1 E-5488 H H H H H 2-((3-cyanobenzy Doxy) 1 E-5489 H H H H H 3-((3-cyanobenzy Doxy) 1 E-5490 H H H H H 4-((3-cyanobenzy Doxy) 1 E-5491 H H H H H 2-((4-cyanobenzy Doxy) 1 E-5492 H H H H H 3-((4-cyanobenzy Doxy) 1 E-5493 H H H H H 4-((4-cyanobenzy Doxy) 1 E-5494 H H H H H 2-((2-n itrobenzy Doxy) 1 E-5495 H H H H H 3-((2-n itrobenzy Doxy) 1 E-5496 H H H H H 4-((2-n itrobenzy Doxy) 1 E-5497 H H H H H 2-((3-n itrobenzy Doxy) 1 E-5498 H H H H H 3-((3-n itrobenzy Doxy) 1 E-5499 H H H H H 4-((3-n itrobenzy Doxy) 1 E-5500 H H H H H 2-((4-n itrobenzy Doxy) 1 E-5501 H H H H H 3-((4-n itrobenzy Doxy) 1 E-5502 H H H H H 4-((4-n itrobenzy Doxy) 1 E-5503 H H H H H 2-N H2 1 E-5504 H H H H H 3-N H 2 1 E-5505 H H H H H 4-N H 2 1 E-5506 H H H H H 2-N HM e 1 E-5507 H H H H H 3-N HM e 1 E-5508 H H H H H 4-N HM e 1
[0410]
[Table 285]
com pound R' R2 R- R44 R (Rd)m P E-5509 H H H H H 2-NH Et 1 E-5510 H H H H H 3-NH Et 1 E-5511 H H H H H 4-NH Et 1 E-5512 H H H H H 2-N (M e) 2 E-5513 H H H H H 3-N (M e) 2 E-5514 H H H H H 4-N (M e) 2 E-5515 H H H H H 2-N(Et) 2 E-5516 H H H H H 3-N (EVt 2 E-5517 H H H H H 4-N (EVt 2 E-5518 H H H H H 2-CHO 1 E-5519 H H H H H 3-CHO 1 E-5520 H H H H H 4-CHO 1 E-5521 H H H H H 2-C (=0)0H 1 E-5522 H H H H H 3-C (=0)0H 1 E-5523 H H H H H 4-C (=0)0H 1 E-5524 H H H H H 2-(1,3-dioxolan-2-yD 1 E-5525 H H H H H 3-(1,3-dioxolan-2-yD 1 E-5526 H H H H H 4-(1,3-dioxolan-2-yD 1 E-5527 H H H H H 2-(1,3-dioxan-2-yD 1 E-5528 H H H H H 3-(1,3-dioxan-2-yD 1 E-5529 H H H H H 4-(1,3-dioxan-2-yD 1 E-5530 H H H H H 2-(1H-in idazol-2-yD 1 E-5531 H H H H H 3-(1H-in idazol-2-yD 1 E-5532 H H H H H 4-(1H-i idazol-2-yD 1 E-5533 H H H H H 2-(thiazol-2-yD 1 E-5534 H H H H H 3-(thiazol-2-yD 1 E-5535 H H H H H 4-(thiazol-2-yD 1 E-5536 H H H H H 2-(oxazol-2-yl) 1 E-5537 H H H H H 3-(oxazol-2-yl) 1 E-5538 H H H H H 4-(oxazol-2-yl) 1 E-5539 H H H H H 2-CH=N0H 1 E-5540 H H H H H 3-CH=N0H 1 E-5541 H H H H H 4-CH=N0H 1 E-5542 H H H H H 2-CH=NOMe 1 E-5543 H H H H H 3-CH=NOMe 1 E-5544 H H H H H 4-CH=NOMe 1 E-5545 H H H H H 2-(4,5-dhydro-3-isoxazolyl) 1 E-5546 H H H H H 3-(4,5-dhydro-3-isoxazolyl) 1 E-5547 H H H H H 4-(4,5-dhydro-3-isoxazolyl) 1 E-5548 H H H H H 2-CN 1 E-5549 H H H H H 3-CN 1 E-5550 H H H H H 4-CN 1 E-5551 H H H H H 2-N0 2 1 E-5552 H H H H H 3-N0 2 1 E-5553 H H H H H 4-N0 2 1 E-5554 H H H H H 2,3- 2 1 E-5555 H H H H H 2,4-F 2 1 E-5556 H H H H H 2,5-F 2 1 E-5557 H H H H H 2,6-F 2 1 E-5558 H H H H H 3,4- 2 1 E-5559 H H H H H 3,5-F 2 1 E-5560 H H H H H 2-F,3-CI 1 E-5561 H H H H H 2-F,4-CI 1 E-5562 H H H H H 2-F,5-CI 1 E-5563 H H H H H 2-F,6-CI 1 E-5564 H H H H H 3-F,2-CI 1 E-5565 H H H H H 3-F,4-CI 1
[0411]
[Table 286]
com pound R' R2 R R4 R (Rd)m P E-5566 H H H H H 3-F,5-CI 1 E-5567 H H H H H 3-F,6-CI 1 E-5568 H H H H H 4-F,2-CI 1 E-5569 H H H H H 4-F,3-CI 1 E-5570 H H H H H 2-F,3-MA e 1 E-5571 H H H H H 2-F,4-MA e 1 E-5572 H H H H H 2-F,5-MvAe 1 E-5573 H H H H H 2-F,6-MAe 1 E-5574 H H H H H 3-F,2-MA e 1 E-5575 H H H H H 3-F,4-MA e 1 E-5576 H H H H H 3-F,5-MvAe 1 E-5577 H H H H H 3-F,6-MA e 1 E-5578 H H H H H 4-F,2-M e 1 E-5579 H H H H H 4-F,3-M e 1 E-5580 H H H H H 2-F,3-CF, 1 E-5581 H H H H H 2-F,4-CF, 1 E-5582 H H H H H 2-F,5--CF 1 E-5583 H H H H H 2-F,6- 1 E-5584 H H H H H 3-F,2- 1 E-5585 H H H H H 3-F,4- 1 E-5586 H H H H H 3-F,5-CF3 1 E-5587 H H H H H 3-F,6-CF 1 E-5588 H H H H H 4-F,2-CF 1 E-5589 H H H H H 4-F,3--CF 1 E-5590 H H H H H 2-F,3-0Me 1 E-5591 H H H H H 2-F,4-0Me 1 E-5592 H H H H H 2-F,5-0Me 1 E-5593 H H H H H 2-F,6-0Me 1 E-5594 H H H H H 3-F,2-0Me 1 E-5595 H H H H H 3-F,4-0Me 1 E-5596 H H H H H 3-F,5-0Me 1 E-5597 H H H H H 3-F,6-0Me 1 E-5598 H H H H H 4-F,2-0Me 1 E-5599 H H H H H 4-F,3-0Me 1 E-5600 H H H H H 2,3-C 1 E-5601 H H H H H 2,4-C 1 E-5602 H H H H H 2,b-L 1 E-5603 H H H H H 2,6-C 1 E-5604 H H H H H 3,4-C 1 E-5605 H H H H H 3,5-C 1 E-5606 H H H H H 2-CI,3-Me 1 E-5607 H H H H H 2-CI,4-Me 1 E-5608 H H H H H 2-CI,5-M e 1 E-5609 H H H H H 2-CI,6-Me 1 E-5610 H H H H H 3-CI,2-Me 1 E-5611 H H H H H 3-CI,4-Me 1 E-5612 H H H H H 3-CI,5-Me 1 E-5613 H H H H H 3-CI,6-Me 1 E-5614 H H H H H 4-CI,2-Me 1 E-5615 H H H H H 4-CI,3-Me 1 E-5616 H H H H H 2-C1,3-CF 3 1 E-5617 H H H H H 2-CI,4-CF 1 E-5618 H H H H H 2-CI,5-CF 1 E-5619 H H H H H 2-C1,6-CF 1 E-5620 H H H H H 3-CI,2-CF 3 1 E-5621 H H H H H 3-CI,4-CF 3 1 E-5622 H H H H H 3-C,5-CF 3 1
[0412]
[Table 287]
com pound R' R2 R R4 R (Rd)m P E-5623 H H H H H 3-C1,6-CF 1 E-5624 H H H H H 4-C1,2-CF 1 E-5625 H H H H H 4-C1,3- 3 1 E-5626 H H H H H 2-C,3-0Me 1 E-5627 H H H H H 2-C,4-0Me 1 E-5628 H H H H H 2-C1,5-0Me 1 E-5629 H H H H H 2-C1,6-0Me 1 E-5630 H H H H H 3-C,2-0Me 1 E-5631 H H H H H 3-CI,4-0Me 1 E-5632 H H H H H 3-C1,5-0Me 1 E-5633 H H H H H 3-C1,6-0Me 1 E-5634 H H H H H 4-C,2-0Me 1 E-5635 H H H H H 4-C,3-0Me 1 E-5636 H H H H H 2,3-M e 2 E-5637 H H H H H 2,4-M e 2 1 E-5638 H H H H H 2,5-Me2 1 E-5639 H H H H H 2,6-Me2 1 E-5640 H H H H H 3,4-M e 2 1 E-5641 H H H H H 3,b-M e 2 1 E-5642 H H H H H 2-M e,3-CF 3 1 E-5643 H H H H H 2-M e,4-CF3 1 E-5644 H H H H H 2-M e,5-CF3 1 E-5645 H H H H H 2-M e,6-CF3 1 E-5646 H H H H H 3-M e,2-F 3 1 E-5647 H H H H H 3-M e,4-CF3 1 E-5648 H H H H H 3-M e,5-CF3 1 E-5649 H H H H H 3-M e,6-CF3 1 E-5650 H H H H H 4-M e,2-CF3 1 E-5651 H H H H H 4-M e,3-CF 3 1 E-5652 H H H H H 2-M e,3-0Me 1 E-5653 H H H H H 2-M e,4-0Me 1 E-5654 H H H H H 2-Me,5-0 Me 1 E-5655 H H H H H 2-M e,6-0Me 1 E-5656 H H H H H 3-M e,2-0Me 1 E-5657 H H H H H 3-M e,4-0Me 1 E-5658 H H H H H 3-Me,5-0 Me 1 E-5659 H H H H H 3-M e,6-0Me 1 E-5660 H H H H H 4-M e,2-0Me 1 E-5661 H H H H H 4-Me,3-0Me 1 E-5662 H H H H H 2,3-0Me 2 1 E-5663 H H H H H 2,4-0Me2 1 E-5664 H H H H H 2,b-0Me 2 1 E-5665 H H H H H 2,6-0Me 2 1 E-5666 H H H H H 3,4-0Me 2 1 E-5667 H H H H H 3,5-0Me 2 1 E-5668 H H H H H 2-0Me,3-F 3 1 E-5669 H H H H H 2-0Me,4-CF 3 1 E-5670 H H H H H 2-0Me,5-CF 3 1 E-5671 H H H H H 2-0Me,6-CF 3 1 E-5672 H H H H H 3-0Me,2-F 3 1 E-5673 H H H H H 3-0Me,4-CF 3 1 E-5674 H H H H H 3-0Me,5-CF 3 1 E-5675 H H H H H 3-0Me,6-CF 3 1 E-5676 H H H H H 4-0Me,2-CF 3 1 E-5677 H H H H H 4-0Me,3- F 3 1 E-5678 H H H H H 2-CH F 2,3-F 1 E-5679 H H H H H 2-CH F 2,4-F
[0413]
[Table 288]
com pound R' R2 R R4 R (Rd)m P E-5680 H H H H H 2-CH F 2,5-F 1 E-5681 H H H H H 2-CH F 2,6-F 1 E-5682 H H H H H 2-CHF 2,3-M e 1 E-5683 H H H H H 2-CHF 2,4-Me 1 E-5684 H H H H H 2-CHF 2,b-Me 1 E-5685 H H H H H 2-CHF 2,6-Me 1 E-5686 H H H H H 2-cycbpropyl,3-F 1 E-5687 H H H H H 2-cycbpropyl,4-F 1 E-5688 H H H H H 2-cycbpropyl,5-F 1 E-5689 H H H H H 2-cycbpropyl,6-F 1 E-5690 H H H H H 2-cycbpropyl,3-M e 1 E-5691 H H H H H 2-cycbpropyl,4-M e 1 E-5692 H H H H H 2-cycbpropyl,5-Me 1 E-5693 H H H H H 2-cycbpropyl,6-M e 1 E-5694 H H H H H 2-ethenyl,3-F 1 E-5695 H H H H H 2-ethenyl,4-F 1 E-5696 H H H H H 2-ethenyl,5-F 1 E-5697 H H H H H 2-ethenyl,6-F 1 E-5698 H H H H H 2-ethenyl,3-Me 1 E-5699 H H H H H 2-ethenyl,4-Me 1 E-5700 H H H H H 2-ethenyl1,5-Me 1 E-5701 H H H H H 2-ethenyl,6-M e 1 E-5702 H H H H H 2-0 Et,3-F 1 E-5703 H H H H H 2-0 Et4-F 1 E-5704 H H H H H 2-0 Et,5-F 1 E-5705 H H H H H 2-0Et,6-F 1 E-5706 H H H H H 2-0Et,3-CI 1 E-5707 H H H H H 2-0Et4-CI 1 E-5708 H H H H H 2-0Et,5-CI 1 E-5709 H H H H H 2-0Et,6-CI 1 E-5710 H H H H H 2-0Et3-Me 1 E-5711 H H H H H 2-0Et4-Me 1 E-5712 H H H H H 2-0Et5-Me 1 E-5713 H H H H H 2-0Et6-Me 1 E-5714 H H H H H 2-0Pr,3-F 1 E-5715 H H H H H 2-0Pr,4-F 1 E-5716 H H H H H 2-0Pr,5-F 1 E-5717 H H H H H 2-0Pr,6-F 1 E-5718 H H H H H 2-0 Pr,3-M e 1 E-5719 H H H H H 2-0 Pr,4-M e 1 E-5720 H H H H H 2-0 Pr,5-M e 1 E-5721 H H H H H 2-0 Pr,6-M e 1 E-5722 H H H H H 2-0 (/-Pr),3-F 1 E-5723 H H H H H 2-0 (/-Pr),4-F 1 E-5724 H H H H H 2-0 (/-Pr),5-F 1 E-5725 H H H H H 2-0 (/-Pr),6-F 1 E-5726 H H H H H 2-0 (/-Pr),3-M e 1 E-5727 H H H H H 2-0 (/-Pr),4-M e 1 E-5728 H H H H H 2-0 (-Pr),5--Me 1 E-5729 H H H H H 2-0 (/-Pr),6-M e 1 E-5730 H H H H H 2-0 CF,,3-F 1 E-5731 H H H H H 2-0 CF3,4-F 1 E-5732 H H H H H 2-0 CF3 ,5-F 1 E-5733 H H H H H 2-0 CF3 ,6-F 1 E-5734 H H H H H 2-0 CF 3 ,3-M e 1 E-5735 H H H H H 2-0 CF3 ,4-M e 1 E-5736 H H H H H 2-0 CF,b-M e 1
[0414]
[Table 289]
com pound R' R2 R R4 R (Rd)m P E-5737 H H H H H 2-0CF 3 ,6-M e 1 E-5738 H H H H H 2-OCHF 2,3-F 1 E-5739 H H H H H 2-OCHF 2,4-F 1 E-5740 H H H H H 2-OCHF 2,b-F 1 E-5741 H H H H H 2-OCHF 2,6-F 1 E-5742 H H H H H 2-0CHF 2 ,3-Me 1 E-5743 H H H H H 2-0 CH F 2,4-M e 1 E-5744 H H H H H 2-0 CH F 2 ,5-M e 1 E-5745 H H H H H 2-0 CH F 2 ,6-M e 1 E-5746 H H H H H 2-(cycbpropybxy),3-F 1 E-5747 H H H H H 2-(cycbpropybxy),4-F 1 E-5748 H H H H H 2-(cycbpropybxy),5-F 1 E-5749 H H H H H 2-(cycbpropybxy),6-F 1 E-5750 H H H H H 2-(cycbpropybxy),3-M e 1 E-5751 H H H H H 2-(cycbpropybxy),4-M e 1 E-5752 H H H H H 2-(cycbpropybxy),5-M e 1 E-5753 H H H H H 2-(cycbpropybxy),6-Me 1 E-5754 H H H H H 2-(oxiran-2-yl),3-F 1 E-5755 H H H H H 2-(oxiran-2-yl),4-F 1 E-5756 H H H H H 2-(oxiran-2-yl),5-F 1 E-5757 H H H H H 2-(oxiran-2-y),6-F 1 E-5758 H H H H H 2-(oxiran-2-yD,3-Me 1 E-5759 H H H H H 2-(oxiran-2-yD,4-Me 1 E-5760 H H H H H 2-(oxiran-2-yD,5-M e 1 E-5761 H H H H H 2-(oxiran-2-yD,6-Me 1 E-5762 H H H H H 2-(oxiran-2-y IethyD,3-F 1 E-5763 H H H H H 2-(oxiran-2-y IethyD,4-F 1 E-5764 H H H H H 2-(oxiran-2-y IethyD,5-F 1 E-5765 H H H H H 2-(oxiran-2-y IethyD,6-F 1 E-5766 H H H H H 2-(oxiran-2-yh ethyD,3-Me 1 E-5767 H H H H H 2-(oxiran-2-yh ethyD,4-Me 1 E-5768 H H H H H 2-(oxiran-2-yh ethyD,5-M e 1 E-5769 H H H H H 2-(oxiran-2-yh ethyD,6-Me 1 E-5770 H H H H H 2-SMe,3-F 1 E-5771 H H H H H 2-SMe,4-F 1 E-5772 H H H H H 2-SMe,5-F 1 E-5773 H H H H H 2-SMe,6-F 1 E-5774 H H H H H 2-SMe,3-M e 1 E-5775 H H H H H 2-SMe,4-M e 1 E-5776 H H H H H 2-SMe,5-Me 1 E-5777 H H H H H 2-SMe,6-M e 1 E-5778 H H H H H 2-SEt,3-F 1 E-5779 H H H H H 2-SEt,4-F 1 E-5780 H H H H H 2-SEt,5-F 1 E-5781 H H H H H 2-SEt,6-F 1 E-5782 H H H H H 2-SEt,3-M e 1 E-5783 H H H H H 2-SEt,4-M e 1 E-5784 H H H H H 2-SEt,5-M e 1 E-5785 H H H H H 2-SEt,6-M e 1 E-5786 H H H H H 2-S (=0)M e,3-F 1 E-5787 H H H H H 2-S (=0)M e,4-F 1 E-5788 H H H H H 2-S (=0)M e,5-F 1 E-5789 H H H H H 2-S (=0)M e,6-F 1 E-5790 H H H H H 3-S (=0)M e,2-F 1 E-5791 H H H H H 3-S (=0)M e,4-F 1 E-5792 H H H H H 3-S (=0)M e,5-F 1 E-5793 H H H H H 3-S (=0)M e,6-F 1
[0415]
[Table 290]
com pound R R2 R R (R)m P E-5794 H H H H H 2-S(=0)Me,3-M e 1 E-5795 H H H H H 2-S(=0)Me,4-M e 1 E-5796 H H H H H 2-S(=0)Me,5-M e 1 E-5797 H H H H H 2-S(=0)Me,6-M e 1 E-5798 H H H H H 3-S(=0)Me,2-M e 1 E-5799 H H H H H 3-S(=0)Me,4-M e 1 E-5800 H H H H H 3-S(=0)Me,5-M e 1 E-5801 H H H H H 3-S(=0)Me,6-M e 1 E-5802 H H H H H 2-S (=0) 2 M e,3-F 1 E-5803 H H H H H 2-S (=0) 2M e,4-F 1 E-5804 H H H H H 2-S (=0) 2 M e,b-F 1 E-5805 H H H H H 2-S (=0) 2 M e,6-F 1 E-5806 H H H H H 2-S(=0) 2Me,3-M e 1 E-5807 H H H H H 2-S (=0) 2M e,4-M e 1 E-5808 H H H H H 2-S(=0) 2Me,5-M e 1 E-5809 H H H H H 2-S(=0) 2Me,6-M e 1 E-5810 H H H H H 2-SCF,,3-F 1 E-5811 H H H H H 2-SGa3 ,4-F 1 E-5812 H H H H H 2-SCF 3 ,b-F 1 E-5813 H H H H H 2-SCF 3 ,6-F 1 E-5814 H H H H H 2-SCF 3 ,3-M e 1 E-5815 H H H H H 2-SCF 3 ,4-M e 1 E-5816 H H H H H 2-SCF 3 ,5-M e 1 E-5817 H H H H H 2-SCF 3 ,6-M e 1 E-5818 H H H H H 2-S(=O)CF 3 ,3-F 1 E-5819 H H H H H 2-S(=0)CF 3 ,4-F 1 E-5820 H H H H H 2-S(=O)CF 3 ,5-F 1 E-5821 H H H H H 2-S(=O)0F 3 ,6-F 1 E-5822 H H H H H 2-S(=0)CF 3 ,3-Me 1 E-5823 H H H H H 2-S(=0)CF 3 ,4-Me 1 E-5824 H H H H H 2-S(=0)CF 3 5-Me 1 E-5825 H H H H H 2-S(=0)CF 3 ,6-Me 1 E-5826 H H H H H 2-S (=0) 2CF3 ,3-F 1 E-5827 H H H H H 2-S (=0) 2CF3A,4-F 1 E-5828 H H H H H 2-S (=0) 2CF3 ,5-F 1 E-5829 H H H H H 2-S (=0) 2CF3 ,6-F 1 E-5830 H H H H H 2-S (=0) 2CF 3 ,3-M e 1 E-5831 H H H H H 2-S (=0) 2CF 3,4-e 1 E-5832 H H H H H 2-S (=0) 2CF 3 ,b-Me 1 E-5833 H H H H H 2-S (=0) 2CF 3 ,6-Me 1 E-5834 H H H H H 2-(cycbpropylthio),3-F 1 E-5835 H H H H H 2-(cycbpropylthio),4-F 1 E-5836 H H H H H 2-(cycbpropylthio),5-F 1 E-5837 H H H H H 2-(cycbpropylthio),6-F 1 E-5838 H H H H H 2-(cycobpropylthio),3-Me 1 E-5839 H H H H H 2-(cycobpropylthio),4-M e 1 E-5840 H H H H H 2-(cycobpropylthio),5-M e 1 E-5841 H H H H H 2-(cycobpropylthio),6-Me 1 E-5842 H H H H H 2-C(=0)Me,3-F 1 E-5843 H H H H H 2-C(=0)Me,4-F 1 E-5844 H H H H H 2-C(=0)Me,5-F 1 E-5845 H H H H H 2-C(=0)Me,6-F 1 E-5846 H H H H H 2-C(=0)Me,3-M e 1 E-5847 H H H H H 2-C(=0)Me,4-M e 1 E-5848 H H H H H 2-C (= )M e,5-M e 1 E-5849 H H H H H 2-C (=0)M e,6-M e 1 E-5850 H H H H H 3-C(=0)Me,2-F 1
[0416]
[Table 291]
com pound R R2 R R (R)m P E-5851 H H H H H 3-C(=0)Me,4-F 1 E-5852 H H H H H 3-C(=0)Me,5-F 1 E-5853 H H H H H 3-C(=0)Me,6-F 1 E-5854 H H H H H 3-C(=0)Me,2-M e 1 E-5855 H H H H H 3-C(=0)Me,4-M e 1 E-5856 H H H H H 3-C(=0)Me,5-M e 1 E-5857 H H H H H 3-C(=0)Me,6--M e 1 E-5858 H H H H H 2-C(=0)0Me,3-F 1 E-5859 H H H H H 2-C(=0)0Me,4-F 1 E-5860 H H H H H 2-C(=0)0Me,5-F 1 E-5861 H H H H H 2-C(=0)0Me,6-F 1 E-5862 H H H H H 2-C(=0)0Me,3 -M e 1 E-5863 H H H H H 2-C(=0)0Me,4 -M e 1 E-5864 H H H H H 2-C(=0)0Me,5-M e 1 E-5865 H H H H H 2-C(=0)0Me,6--M e 1 E-5866 H H H H H 2-C(=0)0Et3-F 1 E-5867 H H H H H 2-C(=0)0Et4-F 1 E-5868 H H H H H 2-C(=0)0Et5-F 1 E-5869 H H H H H 2-C(=0)0Et6-F 1 E-5870 H H H H H 2-C(=0)0Et,3-M e 1 E-5871 H H H H H 2-C(=0)0Et,4-Me 1 E-5872 H H H H H 2-C(=0)0Et,5-M e 1 E-5873 H H H H H 2-C(=0)0Et,6-M e 1 E-5874 H H H H H 2-C(=0)NH 2 ,3-F 1 E-5875 H H H H H 2-C (=0)NH 2 ,4-F 1 E-5876 H H H H H 2-C (=0)NH 2 ,5-F 1 E-5877 H H H H H 2-C (=0)NH 2 ,6-F 1 E-5878 H H H H H 2-C(=0)NH 2,3-M e 1 E-5879 H H H H H 2-C(=0)NH 2 ,4-M e 1 E-5880 H H H H H 2-C(=0)NH 2 ,5-M e 1 E-5881 H H H H H 2-C(=0)NH 2,6-M e 1 E-5882 H H H H H 2-C(=0)NHMe,3-F 1 E-5883 H H H H H 2-C(=0)NHMe,4-F 1 E-5884 H H H H H 2-C(=0)NHMe,5-F 1 E-5885 H H H H H 2-C(=0)NHMe,6-F 1 E-5886 H H H H H 2-C(=0)NHMe,3-M e 1 E-5887 H H H H H 2-C(=0)NHMe,4-M e 1 E-5888 H H H H H 2-C(=0)NHMe,5 -Me 1 E-5889 H H H H H 2-C(=0)NHMe,6--M e 1 E-5890 H H H H H 2-C(=0)NMe 2,3-F 1 E-5891 H H H H H 2-C (= )N M e 2,4-F 1 E-5892 H H H H H 2-C(=0)NMe 2,b- 1 E-5893 H H H H H 2-C(=0)NMe 2,6-F 1 E-5894 H H H H H 2-C(=0)NMe 2,3-Me 1 E-5895 H H H H H 2-C(=0)NMe 2,4-Me 1 E-5896 H H H H H 2-C(=0)NMe 2,b-Me 1 E-5897 H H H H H 2-C(=0)NMe 2 ,6-M e 1 E-5898 H H H H H 2-CH 20H,3-F 1 E-5899 H H H H H 2-CH20H,4-F 1 E-5900 H H H H H 2-CH 20H,5-F 1 E-5901 H H H H H 2-CH 20H,6-F 1 E-5902 H H H H H 2-CH20H,3-M e 1 E-5903 H H H H H 2-CH20H,4--M e 1 E-5904 H H H H H 2-CH20H,b5-M e 1 E-5905 H H H H H 2-CH20H,6-M e 1 E-5906 H H H H H 2-CH 20CH 3 ,3-F 1 E-5907 H H H H H 2-CH 200H 3,44-F 1
[0417]
[Table 292]
com pound R' R2 R R R (R°)m P E-5908 H H H H H 2-GH 20H 3,b-F E-5909 H H H H H 2-GH 20H 3 ,6-F E-5910 H H H H H 2-CH 2UCH 3 ,3-M e E-5911 H H H H H 2-CH 2UCH 3 ,4-M e E-5912 H H H H H 2-CH 2UCH 3 ,b-M e E-5913 H H H H H 2-CH 2UCH 3 ,6-M e E-5914 H H H H H 2-GH 20H 2 CH 3 ,3-F 1 E-5915 H H H H H 2-GH 20H 2CH 3 ,4-F 1 E-5916 H H H H H 2-GH 20H 2CH 3 ,b-F 1 E-5917 H H H H H 2-GH 20H 2CH 3 ,6- 1 E-5918 H H H H H 2-GH 2UCH 2 CH 3 ,3-M e 1 E-5919 H H H H H 2-GH 2 CH 2CH 3 ,4-M e 1 E-5920 H H H H H 2-GH 2UCH 2 CH 3 ,b-M e 1 E-5921 H H H H H 2-GH 2UCH 2 CH 3 ,6-M e 1 E-5922 H H H H H 2-UC(=U)CH 3 ,3-F 1 E-5923 H H H H H 2-UC(=U)CH 3 ,4-F 1 E-5924 H H H H H 2-UC(=U)CH 3 ,b-F 1 E-5925 H H H H H 2-0(=U)GH 3,6-F 1 E-5926 H H H H H 2-00(=U)CH 3 ,3-M e 1 E-5927 H H H H H 2-0(=U)CH 3,4-M e 1 E-5928 H H H H H 2-00(=0)CH 3 ,b-Me 1 E-5929 H H H H H 2-0(=U)CH 3 ,6-M e 1 E-5930 H H H H H 2-OS(=U) 2CH 3,3-F 1 E-5931 H H H H H 2-OS(=U) 20H 3,4-F 1 E-5932 H H H H H 2-OS(=U) 2CH 3,b-F 1 E-5933 H H H H H 2-OS(=U) 20H 3,6-F 1 E-5934 H H H H H 2-OS(=U) 2CH 3 ,3-M e 1 E-5935 H H H H H 2-OS(=U) 20H 3 ,4-M e 1 E-5936 H H H H H 2-OS(=U) 20H 3 ,b-M e 1 E-5937 H H H H H 2-OS(=U) 2 CH 3 ,6-M e 1 E-5938 H H H H H 2-GH 2SCH 3 3-F 1 E-5939 H H H H H 2-GH 2SCH 3,4-F 1 E-5940 H H H H H 2-GH 2SCH 3,5-F 1 E-5941 H H H H H 2-GH 2SCH 3,6-F 1 E-5942 H H H H H 2-OH 2S0H 3,3-M e 1 E-5943 H H H H H 2-OH 2S0H 3,4-M e 1 E-5944 H H H H H 2-GH 2 S0H 3,b-M e 1 E-5945 H H H H H 2-GH 2 S0H 3,6-M e 1 E-5946 H H H H H 2-GH 2SCF 3 ,3-F 1 E-5947 H H H H H 2-GH 2SCF 3 ,4-F 1 E-5948 H H H H H 2-GH 2SCF 3 ,b-F 1 E-5949 H H H H H 2-GH 2SCF 3 ,6-F 1 E-5950 H H H H H 2-OH 2S0F 3 ,3-M e 1 E-5951 H H H H H 2-GH 2S0F 3 ,4-M e E-5952 H H H H H 2-OH 2S0F 3 ,5-M e E-5953 H H H H H 2-OH 2S0F 3 ,6-M e E-5954 H H H H H 2-(benzyloxy),3-F 1 E-5955 H H H H H 2-(benzyloxy),4-F 1 E-5956 H H H H H 2-(benzyloxy),b-F 1 E-5957 H H H H H 2-(benzyloxy),6-F 1 E-5958 H H H H H 2-(benzy bxy),3-M e 1 E-5959 H H H H H 2-(benzy bxy),4-M e 1 E-5960 H H H H H 2-(benzy bxy),b-M e 1 E-5961 H H H H H 2-(benzy bxy),6-M e 1 E-5962 H H H H H 2-NH 2 ,3-F 1 E-5963 H H H H H 2-NH 2 ,44 1 E-5964 H H H H H 2-NH 2,b-H1
[0418]
[Table 293]
com pound R' R2 R R4 R (Rd)m P E-5965 H H H H H 2-NH 2 ,6-F 1 E-5966 H H H H H 2-NH 2,3-Me 1 E-5967 H H H H H 2-NH 2,4-Me 1 E-5968 H H H H H 2-NH 2,-Me 1 E-5969 H H H H H 2-NH 2,6-Me 1 E-5970 H H H H H 2-NHMe,3-F 1 E-5971 H H H H H 2-NHMe,4-F 1 E-5972 H H H H H 2-NHMe,5-F 1 E-5973 H H H H H 2-NHMe,6-F 1 E-5974 H H H H H 2-NHMe,3-M e 1 E-5975 H H H H H 2-NHMe,4-M e 1 E-5976 H H H H H 2-NHMe,5-M e 1 E-5977 H H H H H 2-NHMe,6-M e 1 E-5978 H H H H H 2-NHEt,3-F 1 E-5979 H H H H H 2-NHEt4-F 1 E-5980 H H H H H 2-NHEt,5-F 1 E-5981 H H H H H 2-NHEt,6-F 1 E-5982 H H H H H 2-NHEt,3-M e 1 E-5983 H H H H H 2-NHEt,4-Me 1 E-5984 H H H H H 2-NHEt,5-M e 1 E-5985 H H H H H 2-NHEt,6-M e 1 E-5986 H H H H H 2-NMe 2 ,3-F 1 E-5987 H H H H H 2-NMe 2 ,4-F 1 E-5988 H H H H H 2-NMe 2 ,5-F 1 E-5989 H H H H H 2-NMe 2 ,6-F 1 E-5990 H H H H H 2-NMe 2 ,3-M e 1 E-5991 H H H H H 2-NMe 2 ,4-M e 1 E-5992 H H H H H 2-NMe 2 ,b-M e 1 E-5993 H H H H H 2-NMe 2 ,6-M e 1 E-5994 H H H H H 2-NEt2,3-F 1 E-5995 H H H H H 2-NEt2,4-F 1 E-5996 H H H H H 2-NEt2,5-F 1 E-5997 H H H H H 2-NEt2,6-F 1 E-5998 H H H H H 2-NEt2,3-MAe 1 E-5999 H H H H H 2-NEt2,4-Me 1 E-6000 H H H H H 2-NEt2,5-MAe 1 E-6001 H H H H H 2-NEt2,6-M e 1 E-6002 H H H H H 2-CHO,3-F 1 E-6003 H H H H H 2-CH04-F 1 E-6004 H H H H H 2-CHO,5-F 1 E-6005 H H H H H 2-CHO,6-F 1 E-6006 H H H H H 2-CHO,3-M e 1 E-6007 H H H H H 2-CHO,4-Me 1 E-6008 H H H H H 2-CHO,5-M e 1 E-6009 H H H H H 2-CHO,6-M e 1 E-6010 H H H H H 2-C(=0)0H,3-F 1 E-6011 H H H H H 2-C(=0)0H,4-F 1 E-6012 H H H H H 2-C(=0)0H,5-F 1 E-6013 H H H H H 2-C(=0)0H,6-F 1 E-6014 H H H H H 2-C(=0)0H,3-M e 1 E-6015 H H H H H 2-C(=0)0H,4-M e 1 E-6016 H H H H H 2-C(=0)0H,b5-M e 1 E-6017 H H H H H 2-C(=0)0H,6-M e 1 E-6018 H H H H H 2-(1,3-dbxolan-2-yD,3-F 1 E-6019 H H H H H 2-(1,3-dbxolan-2-yD,4-F 1 E-6020 H H H H H 2-(1,3-dbxolan-2-yD,5-F 1 E-6021 H H H H H 2-0,3-dbxolan-2-yD,6-F 1
[0419]
[Table 294]
com pound R R2 R R (R)m P E-6022 H H H H H 2-0,3-dioxolan-2-yD,3-Me 1 E-6023 H H H H H 2-0,3-dioxolan-2-yD,4-Me 1 E-6024 H H H H H 2-0,3-dioxolan-2-yD,5-M e 1 E-6025 H H H H H 2-0,3-dioxolan-2-yD,6-Me 1 E-6026 H H H H H 2-0,3-dioxan-2-yD,3-F 1 E-6027 H H H H H 2-0,3-dioxan-2-yD,4-F 1 E-6028 H H H H H 2-0,3-dioxan-2-yD,5-F 1 E-6029 H H H H H 2-0,3-dioxan-2-yD,6-F 1 E-6030 H H H H H 2-(1,3-dioxan-2-yD,3-Me 1 E-6031 H H H H H 2-(1,3-dioxan-2-yD,4-Me 1 E-6032 H H H H H 2-(1,3-dioxan-2-yD,5-M e 1 E-6033 H H H H H 2-0,3-dioxan-2-yD,6-Me 1 E-6034 H H H H H 2-(thiazol-2-yD,3-F 1 E-6035 H H H H H 2-(thiazol-2-yD,4-F 1 E-6036 H H H H H 2-(thiazol-2-yD,5-F 1 E-6037 H H H H H 2-(thiazol-2-yD,6-F 1 E-6038 H H H H H 2-(thiazol-2-yD,3-Me 1 E-6039 H H H H H 2-(thiazol-2-yD,4-M e 1 E-6040 H H H H H 2-(thiazol-2-yD,5-M e 1 E-6041 H H H H H 2-(thiazol-2-yD,6-M e 1 E-6042 H H H H H 2-(oxazol-2-y1),3-F 1 E-6043 H H H H H 2-(oxazol-2-yl)4-F 1 E-6044 H H H H H 2-(oxazol-2-y1),5-F 1 E-6045 H H H H H 2-(oxazol-2-y1),6-F 1 E-6046 H H H H H 2-(oxazol-2-yD,3-Me 1 E-6047 H H H H H 2-(oxazol-2-yD,4-Me 1 E-6048 H H H H H 2-(oxazol-2-yD,5-M e 1 E-6049 H H H H H 2-(oxazol-2-yD,6-M e 1 E-6050 H H H H H 2-CH=N0H,3-F 1 E-6051 H H H H H 2-CH=N0H,4-F 1 E-6052 H H H H H 2-CH=N0H,5-F 1 E-6053 H H H H H 2-CH=N0H,6-F 1 E-6054 H H H H H 2-CH=N0H,3-M e 1 E-6055 H H H H H 2-CH=N0H,4-M e 1 E-6056 H H H H H 2-CH=N0H, 5-M e 1 E-6057 H H H H H 2-CH=N0H,6-M e 1 E-6058 H H H H H 2-CH=N0Me,3-F 1 E-6059 H H H H H 2-CH=N0Me,4-F 1 E-6060 H H H H H 2-CH=N0Me,5-F 1 E-6061 H H H H H 2-CH=N0Me,6-F 1 E-6062 H H H H H 2-CH=N0Me,3-M e 1 E-6063 H H H H H 2-CH=N0Me,4-M e 1 E-6064 H H H H H 2-CH=N0Me,5-M e 1 E-6065 H H H H H 2-CH=N0Me,6-M e 1 E-6066 H H H H H 2-CN,3-F 1 E-6067 H H H H H 2-CN,4-F 1 E-6068 H H H H H 2-CN,5-F 1 E-6069 H H H H H 2-CN,6-F 1 E-6070 H H H H H 2-CN,3-CI 1 E-6071 H H H H H 2-CN,4-CI 1 E-6072 H H H H H 2-CN5-Cl 1 E-6073 H H H H H 2-CN,6-Cl 1 E-6074 H H H H H 2-CN,3-M e 1 E-6075 H H H H H 2-CN,4-M e 1 E-6076 H H H H H 2-CN,5-M e 1 E-6077 H H H H H 2-CN,6-M e 1 E-6078 H H H H H 2-CN,3-0Me 1
[0420]
[Table 295]
com pound R' R2 R R4 R (Rd)m P E-6079 H H H H H 2-CN,4-0Me 1 E-6080 H H H H H 2-CN,5-0Me 1 E-6081 H H H H H 2-CN,6-0Me 1 E-6082 H H H H H 3-CN,2-F 1 E-6083 H H H H H 3-CN,4-F 1 E-6084 H H H H H 3-CN,5-F 1 E-6085 H H H H H 3-CN,6-F 1 E-6086 H H H H H 3-CN2-CI 1 E-6087 H H H H H 3-CN,4-CI 1 E-6088 H H H H H 3-CN,5-CI 1 E-6089 H H H H H 3-CN,6-CI 1 E-6090 H H H H H 3-CN,2-M e 1 E-6091 H H H H H 3-CN,4-M e 1 E-6092 H H H H H 3-CN,5-MAe 1 E-6093 H H H H H 3-CN,6-MA e 1 E-6094 H H H H H 3-CN,2-0Me 1 E-6095 H H H H H 3-CN,4-0Me 1 E-6096 H H H H H 3-CN,5-0Me 1 E-6097 H H H H H 3-CN,6-0Me 1 E-6098 H H H H H 4-CN,2-F 1 E-6099 H H H H H 4-CN,3-F 1 E-6100 H H H H H 4-CN 2-C 1 1 E-6101 H H H H H 4-CN 3-C 1 1 E-6102 H H H H H 4-CN,2-M e 1 E-6103 H H H H H 4-CN,3-M e 1 E-6104 H H H H H 4-CN,2-0Me 1 E-6105 H H H H H 4-CN,3-0Me 1 E-6106 H H H H H 2-N0 2,3-F 1 E-6107 H H H H H 2-N0 2 ,4-4 E-6108 H H H H H 2-N0 2 ,5-F 1 E-6109 H H H H H 2-N0 2,6-F 1 E-6110 H H H H H 2-N0 2,3-MAe 1 E-6111 H H H H H 2-N0 2,4-MvAe 1 E-6112 H H H H H 2-N0 2,5-M e 1 E-6113 H H H H H 2-N0 2,6-MA e 1 E-6114 H H H H H 2-M e,3,4-F2 1 E-6115 H H H H H 2-M e,3,b-F 2 1 E-6116 H H H H H 2-M e,3,6-F 2 1 E-6117 H H H H H 2-M e,4,b-F 2 1 E-6118 H H H H H 2-0 M e,3,4-F 2 1 E-6119 H H H H H 2-0 M e,3,5-F 2 1 E-6120 H H H H H 2-0Me,3,6-F 2 1 E-6121 H H H H H 2-0Me,4,5-F 2 1 E-6122 H H H H H 2-(CH 2) 3-3 1 E-6123 H H H H H 2-(CH 2) 4-3 1 E-6124 H H H H H 2-(0CH 20H 2)-3 1 E-6125 H H H H H 2-(0CH 2CH 2CH 2)-3 1 E-6126 H H H H H 2-(CH 2 CH 20)-3 1 E-6127 H H H H H 2-(CH 2 CH 2CH 20)-3 1 E-6128 H H H H H 3-(CH 2) 3-4 1 E-6129 H H H H H 3-(CH 2 4-4 1 E-6130 H H H H H 3-(0CH 2CH 2)-4 1 E-6131 H H H H H 3-(0CH 2CH 2CH 2)-4 1 E-6132 H H H H H 3-(CH 2 CH 20)-4 1 E-6133 H H H H H 3-(CH 20H 2 H 20)-4 1 E-6134 H H H H H 2-(0CH 20)-3 1 E-6135 H H H H H 3-(0CH 20)-4
[0421]
[Table 296]
cornpound R' R2 R(RRtR m P E-6136 H H H H H 2-(00CH 20H 2 0 )-3 1 E-6 137 H H H H H 3-(00CH 20H 2 0 )-4 1 E-6 138 H H H H H 2-(00CF 20 )-3 1 E-6 139 H H H H H 3-(00CF 20 )-4 1 E-6 140 H H H H H 2-Mvle,6-Et 1 E-6 141 H H H H H 2-Mvle,4,b-F 2 1 E-6 142 H H H H H 2-oycopropyl,6-OM e 1 E-6 143 H H H H H 2-Mvieb-Et 1 E-6 144 H H H H H 2,6-Et 2 1 E-6 145 H H H H H 2-Et,6-F 1 E-6 146 H H H H H 2-CH 200CH 3 ,6-CI1 1 E-6 147 H H H H H 2-CH 200CH 20H3 ,6-CI1 1 r7-14 8 H H H H H 2-C H 2 N Me 2 1
[0422]
[Table 297]
3 2 R R
N R H 1 5 (O)p R com pound R1 R2 R R4 R' p F-0001 H H H H H CI 0 F-0002 H H H H H Br 0 F-0003 H H H H H 1 0 F-0004 H H H H H OS(=0) 2Me 0 F-0005 H H H H H OS (=0)2CF 3 0 F-0006 H H H H H OS (=0)2CF 2CF 3 0 F-0007 H H H H H OS (=0) 2 CF 2CF 2 CF3 0 F-0008 H H H H H OS(=O ) 2 F 2UF 2 UF 2CF 3 0 F-0009 H H H H H 0 S(= 0) 2 (4-MePh) 0 F-0010 H H H H H OS(=0) 2N (Me) 2 0 F-0011 H H H H H OS(=0) 2N (Et 2 0 F-0012 H H H H H naphthalen-1-yl 0 F-0013 H H H H H 2-F-naphthabn-1-yl 0 F-0014 H H H H H 2-M e-naphthalen-1-yl 0 F-0015 H H H H H 2-CF 3 -naphthakn-1-yl 0 F-0016 H H H H H 2-0M e-naphthalen-1-y1 0 F-0017 H H H H H naphthaen-2-yl 0 F-0018 H H H H H 1-F-naphthalen-2-yl 0 F-0019 H H H H H 1-M e-naphthalen-2-yl 0 F-0020 H H H H H 1-CF 3 -naphtha bn-2-yl 0 F-0021 H H H H H 1-0M e-naphthalen-2-y1 0 F-0022 H H H H H 3-F-naphthabn-2-yl 0 F-0023 H H H H H 3-M e-naphthabn-2-y 0 F-0024 H H H H H 3-CF3 -naphthakn-2-yl 0 F-0025 H H H H H 3-0 M e-naphthalen-2-y1 0 F-0026 H H H H H pyrid h-2-yl 0 F-0027 H H H H H 3-F-pyrid h-2-y1 0 F-0028 H H H H H 4-F-pyrid h-2-y1 0 F-0029 H H H H H 5-F-pyrid h-2-y1 0 F-0030 H H H H H 6-F-pyrid h-2-y1 0 F-0031 H H H H H 3-C I-pyridin-2-yl 0 F-0032 H H H H H 4-C I-pyridin-2-yl 0 F-0033 H H H H H 5-C Ipyridin-2-yl 0 F-0034 H H H H H 6-C I-pyrdin-2-yl 0 F-0035 H H H H H 3-M e-pyrid h-2-y1 0 F-0036 H H H H H 4-Me-pyrd h-2-yl 0 F-0037 H H H H H 5-M e-pyrd h-2-y1 0 F-0038 H H H H H 6-M e-pyrid h-2-y1 0 F-0039 H H H H H 3-CF 3 -pyrd in-2-y I 0 F-0040 H H H H H 4-CF 3 -pyrd n-2-y1 0 F-0041 H H H H H 5-CF 3-pyrd n-2-y1 0 F-0042 H H H H H 6-CF 3 -pyrd in-2-y1 0 F-0043 H H H H H 3-0M e-pyrd i-2-y1 0 F-0044 H H H H H 4-0M e-pyrd i-2-y1 0 F-0045 H H H H H 5-0M e-pyrid -2-y1 0 F-0046 H H H H H 6-0M e-pyrid -2-y1 0 F-0047 H H H H H 3,4-F 2-Pyrid i-2-y1 0 F-0048 H H H H H 3,5-F 2-pyrid h-2-y1 0 F-0049 H H H H H 3,6-F 2-pyrid i-2-y1 0 F-0050 H H H H H 3,4-C -pyrid n-2-yl 0 F-0051 H H H H H 3,5-C -pyrd h-2-yl 0 F-0052 H H H H H 3,6-C -pyrid i-2-yl C
[0423]
[Table 298]
com pound R' R2 R R4 R p F-0053 H H H H H 3-F-4-Cl-pyridin-2-yl 0 F-0054 H H H H H 3-F-5-Cl-pyridin-2-yl 0 F-0055 H H H H H 3-F-6-Cl-pyridin-2-yl 0 F-0056 H H H H H 3-F-4-Me-pyridin-2-y 0 F-0057 H H H H H 3-F-b-Me-pyridin-2-y 0 F-0058 H H H H H 3-F-6-Me-pyridin-2-y 0 F-0059 H H H H H 3-F-4-0Me-pyridin-2-yI 0 F-0060 H H H H H 3-F-5-0Me-pyridin-2-yI 0 F-0061 H H H H H 3-F-6-0Me-pyridin-2-yI 0 F-0062 H H H H H 3-CI-4-F-pyridin-2-yI 0 F-0063 H H H H H 3-CI-5-F-pyridin-2-y 0 F-0064 H H H H H 3-CI-6-F-pyridin-2-yI 0 F-0065 H H H H H 3-CI-4-Me-pyridin-2-y 0 F-0066 H H H H H 3-CI-5-Me-pyridin-2-y 0 F-0067 H H H H H 3-CI-6-Me-pyridin-2-y 0 F-0068 H H H H H 3 -M e-4-F-pyridin-2-yI 0 F-0069 H H H H H 3 -M e-5-F-pyridin-2-yI 0 F-0070 H H H H H 3 -M e-6-F-pyridin-2-yI 0 F-0071 H H H H H 3-Me-4-Cl-pyridin-2-y 0 F-0072 H H H H H 3-Me-5-Cl-pyridin-2-y 0 F-0073 H H H H H 3-Me-6-Cl-pyridin-2-y 0 F-0074 H H H H H 3,4-(Me) 2-pyridin-2-y 0 F-0075 H H H H H 3,5-(Me) 2-pyridin-2-y 0 F-0076 H H H H H 3,6-(Me) 2-pyridin-2-yl 0 F-0077 H H H H H 3-M e-4-0Me-pyridin-2-yI 0 F-0078 H H H H H 3-M e-5-0Me-pyridin-2-yI 0 F-0079 H H H H H 3-M e-6-0Me-pyridin-2-yI 0 F-0080 H H H H H 3-0F 3 -4-F-pyrdin-2-yl 0 F-0081 H H H H H 3-0F 3 -5-F-pyrdin-2-yl 0 F-0082 H H H H H 3-CF 3 -6-F-pyridin-2-y 0 F-0083 H H H H H 3-GF-4-Me-pyrdn-2-yl 0 F-0084 H H H H H 3-CF 3-b-Me-pyridh-2-y 0 F-0085 H H H H H 3-CF 3-6-Me-pyridh-2-y 0 F-0086 H H H H H 3-0Me-4-F-pyridin-2-yI 0 F-0087 H H H H H 3-0Me-5-F-pyridin-2-yI 0 F-0088 H H H H H 3-0Me-6-F-pyridin-2-yI 0 F-0089 H H H H H 3-0Me-4-CI-pyridin-2-y 0 F-0090 H H H H H 3-0Me-5-CI-pyridin-2-y 0 F-0091 H H H H H 3-0Me-6-Cl-pyridin-2-yI 0 F-0092 H H H H H 3-0Me-4-M e-pyridin-2-y 0 F-0093 H H H H H 3-0Me-5-M e-pyridin-2-y 0 F-0094 H H H H H 3-0Me-6-M e-pyridin-2-y 0 F-0095 H H H H H 3,4-(OMe) 2-pyridin-2-y 0 F-0096 H H H H H 3,b-(OMe) 2-pyridin-2-yl 0 F-0097 H H H H H 3,6-(OMe) 2-pyridin-2-y 0 F-0098 H H H H H pyridh-3-yI 0 F-0099 H H H H H 2-F-pyridin-3-y 0 F-0100 H H H H H 4-F-pyridin-3-y 0 F-0101 H H H H H 5-F-pyridin-3-y 0 F-0102 H H H H H 6-F-pyridin-3-y 0 F-0103 H H H H H 2-Cl-pyridin-3-y 0 F-0104 H H H H H 4-Cl-pyridin-3-y 0 F-0105 H H H H H 5-Cl-pyridin-3-y 0 F-0106 H H H H H 6-Cl-pyridin-3-y 0 F-0107 H H H H H 2-M e-pyridh-3-yI 0 F-0108 H H H H H 4-M e-pyridh-3-yI 0 F-0109 H H H H H b-M e-pyridh-3-yI 0
[0424]
[Table 299]
com pound R' R2 R R4 R p F-0110 H H H H H 6-M e-pyridh-3-yI 0 F-0111 H H H H H 2-CF3 -pyridin-3-y 0 F-0112 H H H H H 4-CF 3 -pyridin-3-yl 0 F-0113 H H H H H 5-CF 3 -pyridin-3-yl 0 F-0114 H H H H H 6-CF 3 -pyridin-3-yl 0 F-0115 H H H H H 2-0Me-pyridin-3-yI 0 F-0116 H H H H H 4-0Me-pyridin-3-yI 0 F-0117 H H H H H 5-0Me-pyridin-3-yI 0 F-0118 H H H H H 6-0Me-pyridin-3-yI 0 F-0119 H H H H H 2,4-F 2-pyridn-3-yl 0 F-0120 H H H H H 2,b- 2-pyrdin-3-yl 0 F-0121 H H H H H 2,6-F 2-pyridh-3-y 0 F-0122 H H H H H 4,b- 2-pyrdn-3-yl 0 F-0123 H H H H H 4,6-F 2-pyrdin-3-yl 0 F-0124 H H H H H 2,4-C -pyridin-3-yI 0 F-0125 H H H H H 2,5-C -pyridin-3-yI 0 F-0126 H H H H H 2,6-C -pyridin-3-yI 0 F-0127 H H H H H 4,5-C -pyridin-3-yl 0 F-0128 H H H H H 4,6-C -pyridin-3-yl 0 F-0129 H H H H H 2-F-4-Cl-pyridin-3-yI 0 F-0130 H H H H H 2-F-5-Cl-pyridin-3-yI 0 F-0131 H H H H H 2-F-6-Cl-pyridin-3-yI 0 F-0132 H H H H H 4-F-2-Cl-pyridin-3-yI 0 F-0133 H H H H H 4-F-5-Cl-pyridin-3-yI 0 F-0134 H H H H H 4-F-6-Cl-pyridin-3-yI 0 F-0135 H H H H H 2-F-4-M e-pyridin-3-y 0 F-0136 H H H H H 2-F-5-M e-pyridin-3-yI 0 F-0137 H H H H H 2-F-6-M e-pyridin-3-yI 0 F-0138 H H H H H 4-F-2-M e-pyridin-3-y 0 F-0139 H H H H H 4-F-5-M e-pyridin-3-y 0 F-0140 H H H H H 4-F-6-MAe-pyridin-3-yI 0 F-0141 H H H H H 2-F-4-0Me-pyridin-3-y 0 F-0142 H H H H H 2-F-5-0Me-pyridin-3-y 0 F-0143 H H H H H 2-F-6-0Me-pyridin-3-y 0 F-0144 H H H H H 4-F-2-0Me-pyridin-3-y 0 F-0145 H H H H H 4-F-5-0Me-pyridin-3-y 0 F-0146 H H H H H 4-F-6-0Me-pyridin-3-y 0 F-0147 H H H H H 2-CI-5-F-pyridin-3-yI 0 F-0148 H H H H H 2-CI-6-F-pyridin-3-y 0 F-0149 H H H H H 4-CI-5-F-pyridin-3-yI 0 F-0150 H H H H H 4-CI-6-F-pyridin-3-y 0 F-0151 H H H H H 2-CI-4-Me-pyridin-3-y 0 F-0152 H H H H H 2-C1-5-Me-pyridin-3-y 0 F-0153 H H H H H 2-CI-6-Me-pyridin-3-y 0 F-0154 H H H H H 4-CI-2-Me-pyridin-3-y 0 F-0155 H H H H H 4-C1-5-Me-pyridin-3-y 0 F-0156 H H H H H 4-CI-6-Me-pyridin-3-y 0 F-0157 H H H H H 2 -M e-5-F-pyridin-3-yI 0 F-0158 H H H H H 2 -M e-6-F-pyridin-3-yI 0 F-0159 H H H H H 4-M e-5-F-pyridin-3-yI 0 F-0160 H H H H H 4-M e-6-F-pyridin-3-yI 0 F-0161 H H H H H 2-M e-5-Cl-pyridin-3-yl 0 F-0162 H H H H H 2-M e-6-Cl-pyridin-3-y 0 F-0163 H H H H H 4-M e-5-Cl--pyridin-3-yl 0 F-0164 H H H H H 4-M e-6-Cl-pyridin-3-y 0 F-0165 H H H H H 2,4-(Me) 2-pyridin-3-y 0 F-0166 H H H H H 2,b-(Me) 2-pyridin-3-y 0
[0425]
[Table 300]
com pound R ' R2 R R4 R ' p F-0167 H H H H H 2,6-(M e) 2-pyrkdin-3-y I 0 F-0168 H H H H H 4,5-(M e) 2-pyrkdin-3-y I 0 F-0169 H H H H H 4,6-(M e) 2-pyridin-3-y I 0 F-0170 H H H H H 2-M e-4-0M e-pyrid in-3-y I 0 F-0171 H H H H H 2-M e=5-0M e-pyrd in-3-y I 0 F-0172 H H H H H 2-M e-6-0M e-pyrid in-3-y I 0 F-0173 H H H H H 4-M e-2-0M e-pyrid in-3-y I 0 F-0174 H H H H H 4-M e=5-0M e-pyrid in-3-y I 0 F-0175 H H H H H 4-M e-6-0M e-pyrid in-3-y I 0 F-0176 H H H H H 2-0F 3 -4-F-pyrd in-3-y I 0 F-0177 H H H H H 2-G0 3 -6-F-pyrd in-3-y I 0 F-0178 H H H H H 2-CF 3 -6-F-pyrd in-3-y I 0 F-0179 H H H H H 4-0F 3 -2-F-pyrd in-3-yI 0 F-0180 H H H H H 4-CF 3 -5-F-pyrd in-3-yI 0 F-0181 H H H H H 4-CF3 -6-F-pyrid in-3-yI 0 F-0182 H H H H H 2-CF 3 -4-M e-pyrd h-3-y I 0 F-0183 H H H H H 2-CF 3 -5-M e-pyrd h-3-y I 0 F-0184 H H H H H 2-C-F 3 6-M e-pyrd n-3-y I 0 F-0185 H H H H H 4-CF 3 -2-M e-pyrd n-3-y I 0 F-0186 H H H H H 4-CF-b--M e-pyrd n-3-y I 0 F-0187 H H H H H 4-CF 3 -6-M e-pyrd h-3-yI 0 F-0188 H H H H H 2-0M e-5-F-pyrid in-3-y I 0 F-0189 H H H H H 2-0M e-6-F-pyrid in-3-yI 0 F-0190 H H H H H 4-0M e5-F-pyrid in-3-yI 0 F-0191 H H H H H 4-0M e-6-F-pyrid in-3-yI 0 F-0192 H H H H H 2-0M e-4-C I-pyridin-3-y 0 F-0193 H H H H H 2-0M e-5-C I-pyridin-3-y 0 F-0194 H H H H H 2-0M e-6-C I-pyridin-3-y 0 F-0195 H H H H H 4-0M e-2-C I-pyridin-3-y 0 F-0196 H H H H H 4-0M e-5-C I-pyrdin-3-y 0 F-0197 H H H H H 4-0M e-6-C I-pyridin-3-y 0 F-0198 H H H H H 2-0M e5-M e-pyrid in-3--y I 0 F-0199 H H H H H 2-0M e-6-M e-pyrid in-3--y I 0 F-0200 H H H H H 4-0M e5-M e-pyrid in-3--y I 0 F-0201 H H H H H 4-0M e-6-M e-pyrid in-3--y I 0 F-0202 H H H H H 2,4-(OM e) 2-pyrdin-3-yI 0 F-0203 H H H H H 2,5-(0 Me)2-pyridin-3-yI 0 F-0204 H H H H H 2,6-(0 Me)2-pyridin-3-yI 0 F-0205 H H H H H 4,-(0 Me)2-pyridin-3-yI 0 F-0206 H H H H H 4,6-(0M e)2-pyridin-3-yI 0 F-0207 H H H H H pyrd h-4-y I 0 F-0208 H H H H H 2-F-pyrid in-4-y I 0 F-0209 H H H H H 3-F-pyrid in-4-y I 0 F-C210 H H H H H 2-C Fpyrdin-4-yI 0 F-0211 H H H H H 3-C -pyrid in-4-yI 0 F-0212 H H H H H 2-M e-pyrid h-4-y I 0 F-0213 H H H H H 3-M e-pyrid h-4-y I 0 F-0214 H H H H H 2-CF3 -pyrid in-4-y I 0 F-0215 H H H H H 3-CF3 -pyrid in-4-y I 0 F-0216 H H H H H 2-0 M e-pyrd in-4-y I 0 F-0217 H H H H H 3-0 M e-pyrd in-4-y I 0 F-0218 H H H H H 2,3-F 2-pyrid h-4-y I 0 F-0219 H H H H H 2,5-F 2-pyrid h-4-y I 0 F-0220 H H H H H 2,6-F 2-pyrid h-4-y I 0 F-0221 H H H H H 3,b-F 2-pyrid n-4-y I 0 F-0222 H H H H H 2,3-C -pyrkdin-4-y I 0 F-0223 H H H H H 2,5-C -pyridin-4-yI 0
[0426]
[Table 301]
com pound R' R2 R R4 R p F-0224 H H H H H 2,6-C -pyridin-4-yl 0 F-0225 H H H H H 3,5-C -pyridin-4-yl 0 F-0226 H H H H H 3-F-2-Cl-pyridin-4-yl 0 F-0227 H H H H H 3-F-5-Cl-pyridin-4-yl 0 F-0228 H H H H H 3-F-6-Cl-pyridin-4-yl 0 F-0229 H H H H H 3-F-2-Me-pyridin-4-y 0 F-0230 H H H H H 3-F-5-Me-pyridin-4-y 0 F-0231 H H H H H 3-F-6-M e-pyridin-4-yI 0 F-0232 H H H H H 3-F-2-0Me-pyridin-4-yI 0 F-0233 H H H H H 3-F-5-0Me-pyridin-4-yI 0 F-0234 H H H H H 3-F-6-0Me-pyridin-4-yI 0 F-0235 H H H H H 3-CI-2-F-pyridin-4-y 0 F-0236 H H H H H 3-CI-6-F-pyridin-4-y 0 F-0237 H H H H H 3-CI-2-Me-pyridin-4-y 0 F-0238 H H H H H 3-CI-5-Me-pyridin-4-y 0 F-0239 H H H H H 3-CI-6-Me-pyridin-4-y 0 F-0240 H H H H H 3-M e-2-F-pyridin-4-yI 0 F-0241 H H H H H 3-M e-6-F-pyridin-4-yI 0 F-0242 H H H H H 3-Me-2-Cl-pyridin-4-y 0 F-0243 H H H H H 3-Me-6-Cl-pyridin-4-y 0 F-0244 H H H H H 2,3-(Me) 2-pyridin-4-y 0 F-0245 H H H H H 3,5-(Me) 2-pyridin-4-y 0 F-0246 H H H H H 3,6-(Me) 2-pyridin-4-y 0 F-0247 H H H H H 3-M e-2-0Me-pyridin-4-yI 0 F-0248 H H H H H 3-M e-5-0Me-pyridin-4-yI 0 F-0249 H H H H H 3-M e-6-0Me-pyridin-4-yI 0 F-0250 H H H H H 3-CF 3 -2-F-pyridin-4-yI 0 F-0251 H H H H H 3-GF 3-b-F-pyrdin-4-yl 0 F-0252 H H H H H 3-CF 3-6-F-pyrdin-4-yl 0 F-0253 H H H H H 3-CF 3-2-Me-pyridh-4-y 0 F-0254 H H H H H 3-F-b-Me-pyrdn-4-yl 0 F-0255 H H H H H 3-CF 3-6-Me-pyridh-4-yI 0 F-0256 H H H H H 3-0Me-2-F-pyridin-4-yI 0 F-0257 H H H H H 3-0Me-6-F-pyridin-4-yI 0 F-0258 H H H H H 3-OMe-2-CI-pyridin-4-yl 0 F-0259 H H H H H 3-OMe-5-CI-pyridin-4-yl 0 F-0260 H H H H H 3-OMe-6-CI-pyridin-4-yl 0 F-0261 H H H H H 3-0Me-2-M e-pyridin-4-yI 0 F-0262 H H H H H 3-0Me-6-M e-pyridin-4-yI 0 F-0263 H H H H H 2,3-(OMe) 2-pyrdin-4-yl 0 F-0264 H H H H H 3,5-(OMe) 2-pyridin-4-y 0 F-0265 H H H H H 3,6-(OMe) 2-pyrdin-4-yl 0 F-0266 H H H H H pyrin idin-2-yl 0 F-0267 H H H H H pyrin idin-4-yl 0 F-0268 H H H H H 5-F-pyrin idin-4-yl 0 F-0269 H H H H H 5-Me-pyrin idin-4-yl 0 F-0270 H H H H H 5-CF 3-pyrin idin-4-yl 0 F-0271 H H H H H 5-OMe-pyrin idin-4-yl 0 F-0272 H H H H H pyrin idin-5-yl 0 F-0273 H H H H H 4-F-pyrin idin-5-yl 0 F-0274 H H H H H 4-Cl-pyrin i-5-yI 0 F-0275 H H H H H 4-Me-pyrmiin -5-y 0 F-0276 H H H H H 4-CF 3-pyrin idin-5-yl 0 F-0277 H H H H H 4-OMe-pyrin idin-5-yl 0 F-0278 H H H H H pyridazin-3-yl 0 F-0279 H H H H H 4-F-pyridazin-3-yl 0 F-0280 H H H H H 4-Cl-pyridazn-3-y 0
[0427]
[Table 302]
com pound R ' R2 R R4 R p F-0281 H H H H H 4-Me-pyridazin-3-yI 0 F-0282 H H H H H 4-CF 3-pyridazh-3-yl 0 F-0283 H H H H H 4-OMe-pyridazin-3-y 0 F-0284 H H H H H pyridazin-4-yl 0 F-0285 H H H H H 3-F-pyridazin-4-yl 0 F-0286 H H H H H 3-Cl-pyridazh-4-yI 0 F-0287 H H H H H 3-Me-pyridazin-4-yI 0 F-0288 H H H H H 3-CF 3-pyridazh-4-yl 0 F-0289 H H H H H 3-OMe-pyridazin-4-y 0 F-0290 H H H H H 5-F-pyridazin-4-yl 0 F-0291 H H H H H 5-Cl-pyridazh-4-y 0 F-0292 H H H H H 5-Me-pyridazin-4-yI 0 F-0293 H H H H H b-0F 3-pyrdiazn-4-yl 0 F-0294 H H H H H b-OMe-pyridazin-4-y 0 F-0295 H H H H H thiophen-2-yI 0 F-0296 H H H H H 3-F-thiophen-2-yI 0 F-0297 H H H H H 3-Cl-thiophen-2-yI 0 F-0298 H H H H H 3-Me-thiophen-2-y 0 F-0299 H H H H H 3-0F 3-thiophen-2-yl 0 F-0300 H H H H H 3-0Me-thiophen-2-yI 0 F-0301 H H H H H thiophen-3-yI 0 F-0302 H H H H H 2-F-thiophen-3-yI 0 F-0303 H H H H H 2-Cl-thiophen-3-yI 0 F-0304 H H H H H 2-Me-thiophen-3-y 0 F-0305 H H H H H 2-CF 3-thiophen-3-yI 0 F-0306 H H H H H 2-0Me-thiophen-3-yI 0 F-0307 H H H H H 4-F-thiophen-3-yI 0 F-0308 H H H H H 4-Cl-thiophen-3-yI 0 F-0309 H H H H H 4-Me-thiophen-3-y 0 F-0310 H H H H H 4-CF 3-thiophen-3-y 0 F-0311 H H H H H 4-0Me-thiophen-3-yI 0 F-0312 H H H H H thiazol-2-y 0 F-0313 H H H H H thiazol-4-yI 0 F-0314 H H H H H 5-F-th iazo I-4-y I 0 F-0315 H H H H H 5-MAe-thiazol-4-y 0 F-0316 H H H H H 5-CF 3-thibzol-4-yI 0 F-0317 H H H H H b-OMe-thiazol-4-yI 0 F-0318 H H H H H thiazol-5-yI 0 F-0319 H H H H H 4-F-thiazol-5-y 0 F-0320 H H H H H 4-M e-thiazol-5-y 0 F-0321 H H H H H 4-CF 3 -thbzol-5-y 0 F-0322 H H H H H 4-0Me-thiazol-b-y 0 F-0323 H H H H H 1 H-pyrrol-1-yI 0 F-0324 H H H H H 2-F-1 H-pyrrol-1-y 0 F-0325 H H H H H 2-M e-1 H-pyrrol-1-y 0 F-0326 H H H H H 2-F 3-1H-pyrrol-1-yl 0 F-0327 H H H H H 2-0Me-1 H-pyrrol-1-y 0 F-0328 H H H H H 1 H-pyrrol-2-yI 0 F-0329 H H H H H 1-MAe-1 H-pyrrol-2-yI 0 F-0330 H H H H H 3-F-1H-pyrrol-2-y 0 F-0331 H H H H H 3-M e-1 H-pyrrol-2-y 0 F-0332 H H H H H 3-CF-i1H-pyrrol-2-y 0 F-0333 H H H H H 3-0Me-1H-pyrrol-2-y 0 F-0334 H H H H H 1-MAe-3-F-1H-pyrrol-2-y 0 F-0335 H H H H H i,3-(Me)2 -1H-pyrrol-2-yl 0 F-0336 H H H H H 1-MAe-3-CF 3 -1H-pyrrol-2-y 0 F-0337 H H H H H I-Me-3-0Me-1H-pyrrol-2-yl 0
[0428]
[Table 303]
com pound R' R2 R R4 R p F-0338 H H H H H 1H-pyrrol-3-yl 0 F-0339 H H H H H 1-M e-1H-pyrrol-3-yl 0 F-0340 H H H H H 2-F-1H-pyrrol-3-yl 0 F-0341 H H H H H 2-M e-1H-pyrrol-3-yl 0 F-0342 H H H H H 2-0F-i1H-pyrrol-3-yl 0 F-0343 H H H H H 2-OMe-1H-pyrrol-3-yl 0 F-0344 H H H H H 1-M e-2-F-1H-pyrrol-3-yl 0 F-0345 H H H H H 1,2-(Me) 2 -1H-pyrrol-3-yl 0 F-0346 H H H H H 1-Me-2-CF 3-1H-pyrrol-3-yl 0 F-0347 H H H H H 1-M e-2-OMe-1H-pyrrol-3-yl 0 F-0348 H H H H H 4-F-1H-pyrrol-3-yl 0 F-0349 H H H H H 4-M e-1H-pyrrol-3-yl 0 F-0350 H H H H H 4-0%-i1H-pyrrol-3-yl 0 F-0351 H H H H H 4-OMe-1H-pyrrol-3-yl 0 F-0352 H H H H H 1-M e-4-F-1H-pyrrol-3-yl 0 F-0353 H H H H H 1,4-(Me) 2 -1H-pyrrol-3-yl 0 F-0354 H H H H H 1-Me-4-CF 3-1H-pyrrol-3-yl 0 F-0355 H H H H H 1-M e-4-OMe-1H-pyrrol-3-yl 0 F-0356 H H H H H 1H-pyrazol--yI 0 F-0357 H H H H H 5-F-1H-pyrazol-1-yI 0 F-0358 H H H H H 5-Ci1H-pyrazol-1-y 0 F-0359 H H H H H 5-M e-1H-pyrazol-1-y 0 F-0360 H H H H H 5-C-1H-pyrazol--yl 0 F-0361 H H H H H 5-0Me-1H-pyrazol-1-yl 0 F-0362 H H H H H 1H-pyrazol-3-yI 0 F-0363 H H H H H 1-M e-1H-pyrazol-3-yl 0 F-0364 H H H H H 4-F-1H-pyrazol-3-y 0 F-0365 H H H H H 4-Ci1H-pyrazol-3-yl 0 F-0366 H H H H H 4-M e-1H-pyrazol-3-yl 0 F-0367 H H H H H 4-CF3-1H-pyrazol-3-yI 0 F-0368 H H H H H 4-0Me-1H-pyrazol-3-yI 0 F-0369 H H H H H 1-Me-4-F-1H-pyrazol-3-yI 0 F-0370 H H H H H 1-M e-4-Ci1H-pyrazol-3-yl 0 F-0371 H H H H H 1,4-(Me) 2-1H-pyrazol-3-yl 0 F-0372 H H H H H 1-Me-4-CF 3 -1H-pyrazol-3-y 0 F-0373 H H H H H 1-M e-4-0Me-1H-pyrazol-3-yl 0 F-0374 H H H H H 1H-pyrazol-4-yI 0 F-0375 H H H H H 1-M e-1H-pyrazol-4-yl 0 F-0376 H H H H H 3-F-1H-pyrazol-4-yl 0 F-0377 H H H H H 3-Ci1H-pyrazol-4-yl 0 F-0378 H H H H H 3-M e-1H-pyrazol-4-yl 0 F-0379 H H H H H 3-0%-1H-pyrazol-4-yI 0 F-0380 H H H H H 3-0Me-1H-pyrazol-4-y 0 F-0381 H H H H H 1-Me-3-F-1H-pyrazol-4-yI 0 F-0382 H H H H H 1-Me-3-CFi1H-pyrazol-4-y 0 F-0383 H H H H H 1,3-(Me) 2-1H-pyrazol-4-y 0 F-0384 H H H H H 1-Me-3-CF 3 -1H-pyrazo1-4--y 0 F-0385 H H H H H 1-M e-3-0Me-1H-pyrazol-4-yl 0 F-0386 H H H H H 5-F-1H-pyrazol-4-yl 0 F-0387 H H H H H 5-Ci1H-pyrazol-4-yl 0 F-0388 H H H H H 5-M e-1H-pyrazol-4-yl 0 F-0389 H H H H H 5-CF-1H-pyrazol-4-yI 0 F-0390 H H H H H 5-0Me-1H-pyrazol-4-yI 0 F-0391 H H H H H 1-Me-5-F-1H-pyrazol-4-yI 0 F-0392 H H H H H 1-M e-5-Ci1H-pyrazol-4-yl 0 F-0393 H H H H H 1,5-(Me) 2-1H-pyrazol-4-yl 0 F-0394 H H H H H I -M e-b-GF 3 -/1H-pyrazol-4-y 0
[0429]
[Table 304]
com pound R' R2 R R4 R p F-0395 H H H H H 1-M e-5-0Me-1H-pyrazol-4-y 0 F-0396 H H H H H 1H-pyrazol-5-y 0 F-0397 H H H H H 1-M e-1H-pyrazol-5-y 0 F-0398 H H H H H 4-F-1H-pyrazol-5-y 0 F-0399 H H H H H 4-CI1H-pyrazol-5-y 0 F-0400 H H H H H 4-M e-1H-pyrazol-5-y 0 F-0401 H H H H H 4-CF-1H-pyrazol-5-yI 0 F-0402 H H H H H 4-0Me-1 H-pyrazol-5-yI 0 F-0403 H H H H H 1-Me-4-F-1/H-pyrazo1-5-yI 0 F-0404 H H H H H 1-M e-4-CI1HH-pyrazol-5-yI 0 F-0405 H H H H H 1,4-(Me) 2 -1 H-pyrazol-5-yl 0 F-0406 H H H H H 1-Me-4-CF 3 -1 H-pyrazoI-5-yI 0 F-0407 H H H H H 1-M e-4-0Me-1H-pyrazol-5-y 0 F-0408 H H H H H furan-2-yI 0 F-0409 H H H H H 3-F-furan-2-y I 0 F-0410 H H H H H 3-Me-furan-2-yI 0 F-0411 H H H H H 3-CF 3 -furan-2-yI 0 F-0412 H H H H H 3-OMe-furan-2-yI 0 F-0413 H H H H H furan-3-yl 0 F-0414 H H H H H 2-F-furan-3-y I 0 F-0415 H H H H H 2-Me-furan-3-yI 0 F-0416 H H H H H 2-CF 3 -furan-3-yI 0 F-0417 H H H H H 2-OMe-furan-3-yI 0 F-0418 H H H H H 4-F-furan-3-yI 0 F-0419 H H H H H 4-M e-furan-3-yI 0 F-0420 H H H H H 4-CF 3 -furan-3-yI 0 F-0421 H H H H H 4-0Me-fu ran-3-yI 0 F-0422 H H H H H isoxazol-3-yI 0 F-0423 H H H H H 4-F-isoxazol-3-yI 0 F-0424 H H H H H 4-Me-isoxazol-3-yI 0 F-0425 H H H H H 4-CF 3 -soxazol-3-yl 0 F-0426 H H H H H 4-0Me-isoxazol-3-yI 0 F-0427 H H H H H isoxazol-4-yI 0 F-0428 H H H H H 5-F-isoxazol-4-yI 0 F-0429 H H H H H 5-Me-isoxazol-4-yI 0 F-0430 H H H H H 5-CF3 -isoxazol-4-yI 0 F-0431 H H H H H b-OMe-isoxazol-4-yI 0 F-0432 H H H H H isoxazol-5-yI 0 F-0433 H H H H H 4-F-isoxazol-5-yI 0 F-0434 H H H H H 4-Me-isoxazol-5-yI 0 F-0435 H H H H H 4-CF 3 -isoxazol-5-yI 0 F-0436 H H H H H 4-0Me-isoxazol-5-yI 0 F-0437 H H H H H 1 H-1,2,3-triazol1-y 0 F-0438 H H H H H 5-F-1 H-1,2,3-triazol-1-y 0 F-0439 H H H H H 5-M e-1 H-1,2,3-triazol-1-yl 0 F-0440 H H H H H -1-1H -1,2,3-triazol-1-yl 0 F-0441 H H H H H 5-0Me-1iH-12,3-triazol--y 0 F-0442 H H H H H 1H-1,2,3-triazol-4-y 0 F-0443 H H H H H 5-F-1H-1,2,3-triazol-4-y 0 F-0444 H H H H H 5-Me-1H-1,2,3-triazo-4-y 0 F-0445 H H H H H 5-CF-1H-1,2,3-triazo1-4-yI 0 F-0446 H H H H H 5-0Me-1iH-12,3-triazol-4-y 0 F-0447 H H H H H 1H-12,3-triazol-5-y 0 F-0448 H H H H H 4-F-1H-1,2,3-triazo-5-yl 0 F-0449 H H H H H 4-Me-1H-1,2,3-triazol-5-y 0 F-0450 H H H H H 4-CF3-1H-1,2,3-triazo-b-yl 0 F-045i H H H H H 4-OMe-1H-1,2,3-triazol-b-yI 0
[0430]
[Table 305] cornpound R1 wR wRrR 4 p F-0452 H H H H H i1H-1,2,4-triazoki-yI 0 F-0453 H H H H H 5 -M e-i1H-12,4-tr ia zo H-yI1 0 F-0454 H H H H H 5-F-i1H-i,2,4-triazol-1-yl 0 F-0455 H H H H H 5-0%,-i/-,2,4-triazoI-v-I 0 F-0456 H H H H H 5-OM e-1-1,2,4-triazoki-yI 0 F-0457 H H H H H i1H-1,2,4-triazok 3-yI 0 F-0458 H H H H H 1i-M e-i1H-1,2,4tr ia zo 3 -yI1 0 F-0459 H H H H H i1H-1,2,4-triazo -5-yI 0 F-0460 H H H H H 1i-M e-i1H-1,2,4tr ia zo -5-yI1 0 F-0461 H H H H H 3,5-(M e) 2 iSoXaZok4-yI 0 F-0462 H H H H H 3,5-(Et)2 -ESoxaZoF-4-yI1 0 F-0463 H H H H H quhino lin-4-yI1 0 F-0464 H H H H H isoq uin olin -4-yI1 0 F-0 4 65 H H H H H 3, 6- (OMe) 2 -Py rid azin-4-yI1 0 F-0 4 66 H H H H H 2,4 -(UM e) 2-p yrmidin -5 -yI1 0
[0431]
[Table 306]
2 0 R3 R
N O 1 (O R, cornpound R1 WR Rj R4 R5 F-5001 H H H H H cI1 1 F-5002 H H H H H Br 1 F-5003 H H H H H 1 1 F-5004 H H H H H OS(=O) 2 M e 1 F-5005 H H H H H OS (=O) 2 CF, 1 F-5006 H H H H H OS (=U) 2 CF 2CF, 1 F-5007 H H H H H OS (=O) 2 CF2 CF 2CF, 1 F-5008 H H H H H 06S(=O) 2CF 2 UF 2 UF2 (CF 3 1 F-5009 H H H H H S(= 0)2 (4-MePh) 1 F-5 010 H H H H H 0 S 0 ) 2N (Me) 2 1 F-5b011 H H H H H 0 S 0) 2 N (Et) 2 1 F-501 2 H H H H H naphtha len-1-yI1 1 F-501 3 H H H H H 2-F-naphtha len-1-yI1 1 F-5b014 H H H H H 2-M e-naphtha len-1-yI1 1 F-501l5 H H H H H 2-CF 3 -naphtha ln-1-y 1 1 F-501 6 H H H H H 2-OM e-naphtia len-1-yI1 1 F-b01l7 H H H H H naphthalIen-2-yI1 1 F-501 8 H H H H H 1 -F-naphthalIen-2-yI1 1 F-501 9 H H H H H 1lA e-naphthalIen-2-yI1 1 F-5020 H H H H H 1l-CF 3 -naphttia In-2-yI1 1 F-5021 H H H H H 1 -0M e-naphthalIen-2-yI1 1 F-5022 H H H H H 3-F-naphttialen-2-yI1 1 F-5023 H H H H H 3-M1e-naphliia In-2-yI1 1 F-5024 H H H H H 3-CF 3 -naphtha In-2-yI1 1 F-5025 H H H H H 3-OM e-naphtiialen-2-yI1 1 F-5026 H H H H H pyri i-2-yI1 1 F-5027 H H H H H 3-F-pyrkid -2-yI1 1 F-5028 H H H H H 4-F-pyrid h-2-yI1 1 F-5029 H H H H H 5-F-pyrkid -2-yI1 1 F-5030 H H H H H 6-F-pyri -2-yI1 1 F-5031 H H H H H 3 C I--pyrid in-2-yI1 1 F-5032 H H H H H 4 C I-pyr~idin-2-yI1 1 F-5033 H H H H H 5-CI-pyriin-2-yI1 1 F-5034 H H H H H 6 C I-pyriin-2-yI1 1 F-5035 H H H H H 3-M e-pyri -2-yI1 1 F-5036 H H H H H 4-M e-pyrid i-2-yI1 1 F-5037 H H H H H 5-M e-pyrid i-2-yI1 1 F-5038 H H H H H 6-M e-pyri -2-yI1 1 F-5039 H H H H H 3-CF 3-Pyid in-2-y 1 1 F-5040 H H H H H 4-0CF 3 -pyrid n-2-yI1 1 F-5041 H H H H H 5-CF 3 -Pyrid n-2-y 1 1 F-5042 H H H H H 6--CF 3-Pyid in-2-yI1 1 F-5043 H H H H H 3-0 Me-pyrid in-2-yI1 1 F-5044 H H H H H 4-0 Me-pyrid in-2-yI1 1 F-5045 H H H H H 5 --OMe-py r idii-2-yI1 1 F-5b0 46 H H H H H 6 --OMe-p y r iii-2-yI1 1 F-5 0 47 H H H H H 3A4-+ 2 -P yrrii-2-y 1 1 F-5 048 H H H H H 3,5-F 2 -Pyri -2-y 1 1 F-5049 H H H H H 3,6-F 2 -Pyri i-2-y 1 1 F-5050 H H H H H 3,4-C -pyri -2-yI1 1 F-5051 H H H H H 3,5-C -pyridii-2-yI1 1 F-5052 H H H H H 3,6-C -pyriduii-2-y I1
[0432]
[Table 307]
com pound R' R2 R R4 R p F-5053 H H H H H 3-F-4-Cl-pyridin-2-yl 1 F-5054 H H H H H 3-F-5-Cl-pyridin-2-yl 1 F-5055 H H H H H 3-F-6-Cl-pyridin-2-yl 1 F-5056 H H H H H 3-F-4-M e-pyridin-2-yI 1 F-5057 H H H H H 3-F-b-M e-pyridin-2-y 1 F-5058 H H H H H 3-F-6-M e-pyridin-2-y 1 F-5059 H H H H H 3-F-4-0Me-pyridin-2-y 1 F-5060 H H H H H 3-F-5-0Me-pyridin-2-y 1 F-5061 H H H H H 3-F-6-0Me-pyridin-2-y 1 F-5062 H H H H H 3-CI-4-F-pyridin-2-yI 1 F-5063 H H H H H 3-CI-5-F-pyridin-2-yI 1 F-5064 H H H H H 3-CI-6-F-pyridin-2-yI 1 F-5065 H H H H H 3-CI-4-Me-pyridin-2-y 1 F-5066 H H H H H 3-C-5-Me-pyridin-2-y 1 F-5067 H H H H H 3-CI-6-Me-pyridin-2-y 1 F-5068 H H H H H 3 -M e-4-F-pyridin-2-y 1 F-5069 H H H H H 3 -M e-5-F-pyridin-2-y 1 F-5070 H H H H H 3 -M e-6-F-pyridin-2-yI 1 F-5071 H H H H H 3-M e-4-Cl-pyridin-2-y 1 F-5072 H H H H H 3-M e-5-Cl-pyridin-2-yl 1 F-5073 H H H H H 3-M e-6-Cl-pyridin-2-y 1 F-5074 H H H H H 3,4-(Me) 2-pyridin-2-y 1 F-5075 H H H H H 3,5-(Me) 2-pyridin-2-y 1 F-5076 H H H H H 3,6-(Me) 2-pyridin-2-yl 1 F-5077 H H H H H 3-M e-4-0Me-pyridin-2-y 1 F-5078 H H H H H 3-M e-5-0Me-pyridin-2-y 1 F-5079 H H H H H 3-M e-6-0Me-pyridin-2-y 1 F-5080 H H H H H 3-0F 3 -4-F-pyrdin-2-yl 1 F-5081 H H H H H 3-0F 3 -5-F-pyrdin-2-yl 1 F-5082 H H H H H 3-CF 3 -6-F-pyridin-2-yI 1 F-5083 H H H H H 3-GF-4-Me-pyrdn-2-yl 1 F-5084 H H H H H 3-CF 3-b-Me-pyridh-2-y 1 F-5085 H H H H H 3-CF 3-6-Me-pyridh-2-y 1 F-5086 H H H H H 3-0Me-4-F-pyridin-2-yI 1 F-5087 H H H H H 3-0Me-5-F-pyridin-2-yI 1 F-5088 H H H H H 3-0Me-6-F-pyridin-2-yI 1 F-5089 H H H H H 3-0Me-4-CI-pyridin-2-y 1 F-5090 H H H H H 3-0Me-5-CI-pyridin-2-y 1 F-5091 H H H H H 3-0Me-6-CI-pyridin-2-y 1 F-5092 H H H H H 3-0Me-4-M e-pyridin-2-y 1 F-5093 H H H H H 3-0Me-5-M e-pyridin-2-y 1 F-5094 H H H H H 3-0Me-6-M e-pyridin-2-y 1 F-5095 H H H H H 3,4-(OMe) 2-pyridin-2-y 1 F-5096 H H H H H 3,b-(OMe) 2-pyridin-2-yl 1 F-5097 H H H H H 3,6-(OMe) 2-pyridin-2-y 1 F-5098 H H H H H pyridh-3-yI 1 F-5099 H H H H H 2-F-pyridin-3-y 1 F-5100 H H H H H 4-F-pyridin-3-y 1 F-5101 H H H H H 5-F-pyridin-3-y 1 F-5102 H H H H H 6-F-pyridin-3-yI 1 F-5103 H H H H H 2-Cl-pyridin-3-y 1 F-5104 H H H H H 4-Cl-pyridin-3-y 1 F-5105 H H H H H 5-Cl-pyridin-3-y 1 F-5106 H H H H H 6-Cl-pyridin-3-y 1 F-5107 H H H H H 2-M e-pyridh-3-yI 1 F-5108 H H H H H 4-M e-pyridh-3-yI 1 F-5109 H H H H H b-M e-pyridh-3-yI 1
[0433]
[Table 308]
com pound R' R2 R R4 R p F-5110 H H H H H 6-M e-pyridh-3-yI 1 F-5111 H H H H H 2-CF3 -pyridin-3-y 1 F-5112 H H H H H 4-CF 3 -pyridin-3-yl 1 F-5113 H H H H H 5-CF 3 -pyridin-3-yl 1 F-5114 H H H H H 6-CF 3 -pyridin-3-yl 1 F-5115 H H H H H 2-0Me-pyridin-3-yI 1 F-5116 H H H H H 4-0Me-pyridin-3-yI 1 F-5117 H H H H H 5-0Me-pyridin-3-yI 1 F-5118 H H H H H 6-0Me-pyridin-3-yI 1 F-5119 H H H H H 2,4-F 2-pyridn-3-yl 1 F-5120 H H H H H 2,b- 2-pyrdin-3-yl 1 F-5121 H H H H H 2,6-F 2-pyridh-3-y 1 F-5122 H H H H H 4,b- 2-pyrd n-3-yl 1 F-5123 H H H H H 4,6-F 2-pyrdin-3-yl 1 F-5124 H H H H H 2,4-C -pyridin-3-yl 1 F-5125 H H H H H 2,5-C -pyridin-3-yI 1 F-5126 H H H H H 2,6-C -pyridin-3-yI 1 F-5127 H H H H H 4,5-C -pyridin-3-yl 1 F-5128 H H H H H 4,6-C -pyridin-3-yl 1 F-5129 H H H H H 2-F-4-Cl-pyridin-3-yI 1 F-5130 H H H H H 2-F-5-Cl-pyridin-3-yI 1 F-5131 H H H H H 2-F-6-Cl-pyridin-3-yI 1 F-5132 H H H H H 4-F-2-Cl-pyridin-3-yI 1 F-5133 H H H H H 4-F-5-Cl-pyridin-3-yI 1 F-5134 H H H H H 4-F-6-Cl-pyridin-3-yI 1 F-5135 H H H H H 2-F-4-M e-pyridin-3-yI 1 F-5136 H H H H H 2-F-5-M e-pyridin-3-yI 1 F-5137 H H H H H 2-F-6-M e-pyridin-3-yI 1 F-5138 H H H H H 4-F-2-M e-pyridin-3-yI 1 F-5139 H H H H H 4-F-5-M e-pyridin-3-yI 1 F-5140 H H H H H 4-F-6-MAe-pyridin-3-yI 1 F-5141 H H H H H 2-F-4-0Me-pyridin-3-y 1 F-5142 H H H H H 2-F-5-0Me-pyridin-3-y 1 F-5143 H H H H H 2-F-6-0Me-pyridin-3-y 1 F-5144 H H H H H 4-F-2-0Me-pyridin-3-y 1 F-5145 H H H H H 4-F-5-0Me-pyridin-3-y 1 F-5146 H H H H H 4-F-6-0Me-pyridin-3-y 1 F-5147 H H H H H 2-CI-5-F-pyridin-3-yI 1 F-5148 H H H H H 2-CI-6-F-pyridin-3-y 1 F-5149 H H H H H 4-CI-5-F-pyridin-3-yI 1 F-5150 H H H H H 4-CI-6-F-pyridin-3-y 1 F-5151 H H H H H 2-CI-4-Me-pyridin-3-y 1 F-5152 H H H H H 2-C1-5-Me-pyridin-3-y 1 F-5153 H H H H H 2-CI-6-Me-pyridin-3-y 1 F-5154 H H H H H 4-CI-2-Me-pyridin-3-y 1 F-5155 H H H H H 4-C1-5-Me-pyridin-3-y 1 F-5156 H H H H H 4-CI-6-Me-pyridin-3-y 1 F-5157 H H H H H 2-Me-5-F-pyridin-3-y F-5158 H H H H H 2-M e-6-F-pyridin-3-yI 1 F-5159 H H H H H 4-M e-5-F-pyridin-3-yI 1 F-5160 H H H H H 4-M e-6-F-pyridin-3-yI 1 F-5161 H H H H H 2-M e-5-Cl-pyridin-3-y 1 F-5162 H H H H H 2-M e-6-Cl-pyridin-3-y 1 F-5163 H H H H H 4-M e-5-Cl-pyridin-3-y 1 F-5164 H H H H H 4-M e-6-Cl-pyridin-3-y 1 F-5165 H H H H H 2,4-(Me) 2-pyridin-3-yl 1 F-5166 H H H H H 2,b-(Me) 2-pyridin-3-yl 1
[0434]
[Table 309]
com pound R' R2 R R4 R ' p F-5167 H H H H H 2,6-(M e) 2-pyridin-3-y| 1 F-5168 H H H H H 4,5-(M e) 2-pyrkdin-3-yI 1 F-5169 H H H H H 4,6-(M e) 2-pyridin-3-y| 1 F-5170 H H H H H 2-M e-4-0M e-pyrid in-3-yI 1 F-5171 H H H H H 2-M e5-0M e-pyrd in-3-yI 1 F-5172 H H H H H 2-M e-6-0M e-pyrid in-3-y 1 F-5173 H H H H H 4-M e-2-0M e-pyrid in-3-yI 1 F-5174 H H H H H 4-M e=5-0M e-pyrid in-3-yI 1 F-5175 H H H H H 4-M e-6-0M e-pyrid in-3-yI 1 F-5176 H H H H H 2-0F 3 -4-F-pyrd in-3-y| 1 F-5177 H H H H H 2-G0 3 -5-F-pyrd in-3-y| 1 F-5178 H H H H H 2-CF 3 -6-F-pyrd in-3-yI 1 F-5179 H H H H H 4-0F 3 -2-F-pyrd in-3-y| 1 F-5180 H H H H H 4-CF 3 -5-F-pyrd in-3-y| 1 F-5181 H H H H H 4-CF 3 -6-F-pyrid in-3-y 1 F-5182 H H H H H 2-CF 3 -4-M e-pyrd h-3-y 1 F-5183 H H H H H 2-CF 3 -5-M e-pyrd h-3-y 1 F-5184 H H H H H 2-C-F 3 6-M e-pyrd n-3-y| 1 F-5185 H H H H H 4-CF 3 -2-M e-pyrd n-3-y| 1 F-5186 H H H H H 4-CF 3 -b-M e-pyrd n-3-y| 1 F-5187 H H H H H 4-CF 3-6-M e-pyrd h-3-y 1 F-5188 H H H H H 2-0M e-5-F-pyrid in-3-y 1 F-5189 H H H H H 2-0M e-6-F-pyrid in-3-y 1 F-5190 H H H H H 4-0M e-5-F-pyrid in-3-y 1 F-5191 H H H H H 4-0M e-6-F-pyrid in-3-y 1 F-5192 H H H H H 2-0M e-4-C I-pyridin-3-y 1 F-5193 H H H H H 2-0M e-5-C I-pyridin-3-y 1 F-5194 H H H H H 2-0M e-6-C I-pyridin-3-y 1 F-5195 H H H H H 4-0M e-2-C I-pyridin-3-y 1 F-5196 H H H H H 4-0M e-5-C I-pyridin-3-y 1 F-5197 H H H H H 4-0M e-6-C I-pyridin-3-y 1 F-5198 H H H H H 2-0M e-5-M e-pyrid in-3-yI 1 F-5199 H H H H H 2-0M e-6-M e-pyrid in-3-yI 1 F-5200 H H H H H 4-0M e-5-M e-pyrid in-3-yI 1 F-5201 H H H H H 4-0M e-6-M e-pyrid in-3-yI 1 F-5202 H H H H H 2,4-(OM e) 2-pyrkdin-3-yI 1 F-5203 H H H H H 2,5-(0 Me) 2-pyridin-3-y| 1 F-5204 H H H H H 2,6-(0 Me) 2-pyridin-3-y| 1 F-5205 H H H H H 4,-(0 Me) 2-pyridin-3-y| 1 F-5206 H H H H H 4,6-(0M e) 2-pyridin-3-y| 1 F-5207 H H H H H pyrd h-4-yI 1 F-5208 H H H H H 2-F-pyrid in-4-y 1 F-5209 H H H H H 3-F-pyrid in-4-y 1 F-5210 H H H H H 2-Cl-pyridin-4-y 1 F-5211 H H H H H 3-C -pyrd in-4-y 1 F-5212 H H H H H 2-M e-pyrid h-4-yI 1 F-5213 H H H H H 3-M e-pyrid h-4-yI 1 F-5214 H H H H H 2-CF3 -pyrid in-4-y 1 F-5215 H H H H H 3-CF 3 -pyrid in-4-yI 1 F-5216 H H H H H 2-0 M e-pyrd in-4-yI 1 F-5217 H H H H H 3-0 M e-pyrd in-4-yI 1 F-5218 H H H H H 2,3-F 2-pyrid h-4-yI 1 F-5219 H H H H H 2,5-F 2-pyrid h-4-yI 1 F-5220 H H H H H 2,6-F 2-pyrid h-4-yI 1 F-5221 H H H H H 3,b-F 2-pyrid n-4-y| 1 F-5222 H H H H H 2,3-C -pyrkdin-4-yI 1 F-5223 H H H H H 2,5-C -pyridin-4-y 1
[0435]
[Table 310]
com pound R' R2 R R4 R p F-5224 H H H H H 2,6-C -pyridin-4-yl 1 F-5225 H H H H H 3,5-C -pyridin-4-yl 1 F-5226 H H H H H 3-F-2-Cl-pyridin-4-yl 1 F-5227 H H H H H 3-F-5-Cl-pyridin-4-yl 1 F-5228 H H H H H 3-F-6-Cl-pyridin-4-yl 1 F-5229 H H H H H 3-F-2-M e-pyridin-4-yI 1 F-5230 H H H H H 3-F-5-M e-pyridin-4-yI 1 F-5231 H H H H H 3-F-6-M e-pyridin-4-yI 1 F-5232 H H H H H 3-F-2-0Me-pyridin-4-yI 1 F-5233 H H H H H 3-F-5-0Me-pyridin-4-yI 1 F-5234 H H H H H 3-F-6-0Me-pyridin-4-yI 1 F-5235 H H H H H 3-CI-2-F-pyridin-4-y 1 F-5236 H H H H H 3-CI-6-F-pyridin-4-y 1 F-5237 H H H H H 3-CI-2-Me-pyridin-4-y 1 F-5238 H H H H H 3-CI-5-Me-pyridin-4-y 1 F-5239 H H H H H 3-CI-6-Me-pyridin-4-y 1 F-5240 H H H H H 3-M e-2-F-pyridin-4-yI 1 F-5241 H H H H H 3-M e-6-F-pyridin-4-yI 1 F-5242 H H H H H 3-Me-2-Cl-pyridin-4-y 1 F-5243 H H H H H 3-Me-6-Cl-pyridin-4-y 1 F-5244 H H H H H 2,3-(Me) 2-pyridin-4-y 1 F-5245 H H H H H 3,5-(Me) 2-pyridin-4-y 1 F-5246 H H H H H 3,6-(Me) 2-pyridin-4-y 1 F-5247 H H H H H 3-M e-2-0Me-pyridin-4-yI 1 F-5248 H H H H H 3-M e-5-0Me-pyridin-4-yI 1 F-5249 H H H H H 3-M e-6-0Me-pyridin-4-yI 1 F-5250 H H H H H 3-CF 3 -2-F-pyridin-4-y 1 F-5251 H H H H H 3-GF 3 -b-F-pyrdin-4-yl 1 F-5252 H H H H H 3-0F 3 -6-F-pyrdin-4-yl 1 F-5253 H H H H H 3-CF 3-2-Me-pyridh-4-y 1 F-5254 H H H H H 3- F-b-Me-pyrdn-4-yl 1 F-5255 H H H H H 3-CF 3-6-Me-pyridh-4-yI 1 F-5256 H H H H H 3-0Me-2-F-pyridin-4-yI 1 F-5257 H H H H H 3-0Me-6-F-pyridin-4-yI 1 F-5258 H H H H H 3-OMe-2-Cl-pyridin-4-yl 1 F-5259 H H H H H 3-OMe-5-Cl-pyridin-4-yl 1 F-5260 H H H H H 3-OMe-6-Cl-pyridin-4-yl 1 F-5261 H H H H H 3-0Me-2-M e-pyridin-4-yI 1 F-5262 H H H H H 3-0Me-6-M e-pyridin-4-yI 1 F-5263 H H H H H 2,3-(OMe) 2-pyrdin-4-yl 1 F-5264 H H H H H 3,5-(OMe) 2-pyridin-4-y 1 F-5265 H H H H H 3,6-(OMe) 2-pyrdin-4-yl 1 F-5266 H H H H H pyrimi idin-2-yl 1 F-5267 H H H H H pyrimi idin-4-yl 1 F-5268 H H H H H 5-F-pyril idin-4-yl 1 F-5269 H H H H H 5-Me-pyril idin-4-yl 1 F-5270 H H H H H 5-CF 3-pyril idin-4-yl 1 F-5271 H H H H H 5-OMe-pyrikl idin-4-yl 1 F-5272 H H H H H pyrimi idin-5-yl 1 F-5273 H H H H H 4-F-pyrikl idin-5-yl 1 F-5274 H H H H H 4-CI-pyril idn-5-yI 1 F-5275 H H H H H 4-Me-pyri idin-5-y 1 F-5276 H H H H H 4-CF 3-pyrim idin-5-yl 1 F-5277 H H H H H 4-OMe-pyrin1 idin-5-yl 1 F-5278 H H H H H pyridazin-3-yl 1 F-5279 H H H H H 4-F-pyridazin-3-yl 1 F-5280 H H H H H 4-Cl-pyridazn-3-y 1
[0436]
[Table 311]
com pound R' R2 R R4 R p F-5281 H H H H H 4-M e-pyridazin-3-yI 1 F-5282 H H H H H 4-CF 3-pyridazh-3-yl 1 F-5283 H H H H H 4-OMe-pyridazin-3-y 1 F-5284 H H H H H pyridazin-4-yl 1 F-5285 H H H H H 3-F-pyridazin-4-yl 1 F-5286 H H H H H 3-Cl-pyridazh-4-y 1 F-5287 H H H H H 3-Me-pyridazin-4-yI 1 F-5288 H H H H H 3-CF 3-pyridazh-4-yl 1 F-5289 H H H H H 3-OMe-pyridazin-4-y 1 F-5290 H H H H H 5-F-pyridazin-4-yl 1 F-5291 H H H H H 5-Cl-pyridazh-4-y 1 F-5292 H H H H H 5-Me-pyridazin-4-yI 1 F-5293 H H H H H b-0F 3-pyrdiazn-4-yl 1 F-5294 H H H H H b-OMe-pyridazin-4-y 1 F-5295 H H H H H thiophen-2-yI 1 F-5296 H H H H H 3-F-thiophen-2-yI 1 F-5297 H H H H H 3-Cl-thiophen-2-yI 1 F-5298 H H H H H 3-Me-thiophen-2-y 1 F-5299 H H H H H 3-0F3 -thiophen-2-yl 1 F-5300 H H H H H 3-0Me-thiophen-2-y 1 F-5301 H H H H H thiophen-3-y 1 F-5302 H H H H H 2-F-thiophen-3-y 1 F-5303 H H H H H 2-Cl-thiophen-3-y 1 F-5304 H H H H H 2-Me-thiophen-3-y 1 F-5305 H H H H H 2-CF 3 -thiophen-3-y 1 F-5306 H H H H H 2-0Me-thiophen-3-y 1 F-5307 H H H H H 4-F-thiophen-3-y 1 F-5308 H H H H H 4-Cl-thiophen-3-y 1 F-5309 H H H H H 4-Me-thiophen-3-y 1 F-5310 H H H H H 4-CF 3 -thiophen-3-y 1 F-5311 H H H H H 4-0Me-thiophen-3-y 1 F-5312 H H H H H thiazol-2-y 1 F-5313 H H H H H thiazol-4-y 1 F-5314 H H H H H 5-F-thiazol-4-y 1 F-5315 H H H H H 5-MAe-thiazol-4-y 1 F-5316 H H H H H 5-CF3 -thibzol-4-y 1 F-5317 H H H H H b-OMe-thiazol-4-y 1 F-5318 H H H H H thiazol-5-y 1 F-5319 H H H H H 4-F-thiazol-5-y 1 F-5320 H H H H H 4-M e-thiazol-5-y 1 F-5321 H H H H H 4-CF 3 -thibzol-5-y 1 F-5322 H H H H H 4-0Me-thiazol-b-y 1 F-5323 H H H H H 1H-pyrrol1-yI 1 F-5324 H H H H H 2-F-1H-pyrrol1-y 1 F-5325 H H H H H 2-M e-1 H-pyrrol1-y 1 F-5326 H H H H H 2-F 3-1H-pyrrol1-yl 1 F-5327 H H H H H 2-0Me-1/H-pyrrol1-y 1 F-5328 H H H H H 1H-pyrrol-2-yI 1 F-5329 H H H H H 1-MAe-1 H-pyrrol-2-yI 1 F-5330 H H H H H 3-F-1 H-pyrrol-2-y 1 F-5331 H H H H H 3-M e-1 H-pyrrol-2-y 1 F-5332 H H H H H 3-CF 3-1H-pyrrol-2-y 1 F-5333 H H H H H 3-0Me-1/H-pyrrol-2-y 1 F-5334 H H H H H 1-MAe-3-F-1H-pyrrol-2-y 1 F-5335 H H H H H 1,3-(Me)2 -1H-pyrrol-2-yl 1 F-5336 H H H H H 1-MAe-3-CF 3-1H-pyrrol-2-y 1 F-5337 H H H H H 1-MAe-3-0Me-1H-pyrrol-2-y 1
[0437]
[Table 312]
com pound R' R2 R R4 R p F-5338 H H H H H 1H-pyrrol-3-yl 1 F-5339 H H H H H 1-M e-1H-pyrrol-3-yl 1 F-5340 H H H H H 2-F-1H-pyrrol-3-yl 1 F-5341 H H H H H 2-M e-1H-pyrrol-3-yl 1 F-5342 H H H H H 2-F 3-1H-pyrrol-3-yl 1 F-5343 H H H H H 2-OMe-1 H-pyrrol-3-yl 1 F-5344 H H H H H 1-M e-2-F-1H-pyrrol-3-yl 1 F-5345 H H H H H 1,2-(Me) 2 -1 H-pyrrol-3-yl 1 F-5346 H H H H H 1-M e-2-CF 3 -1H-pyrrol-3-yl 1 F-5347 H H H H H 1-M e-2-OMe-1 H-pyrrol-3-yl 1 F-5348 H H H H H 4-F-1H-pyrrol-3-yl 1 F-5349 H H H H H 4-M e-1H-pyrrol-3-yl 1 F-5350 H H H H H 4-F 3-1H-pyrrol-3-yl 1 F-5351 H H H H H 4-OMe-1 H-pyrrol-3-yl 1 F-5352 H H H H H 1-M e-4-F-1H-pyrrol-3-yl 1 F-5353 H H H H H 1,4-(Me) 2 -1 H-pyrrol-3-yl 1 F-5354 H H H H H 1-M e-4-CF 3 -1H-pyrrol-3-yl 1 F-5355 H H H H H 1-M e-4-OMe-1 H-pyrrol-3-yl 1 F-5356 H H H H H 1 H-pyrazol-y 1 F-5357 H H H H H 5-F-1H-pyrazol1-y 1 F-5358 H H H H H 5-C-1HH-pyrazol-1-y 1 F-5359 H H H H H 5-M e-1 H-pyrazol1-y 1 F-5360 H H H H H 5-CF3 -1H-pyrazol1-y 1 F-5361 H H H H H 5-0Me-1 H-pyrazol-1-y 1 F-5362 H H H H H 1 H-pyrazol-3-y 1 F-5363 H H H H H 1 -M e-1 H-pyrazol-3-y 1 F-5364 H H H H H 4-F-1 H-pyrazol-3-y 1 F-5365 H H H H H 4-C-1HH-pyrazol-3-y 1 F-5366 H H H H H 4-M e-1 H-pyrazol-3-y 1 F-5367 H H H H H 4-CF3 -1H-pyrazol-3-y 1 F-5368 H H H H H 4-0Me-1H-pyrazol-3-y 1 F-5369 H H H H H 1-Me-4-F-1H-pyrazol-3-y 1 F-5370 H H H H H 1-M e-4-C-1HH-pyrazol-3-y 1 F-5371 H H H H H 1,4-(Me) 2-1H-pyrazol-3-yl 1 F-5372 H H H H H 1-M e-4-CF 3-1H-pyrazol-3-y 1 F-5373 H H H H H 1 -M e-4-0Me-1 H-pyrazol-3-y 1 F-5374 H H H H H 1 H-pyrazol-4-y 1 F-5375 H H H H H 1 -M e-1 H-pyrazol-4-y 1 F-5376 H H H H H 3-F-1 H-pyrazol-4-y 1 F-5377 H H H H H 3-C-1HH-pyrazol-4-y 1 F-5378 H H H H H 3-M e-1 H-pyrazol-4-y 1 F-5379 H H H H H 3-0F3 -1H-pyrazol-4-yl 1 F-5380 H H H H H 3-0Me-1 H-pyrazol-4-y 1 F-5381 H H H H H 1-Me-3-F-1 H-pyrazol-4-y 1 F-5382 H H H H H 1 -M e-3-C-1HH-pyrazol-4-y 1 F-5383 H H H H H 1,3-(Me) 2-1H-pyrazol-4-yl 1 F-5384 H H H H H 1-M e-3-CF 3-1H-pyrazol-4-yI 1 F-5385 H H H H H 1 -M e-3-0Me-1 H-pyrazol-4-y 1 F-5386 H H H H H 5-F-1 H-pyrazol-4-y 1 F-5387 H H H H H 5-C-1HH-pyrazol-4-y 1 F-5388 H H H H H 5-M e-1 H-pyrazol-4-y 1 F-5389 H H H H H 5-CF3 -1H-pyrazol-4-y 1 F-5390 H H H H H 5-0Me-1 H-pyrazol-4-y 1 F-5391 H H H H H 1-Me-5-F-1 H-pyrazol-4-y 1 F-5392 H H H H H 1 -M e-5-C-1HH-pyrazol-4-y 1 F-5393 H H H H H 1,5-(Me) 2-1 H-pyrazol-4-yl 1 F-5394 H H H H H 1-M e-b-F 3 -1 H-pyrazol-4-yl 1
[0438]
[Table 313]
com pound R' R2 R R4 R p F-5395 H H H H H 1-M e-5-0Me-1H-pyrazol-4-y 1 F-5396 H H H H H 1H-pyrazol-5-y 1 F-5397 H H H H H 1-M e-1 H-pyrazol-5-yI 1 F-5398 H H H H H 4-F-1/H-pyrazol-5-y 1 F-5399 H H H H H 4-CI-1H-pyrazol-5-y 1 F-5400 H H H H H 4-M e-1 H-pyrazol-5-y 1 F-5401 H H H H H 4-CF3 -1H-pyrazol-5-y 1 F-5402 H H H H H 4-0Me-1 H-pyrazol-5-yI 1 F-5403 H H H H H 1-Me-4-F-1H-pyrazo1-5-y 1 F-5404 H H H H H 1-M e-4-C-1HH-pyrazol-5-y 1 F-5405 H H H H H 1,4-(Me) 2-1 H-pyrazol-b-yl 1 F-5406 H H H H H 1-Me-4-CF3 -1H-pyrazo-5-yI 1 F-5407 H H H H H 1-M e-4-0Me-1H-pyrazol-5-y 1 F-5408 H H H H H fu ran-2-yI 1 F-5409 H H H H H 3-F-furan-2-yI 1 F-5410 H H H H H 3-M e-furan-2-yI 1 F-5411 H H H H H 3-CF3-furan-2-yI 1 F-5412 H H H H H 3-OMe-furan-2-yI 1 F-5413 H H H H H furan-3-yl 1 F-5414 H H H H H 2-F-furan-3-y 1 F-5415 H H H H H 2-M e-furan-3-yI 1 F-5416 H H H H H 2-CF 3 -furan-3-yI 1 F-5417 H H H H H 2-OMe-furan-3-yI 1 F-5418 H H H H H 4-F-furan-3-y 1 F-5419 H H H H H 4-M e-furan-3-yI 1 F-5420 H H H H H 4-CF 3 -furan-3-yI 1 F-5421 H H H H H 4-0Me-fu ran-3-yI 1 F-5422 H H H H H isoxazol-3-yI 1 F-5423 H H H H H 4-F-isoxazol-3-yI 1 F-5424 H H H H H 4-Me-isoxazol-3-yI 1 F-5425 H H H H H 4-CF 3 -soxazol-3-yl 1 F-5426 H H H H H 4-0Me-isoxazol-3-y 1 F-5427 H H H H H isoxazol-4-yI 1 F-5428 H H H H H 5-F-isoxazol-4-yI 1 F-5429 H H H H H 5-Me-isoxazol-4-y 1 F-5430 H H H H H 5-CF3 -isoxazol-4-y 1 F-5431 H H H H H b-OMe-soxazo-4-y 1 F-5432 H H H H H isoxazol-5-y 1 F-5433 H H H H H 4-F-isoxazol-5-yI 1 F-5434 H H H H H 4-Me-isoxazol-5-y 1 F-5435 H H H H H 4-CF 3 -isoxazol-5-yI 1 F-5436 H H H H H 4-0Me-soxazol-b-y 1 F-5437 H H H H H 1H-1,2,3-triazol1-y 1 F-5438 H H H H H 5-F-1 H-1,2,3-triazol-1-y 1 F-5439 H H H H H 5-M e-1 H-1,2,3-triazol-1-yl 1 F-5440 H H H H H b-F 3 1H-1,2,3-triazol-1-yl 1 F-5441 H H H H H 5-0Me-1H-1,2,3-triazol-1-yI 1 F-5442 H H H H H 1H-1,2,3-triazol-4-y 1 F-5443 H H H H H 5-F-1 H-1,2,3-triazol-4-y 1 F-5444 H H H H H 5-M e-1 H-1,2,3-triazol-4-yl 1 F-5445 H H H H H 5-CF-1H-1,2,3-triazo1-4-yI 1 F-5446 H H H H H 5-0Me-1H-1,2,3-triazol-4-y 1 F-5447 H H H H H 1H-1,2,3-triazol-5-y 1 F-5448 H H H H H 4-F-1H-1,2,3-triazol-5-yI 1 F-5449 H H H H H 4-M e-1 H-1,2,3-triazol-5-yl 1 F-5450 H H H H H 4-CF-1H-1,2,3-triazo-5-yI 1 F-5451 H H H H H 4-0Me-1 H-1,2,3-triazo-b-y 1
[0439]
[Table 314] com pound- R' R2 R R4 R b' p F-5452 H H H H H 1 H-1,2,4-triazol1-y 1 F-5453 H H H H H 5-Me-1H-1,2,4-triazol-1-yl 1 F-5454 H H H H H 5-F-1H-1,2,4-triazol-1-y 1 F-5455 H H H H H 5F,-1 H--1,2,4-triazol-1-yl 1 F-5456 H H H H H 5-0Me1H-1/H-1,2,4-triazol-1-yI 1 F-5457 H H H H H 1 H-1,2,4-triazol-3-y 1 F-5458 H H H H H 1-M e-1 H-1,2,4-triazol-3-yl 1 F-5459 H H H H H 1 H-1,2,4-triazol-5-y 1 F-5460 H H H H H 1-M e-1 H-1,2,4-triazol-5-yl 1 F-5461 H H H H H 3,b-(Me)2 -isoxazol-4-yl 1 F-5462 H H H H H 3,5-(Et)2 -isoxazol-4-y 1 F-5463 H H H H H 1,3,5-(Me)3 -1 H-pyrazol-4-yI 1 F-5464 H H H H H quholin-4-yI 1 F-5465 H H H H H isoquinolin-4-yI 1 F-5466 H H H H H 3,6-(0M e) 2-pyridazh-4-y 1 1 F-5467 H H H H H 2,4-(0M e) 2 -pyrm idnh-5-y 1 1
[0440] On the other hand, the present compound represented by general
formula [I] or [II] can be produced in accordance with, but not limited to, the production
methods shown below. Hereinafter, for example, "compound represented by general
formula [I]" is synonymous to "compound represented by formula [I]" and "compound [I]".
[0441] <Production method 1>
A compound represented by general formula [VI] among the present compounds
can be produced, for example, in accordance with the following method.
[0442] [Chemical formula 3]
R3 R2 O R17 R1 8 S0 2X' R3 R2 O R17 R4 N 11I R4 / NN 0N N- OH (R'SO 2 )2 0 N- 18 R1 R 5 [V] R R5 R
[III] [ VI ] (wherein, R r e presents a Ci-C 6 alkyl group, R1 8 represents a Ci-C6 alkyl group,
Ci-C6 haloalkyl group, di(Ci-C6 alkyl)amino group, or a phenyl group that is unsubstituted or
substituted with (Rm, X 1 represents a halogen atom, and R1, R2, R3, R4, R', and R9 are as
defined above.)
That is, the compound represented by general formula [VI] can be produced by
reacting compound [III] and compound [IV] or compound [V] in an appropriate solvent in the presence of an appropriate base.
[0443] The compound represented by general formula [III] used in the
present reaction can be produced by a method described in WO 2012/028332 A, WO
2014/114649 A, WO 2016/027790 A, WO 2016/166250 A, or US 5,055,482, or produced in
accordance with such a method.
[0444] The use amount of compound [IV] or compound [V] used in the
present reaction may be appropriately selected from the range of 1 to 5 mol, and is preferably
1.0 to 2.0 mol, relative to 1 mol of compound [III].
[0445] Examples of the solvent that can be used in the present reaction
include halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane,
or carbon tetrachloride; ethers such as diethylether, tetrahydrofuran, or 1,4-dioxane, 1,2
dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene,
xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N
dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; aliphatic
hydrocarbons such as pentane, hexane, cyclohexane, or heptane; nitriles such as acetonitrile,
or propionitrile; pyridines such as pyridine, or picoline; tertiary amines such as triethylamine,
or tributylamine; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to
300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [III].
[0446] Examples of the base that can be used in the present reaction include
inorganic bases such as hydroxides of alkali metal(e.g. sodium hydroxide or potassium
hydroxide); hydroxides of alkali earth metal(e.g. calcium hydroxide or magnesium
hydroxide); carbonates of alkali metal(e.g. sodium carbonate or potassium
carbonate); bicarbonates of alkali metal(e.g. sodium hydrogen carbonate or potassium
hydrogen carbonate); metal hydrides(e.g. sodium hydride or potassium hydride); metal salts
of alcohol(e.g. sodium methoxide, sodium ethoxide, or potassium tert-butoxide); or
organic bases such as triethylamine, N,N-dimethylaniline, pyridine, 4-N,N
dimethylaminepyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of
the base may be appropriately selected from the range of 1.0 to 5.0 mol, and is preferably 1.0 to 3.5 mol, relative to 1 mol of compound [III]. The organic bases such as triethylamine or pyridine can also be used as the solvent.
[0447] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -70°C to a reflux temperature in a reaction system,
and is preferably in the range of0°C to 150°C.
[0448] The reaction time of the present reaction is typically 10 minutes to 24
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0449] After end of the reaction, water is added to the reaction mixture, and
then extraction with an organic solvent is conducted, and then concentration or the like
operation is conducted, and thus compound [VI] can be isolated. The isolated compound
[VI] can be further purified by column chromatography, recrystallization, or the like as
necessary.
[0450] <Production method 2>
A compound represented by general formula [VIII] among the present
compounds can be produced, for example, in accordance with the following method.
[0451] [Chemical formula 4]
R3 R2 O R17 R3 R2 N R17
R4 NN O R4 N/ N- N- X R1 R5 R1 R5
[VII] [VIII]
(wherein, R 1, R 2, R3, R4, R5 , R 17, and X1 are as defined above.)
That is, the compound represented by general formula [VIII] can be produced by
reacting compound [VII] and a halogenating agent in an appropriate solvent in the presence or
absence of an appropriate acid, in the presence or absence of an appropriate oxidizing agent.
[0452] The compound represented by general formula [VII] used in the
present reaction can be produced by a method described in WO 2008/019357 A or WO
2008/157740 A, or produced in accordance with such a method.
[0453] Examples of the halogenating agent used in the present reaction
include fluorine, chlorine, bromine, iodine, N-chlorosuccinimide, N-bromosuccinimide, N
iodosuccinimide, sulfuryl chloride, iodine monochloride, tert-butyl hypochlorite, N-fluoro-N'
(chloromethyl)-triethylenediaminebis(tetrafluoroborate), 1-fluoro-2,6-dichloropyridinium
tetrafluoroborate, or 1,3-dibromo-5,5-dimethylhydantoin. The use amount of the
halogenating agent may be appropriately selected from the range of 1.0 to 10 mol, and is
preferably 1.0 to 3.0 mol, relative to 1 mol of compound [VII].
[0454] Examples of the oxidizing agent that can be used in the present
reaction include ammonium hexanitratocerate (IV), hydrogen peroxide, or iodobenzene
diacetate. The use amount of the oxidizing agent may be appropriately selected from the
range of 0 to 10 mol, and is preferably 0 to 3.0 mol, relative to1 mol of compound [VII].
[0455] Examples of the solvent that can be used in the present reaction
include inorganic acids such as sulfuric acid; ethers such as diethylether, tetrahydrofuran, 1,4
dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as
benzene, toluene, xylene, or chlorobenzene; halogenated hydrocarbons such as
dichloromethane, chloroform, 1,2-dichloroethane, or carbon tetrachloride; aprotic polar
solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone,
dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl
cellosolve; nitriles such as acetonitrile or propionitrile; carboxylic acids such as acetic acid or
trifluoroacetic acid; pyridines such as pyridine or picoline; ketones such as acetone or
methyl ethyl ketone; water, or mixed solvents thereof. The use amount of the solvent is 0.1
to 100 liters, preferably 0.3 to 10 liters relative to 1 mol of compound [VII].
[0456] Examples of the acid that can be used in the present reaction include
inorganic acids such as sulfuric acid; or carboxylic acids such as acetic acid or trifluoro acetic
acid. The use amount of the acid may be appropriately selected from the range of 1.0 to 10
mol, and is preferably 0 to 3.0 mol, relative to 1 mol of compound [VII]. The acid may be
used as the solvent.
[0457] The reaction temperature of the present reaction may be selected from any range of temperature from -60°C to a reflux temperature in a reaction system, and is preferably in the range of -20°C to 100°C.
[0458] The reaction time of the present reaction is typically 10 minutes to 24
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0459] After end of the reaction, water is added to the reaction mixture, and
then extraction with an organic solvent is conducted, and then concentration or the like
operation is conducted, and thus compound [VIII] can be isolated. The isolated compound
[VIII] can be further purified by column chromatography, recrystallization, or the like as
necessary.
[0460] <Production method 3>
A compound represented by general formula [XII] among the compounds of the
present invention can be produced, for example, in accordance with the following method.
[0461] [Chemical formula 5]
HO, B-Q R3 R2 0 HO R3 R2 0
4 R 4 NN R19 [X] /R NR9 N- L N R1 R5 O -Q R1 R 5
[IX] [XII] [XI]
(wherein, L represents a halogen atom, C1-C6 alkylsulfonyloxy group, C1-C6
haloalkylsulfonyloxy group, di(Ci-C6 alkyl)sulfamoyloxy group, or a phenylsulfonyloxy
group that is unsubstituted or substituted with (R9)m, Q" represents a C6 -Cio aryl group that is
unsubstituted or substituted with (R8 )m or a heteroaryl group that is unsubstituted or
substituted with (R8 )m, R 19 represents a group OR or a group NR6 R7 , and m, R, R2 , R3 , R4 ,
R,R6 ,R 8, R9, and R are as defined above.)
[0462] Some of [X] or [XI] used herein are known compounds, part of which
are commercially available. The remainder can be easily synthesized according to the method described in literature, for example, in the methods described in Chemical Review,
1995, vol. 95, p. 2457; Journal of Organic Chemistry, 1995, vol. 60, p. 7508; Journal of
Organic Chemistry 1997, vol. 62, p. 6458 and so on.
[0463] That is, the compound represented by general formula [XII] can be
produced by reacting compound [IX] and compound [X] or compound [XI] in an appropriate
solvent in the presence of an appropriate catalyst and an appropriate base.
[0464] The use amount of compound [X] or compound [XI] used in the
present reaction may be appropriately selected from the range of 1.0 to 10mol, and is
preferably 1.0 to 3.0 mol, relative to 1 mol of compound [IX].
[0465] Examples of the solvent that can be used in the present reaction
include ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or
methyl tert-butylether; aromatic hydrocarbons such as benzene, toluene, xylene, or
chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N
dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such
as methanol, ethanol, 2-propanol, or methyl cellosolve; aliphatic hydrocarbons such as
pentane, hexane, cyclohexane, or heptane; water, or mixed solvents thereof. The use amount
of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound
[IX].
[0466] Examples of the catalyst that can be used in the present reaction
include palladium catalysts such as palladium-carbon, palladium chloride, palladium
acetate, tris(dibenzylideneacetone)dipalladium, bis(dibenzylideneacetone)dipalladium,
bis(triphenylphosphine)palladium dichloride, tetrakis(triphenylphosphine)palladium,
[1,1'-bis(diphenylphosphino)ferrocene]palladium dichloride, or [1,2
bis(diphenylphosphino)ethane]palladium dichloride; or copper catalysts such as metal copper,
copper (I) acetate, coper (II) acetate, copper (I) oxide, copper(II) oxide, copper (I) chloride, or
copper (I) iodide.
[0467] Besides the above, a palladium catalyst prepared from a palladium
catalyst and a ligand may be used. Examples of the palladium catalyst include palladium acetate, tris(dibenzylidene acetone)dipalladium, and bis(dibenzylidene acetone)palladium.
Examples of the ligand include triphenylphosphine, tri(tert-butyl)phosphine,
tricyclohexylphosphine, SPhos, Xantphos, and BINAP.
[0468] The use amount of the catalyst may be appropriately selected from the
range of 0.001 to 1.0 mol, and is preferably 0.01 to 0.5 mol, relative to 1 mol of compound
[IX].
[0469] Examples of the base that can be used in the present reaction include
organic bases such as pyridine, diisopropylethylamine, or triethylamine; hydroxides of alkali
metal such as sodium hydroxide or potassium hydroxide; carbonates of alkali metal such as
sodium carbonate, potassium carbonate, or cesium carbonate; bicarbonates of alkali metal
such as sodium hydrogen carbonate or potassium hydrogen carbonate; metal salts of alcohol
such as sodium methoxide, sodium ethoxide, or potassium tert-butoxide; tripotassium
phosphate, potassium fluoride, or cesium fluoride. The use amount of the base may be
appropriately selected from the range of 0.1 to 10 mol, and is preferably 1.0 to 5.0 mol,
relative to 1 mol of compound [IX].
[0470] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -30°C to a reflux temperature in a reaction system,
and is preferably in the range of0°C to 150°C.
[0471] The reaction time of the present reaction is typically 1 minute to 72
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0472] After end of the reaction, water is added to the reaction mixture, and
then the precipitated solid is filtered off or extracted with an organic solvent, followed by
concentration or the like operation, and thus compound [XII] can be isolated. The isolated
compound [XII] can be further purified by column chromatography, recrystallization, or the
like as necessary.
[0473] <Production method 4>
A compound represented by general formula [XIV] among the present compounds can be produced, for example, in accordance with the following method.
[0474] [Chemical formula 6] R R2 17 Ra R2 0
RNN O'rR RN OH
R1 R 5 R1 R5
[XIII] [XIV]
(wherein, Q, R', R 2, R3 , R 4, R5 , and R are as defined above.)
[0475] That is, the compound represented by general formula [XIV] can be
produced by hydrolysis of compound [XIII] in an appropriate solvent in the presence of an
appropriate base or appropriate acid.
[0476] Examples of the base that can be used in the present reaction include
inorganic bases such as hydroxides of alkali metal(e.g. sodium hydroxide, potassium
hydroxide, lithium hydroxide, or barium hydroxide); carbonates of alkali metal(e.g. sodium
carbonate or potassium carbonate); bicarbonates of alkali metal(e.g. sodium hydrogen
carbonate or potassium hydrogen carbonate). The use amount of the base may be
appropriately selected from the range of 0.1 to 50 mol, and is preferably 0.5 to 20 mol,
relative to 1 mol of compound [XIII].
[0477] Examples of the acid that can be used in the present reaction include
inorganic acids such as hydrochloric acid, hydrobromic acid, or sulfuric acid; or carboxylic
acids such as acetic acid or trifluoro acetic acid. The use amount of the acid may be
appropriately selected from the range of I to 1000 mol, and is preferably I to 100 mol,
relative to 1 mol of compound [XIII].
[0478] Examples of the solvent that can be used in the present reaction
include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2
dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene,
xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N
dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such
as methanol, ethanol, 2-propanol, or methyl cellosolve; nitriles such as acetonitrile or propionitrile; ketones such as acetone or methylethylketone; water, or mixed solvents thereof.
The use amount of the solvent is 0.1 to 500 liters, preferably 0.3 to 30 liters relative to 1 mol
of compound [XIII].
[0479] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -30°C to a reflux temperature in a reaction system,
and is preferably in the range of0°C to 150°C.
[0480] The reaction time of the present reaction is typically 10 minutes to 72
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0481] After end of the reaction, the reaction mixture water is neutralized by
adding water, and then the precipitated solid is filtered off or extracted with an organic
solvent, followed by concentration or the like operation, and thus compound [XIV] can be
isolated. The isolated compound [XIV] can be further purified by column chromatography,
recrystallization, or the like as necessary.
[0482] <Production method 5>
A compound represented by general formula [XVII] among the present
compounds can also be produced, for example, in accordance with the following method.
[0483] [Chemical formula 7]
R3 R2 O R3 R2 O 0 R 4 ,N X R4 \ NN OH N- , N- ,; R1 R 5 RQR5
[XIV] [XV] R7 NH R R3 R2 O 7
[XVI] N N S R4 / N R '
N- Q R1 R 5
[ XVII] (wherein, Q, R 1, R 2, R 3, R4, R, R6, R7, and X1 are as defined above.)
[0484] That is, the compound represented by general formula [XVII] can be
produced by (step 1) making compound [XIV] into compound [XV] by using an acid
halogenating agent in an appropriate solvent in the presence or absence of an appropriate
catalyst, and then (step 2) reacting with compound [XVI] or a salt thereof in an appropriate
solvent in the presence or absence of an appropriate base.
[0485] (Step 1)
Examples of the acid halogenating agent that can be used in the present reaction
include thionyl chloride, oxalyl chloride, or phosphoryl chloride. The use amount of the
acid halogenating agent may be appropriately selected from the range of 0.1 to 30 mol, and is
preferably 0.5 to 10 mol, relative to 1 mol of compound [XIV].
[0486] Examples of the catalyst that can be used in the present reaction
include N,N-dimethylformamide. The use amount of the catalyst may be appropriately
selected from the range of 0.01 to 1.0 mol, and is preferably 0.01 to 0.1 mol, relative to 1 mol
of compound [XIV].
[0487] Examples of the solvent that can be used in the present reaction
include ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2
dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene,
xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform,
1,2-dichloroethane, or carbon tetrachloride; nitriles such as acetonitrile or propionitrile; esters
such as ethyl acetate, or ethyl propionate; aliphatic hydrocarbons such as pentane, hexane,
cyclohexane, or heptane; or mixed solvents thereof. The use amount of the solvent is 0.1 to
100 liters, preferably 0.3 to 10 liters relative to 1 mol of compound [XIV].
[0488] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -30°C to a reflux temperature in a reaction system,
and is preferably in the range of0°C to 150°C.
[0489] The reaction time of the present reaction is typically 10 minutes to 24
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0490] After end of the reaction, compound [XV] can be isolated by
conducting concentration or the like operation.
[0491] (Step 2)
The use amount of compound [XVI] used in the present reaction may be
appropriately selected from the range of typically I to 500 mol, and is preferably 1.0 to 300
mol, relative to 1 mol of compound [XV].
[0492] Examples of the solvent that can be used in the present reaction
include ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2
dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene,
xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform,
1,2-dichloroethane, or carbon tetrachloride; aprotic polar solvents such as N,N
dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or
sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; nitriles such
as acetonitrile or propionitrile; esters such as ethyl acetate or ethyl propionate; aliphatic
hydrocarbons such as pentane, hexane, cyclohexane, or heptane; pyridines such as pyridine or
picoline; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters,
preferably 0.2 to 50 liters relative to 1 mol of compound [XV].
[0493] Examples of the base that can be used in the present reaction include
inorganic bases such as hydroxides of alkali metal(e.g. sodium hydroxide or potassium
hydroxide); hydroxides of alkali earth metal(e.g. calcium hydroxide or magnesium
hydroxide); carbonates of alkali metal(e.g. sodium carbonate or potassium
carbonate); bicarbonates of alkali metal(e.g. sodium hydrogen carbonate or potassium
hydrogen carbonate): metal hydrides(e.g. sodium hydride or potassium hydride); metal salts
of alcohol(e.g. sodium methoxide, sodium ethoxide, or potassium tert-butoxide); or
organic bases such as triethylamine, N,N-dimethylaniline, pyridine, 4-N,N
dimethylaminepyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of
the base may be appropriately selected from the range of 0 to 5 mol, and is preferably 0 to 1.2
mol, relative to 1 mol of compound [XV].
[0494] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -30°C to a reflux temperature in a reaction system,
and is preferably in the range of0°C to 150°C.
[0495] The reaction time of the present reaction is typically 10 minutes to 24
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0496] After end of the reaction, water is added to the reaction mixture, and
then the precipitated solid is filtered off or extracted with an organic solvent, followed by
concentration or the like operation, and thus compound [XVII] can be isolated. The isolated
compound [XVII] can be further purified by column chromatography, recrystallization, or the
like as necessary.
[0497] <Production method 6>
A compound represented by general formula [XVII] among the present
compounds can also be produced, for example, in accordance with the following method.
[0498] [Chemical formula 8]
/7 NH 3 2 R R 0 R6 R3 R2 7 , OH [XVI] ,R R4 - N R4 -N ;'6 N R 1 R5 R 1 R5
[XIV] [ XVII]
(wherein, Q, R', R 2, R 3, R4, R , R , and R are as defined above.)
[0499] That is, the compound represented by general formula [XVII] can be
produced by reacting compound [XIV] and compound [XVI] or a salt thereof in an
appropriate solvent in the presence or absence of an appropriate condensing agent and an
appropriate base.
[0500] The use amount of compound [XVI] or a salt thereof used in the
present reaction may be appropriately selected from the range of 1 to 10 mol, and is preferably 1.0 to 3.0 mol, relative to 1 mol of compound [XIV].
[0501] Examples of the condensing agent that can be used in the present
reaction include 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride, a mixture of
1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride and 1-hydroxybenzotriazole,
1-ethyl-3-(3-dimethylaminopropyl)carbodiimide, a mixture of 1-ethyl-3-(3
dimethylaminopropyl)carbodiimide and 1-hydroxybenzotriazole, N,N'
dicyclohexylcarbodiimide, N,N'-diisopropylcarbodiimide, N,N'-carbonyldiimidazole, 4-(4,6
dimethoxy-1,3,5-triazine-2-yl)-4-methylmorpholinium chloride, 1H-benzotriazole-1
yloxytris(dimethylamino)phosphonium hexafluorophosphate, {{[(1-cyano-2-ethoxy-2
oxoethylidene)amino]oxy}-4-morpholinomethylene}dimethylammonium
hexafluorophosphate, or O-(7-azabenzotriazole-1-yl)-N,N,N',N'-tetramethyluronium
hexafluorophosphate. The use amount of the condensing agent may be appropriately
selected from the range of 1.0 to 10 mol, and is preferably 1.0 to 6.0 mol, relative to 1 mol of
compound [XIV].
[0502] When a base is used in the present reaction, examples of the base that
can be used include organic bases such as triethylamine, 4-methylmorpholine,
diisopropylethylamine, 1,8-diazabicyclo[5.4.0]-7-undecene, pyridine, or 2,6-lutidine. The
use amount of the base may be appropriately selected from the range of 0 to 10 mol, and is
preferably 0.1 to 6.0 mol, relative to 1 mol of compound [XIV].
[0503] Examples of the solvent that can be used in the present reaction
include halogenated hydrocarbons such as dichloromethane, chloroform, or 1,2
dichloroethane, or carbon tetrachloride; aliphatic hydrocarbons such as pentane, hexane,
cyclohexane, or heptane; esters such as ethyl acetate, or ethyl propionate; nitriles such as
acetonitrile or propionitrile; aprotic polar solvents such as N,N-dimethylformamide, N,N
dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; ethers such as
diethylether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or methyl tert-butyl ether; or
mixed solvents thereof. The use amount of the solvent is 0.1 to 100 liters, preferably 0.3 to
50 liters relative to 1 mol of compound [XIV].
[0504] The present reaction can be conducted in the presence of a catalyst as
necessary, and examples of the catalyst include 4-(N,N-dimethyl)aminopyridine. The use
amount of the catalyst may be appropriately selected from the range of 0.001 to 10 mol, and is
preferably 0.01 to 0.3 mol, relative to 1 mol of compound [XIV].
[0505] The reaction temperature of the present reaction may be selected from
any range of temperature from -20°C to a reflux temperature in a reaction system, and is
preferably in the range of0°C to 80°C.
[0506] The reaction time of the present reaction is typically 1 minute to 48
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0507] After end of the reaction, water is added to the reaction mixture, and
then the precipitated solid is filtered off or extracted with an organic solvent, followed by
concentration or the like operation, and thus compound [XVII] can be isolated. The isolated
compound [XVII] can be further purified by column chromatography, recrystallization, or the
like as necessary.
[0508] <Production method 7>
A compound represented by general formula [XVII] among the present
compounds can be produced, for example, in accordance with the following method.
[0509] [Chemical formula 9] 7 R NH R3 R2 0 R6 R3 R2 0 Rr NN OR [XVI ] N R4N R
N- .; N- .; Q R1 R 5 R1 R 5
[XIII] [ XVII] (wherein, Q, R', R 2, R3 , R 4, R', R6 , R7 , and R1 7 are as defined above.)
[0510] That is, the compound represented by general formula [XVII] can be
produced by reacting the compound represented by general formula [XIII] and the compound
represented by general formula [XVI] in an appropriate solvent in the presence or absence of an appropriate base.
[0511] The use amount of compound [XVI] used in the present reaction may
be appropriately selected from the range of typically 1.0 to 500 mol, and is preferably 1.0 to
300 mol, relative to 1 mol of compound [XIII].
[0512] Examples of the solvent that can be used in the present reaction
include ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2
dimethoxyethane, or methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene,
xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform,
1,2-dichloroethane, or carbon tetrachloride; aprotic polar solvents such as N,N
dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or
sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; nitriles such
as acetonitrile or propionitrile; esters such as ethyl acetate or ethyl propionate; aliphatic
hydrocarbons such as pentane, hexane, cyclohexane, or heptane; pyridines such as pyridine or
picoline; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters,
preferably 0.2 to 50 liters relative to 1 mol of compound [XIII].
[0513] Examples of the base that can be used in the present reaction include
inorganic bases such as hydroxides of alkali metal(e.g. sodium hydroxide or potassium
hydroxide); hydroxides of alkali earth metal(e.g. calcium hydroxide or magnesium
hydroxide); carbonates of alkali metal(e.g. sodium carbonate or potassium
carbonate); bicarbonates of alkali metal(e.g. sodium hydrogen carbonate or potassium
hydrogen carbonate): metal hydrides(e.g. sodium hydride or potassium hydride); metal salts
of alcohol(e.g. sodium methoxide, sodium ethoxide, or potassium tert-butoxide); or
organic bases such as triethylamine, N,N-dimethylaniline, pyridine, 4-N,N
dimethylaminepyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of
the base may be appropriately selected from the range of 0 to 5.0 mol, and is preferably 0 to
1.2 mol, relative to 1 mol of compound [XIII].
[0514] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -30°C to a reflux temperature in a reaction system, and is preferably in the range of0°C to 150°C.
[0515] The reaction time of the present reaction is typically 10 minutes to 1
week although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0516] After end of the reaction, water is added to the reaction mixture, and
then extraction with an organic solvent is conducted, and then concentration or the like
operation is conducted, and thus compound [XVII] can be isolated. The isolated compound
[XVII] can be further purified by column chromatography, recrystallization, or the like as
necessary.
[0517] <Production method 8>
A compound represented by general formula [XIX] among the present
compounds can be produced, for example, in accordance with the following method.
[0518] [Chemical formula 10]
R3 R2 0 R3 R2 0
R4N R1 R419 N- N R1 R - R R5
[XVIII] [XIX] (wherein, Q, R', R 2, R 3, R 4, R5, and R1 9 are as defined above.)
[0519] That is, the compound represented by general formula [XIX] can be
produced by reacting compound [XVIII] and an appropriate oxidizing agent in an appropriate
solvent in the presence or absence of a catalyst.
[0520] Examples of the solvent that can be used in the present reaction
include halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane,
carbon tetrachloride; ethers such as diethylether, tetrahydrofuran, 1,4-dioxane, 1,2
dimethoxyethane, or methyl tert-butyl ether; aprotic polar solvents such as N,N
dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or
sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; ketones such
as acetone or methyl ethyl ketone; nitriles such as acetonitrile or propionitrile; acetic acid, water, or mixtures thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.3 to 200 liters relative to 1 mol of compound [XVIII].
[0521] Examples of the oxidizing agent that can be used in the present
reaction include organic peroxides such as m-chloroperbenzoic acid, performic acid, or
peracetic acid; and inorganic peroxides such as hydrogen peroxide, potassium permanganate,
OXONE (registered tradename available from E. I. du Pont de Nemours and Company,
product containing potassium peroxymonosulfate), or sodium periodate. The use amount of
the oxidizing agent is 0.5 to 3.0 mol, relative to 1 mol of compound [XVIII].
[0522] Examples of the catalyst that can be used in the present reaction
include sodium tungstate. The use amount of the catalyst is 0.01 to 0.5 mol, relative to 1
mol of compound [XVIII].
[0523] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -30°C to a reflux temperature in a reaction system,
and is preferably in the range of -10°C to 100°C.
[0524] The reaction time of the present reaction is typically 10 minutes to 48
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0525] After end of the reaction, water is added to the reaction mixture, and
then extraction with an organic solvent is conducted, and then concentration or the like
operation is conducted, and thus compound [XIX] can be isolated. Alternatively, compound
[XIX] can also be isolated by concentrating the solvent of the reaction mixture. The isolated
compound [XIX] can be further purified by column chromatography, recrystallization, or the
like as necessary.
[0526] <Production method 9>
A compound represented by general formula [XX] among the present compounds
can be produced, for example, in accordance with the following method.
[0527] [Chemical formula 11]
3 R2 R3 R2 OR O
R4 L/ RN -B(OR 20 )2 12 4 B( 2)
R1 R 5 L R1 R5
[IX] [XX]
(wherein, R 2 0 s, which may be the same or different, each represent a hydrogen
atom or C1-C alkyl, or two R 2 0s may together form -H2 C H2- or -C(CH 3) 2C(CH 3)2 -, and L,
R 1, R 2, R3, R4, R and R1 9 are as defined above.)
[0528] That is, the compound represented by general formula [XX] can be
produced by reacting compound [IX] and compound -[B(OR 2 0 ) 2 ]2 in an appropriate solvent in
the presence of an appropriate catalyst and an appropriate base.
[0529] The use amount of compound -[B(OR 2 0) 2 ]2 used in the present
reaction may be appropriately selected from the range of 1 to 10 mol, and is preferably 1.0 to
3.0 mol, relative to 1 mol of compound [IX].
[0530] Examples of the solvent that can be used in the present reaction
include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or
methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or
chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N
dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such
as methanol, ethanol, 2-propanol, or methyl cellosolve; aliphatic hydrocarbons such as
pentane, hexane, cyclohexane, or heptane; water, or mixed solvents thereof. The use amount
of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound
[IX].
[0531] Examples of the catalyst that can be used in the present reaction
include palladium catalysts such as palladium-carbon, palladium chloride, palladium acetate,
tris(dibenzylideneacetone)dipalladium, bis(dibenzylideneacetone)palladium,
bis(triphenylphosphine)palladium dichloride, tetrakis(triphenylphosphine)palladium, [1,1'
bis(diphenylphosphino)ferrocene]palladium dichloride, or [1,2
bis(diphenylphosphino)ethane]palladium dichloride; or copper catalysts such as metal copper, copper (I) acetate, coper (II) acetate, copper (I) oxide, copper (II) oxide, copper (I)chloride, or copper (I) iodide.
[0532] Besides the above, a palladium catalyst prepared from a palladium
catalyst and a ligand may be used. Examples of the palladium catalyst include palladium
acetate, tris(dibenzylidene acetone)dipalladium, and bis(dibenzylidene acetone)palladium.
Examples of the ligand include triphenylphosphine, tri(tert-butyl)phosphine,
tricyclohexylphosphine, SPhos, Xantphos, and BINAP.
[0533] The use amount of the catalyst may be appropriately selected from the
range of 0.001 to 1.0 mol, and is preferably 0.01 to 0.5 mol, relative to 1 mol of compound
[IX].
[0534] Examples of the base that can be used in the present reaction include
organic bases such as pyridine, diisopropylethylamine, or triethylamine; carbonates of alkali
metal such as sodium carbonate, potassium carbonate, or cesium carbonate; bicarbonates of
alkali metal such as sodium hydrogen carbonate or potassium hydrogen carbonate; metal salts
of alcohol such as sodium methoxide, sodium ethoxide, or potassium tert-butoxide; potassium
phosphate, potassium fluoride, cesium fluoride, or potassium acetate. The use amount of the
base may be appropriately selected from the range of 0.1 to 10 mol, and is preferably 1.0 to
5.0 mol, relative to 1 mol of compound [IX].
[0535] The reaction temperature of the present reaction may be selected from
any range of temperature typically from 25°C to a reflux temperature in a reaction system,
and is preferably in the range of 30°C to 150°C.
[0536] The reaction time of the present reaction is typically 1 minute to 72
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0537] After end of the reaction, water is added to the reaction mixture, and
then the precipitated solid is filtered off or extracted with an organic solvent, followed by
concentration or the like operation, and thus compound [XX] can be isolated. The isolated
compound [XX] can be further purified by column chromatography, recrystallization, or the like as necessary.
[0538] <Production method 10>
A compound represented by general formula [XII] among the present compounds
can be produced, for example, in accordance with the following method.
[Chemical formula 12]
R3 R2 O Q"--- R3 R2 O
[XXI] R4 \ NN R9 R4 \ NN R19 N- B(OR20)2 N R1 R 5 R1 R 5
[XX ] [XII ]
(wherein, Q", L, R', R 2, R3 , R4 , R5 , R1 9 and R 20 are as defined above.)
[0539] That is, the compound represented by general formula [XII] can be
produced by reacting compound [XX] and compound [XXI] in an appropriate solvent in the
presence of an appropriate catalyst and an appropriate base.
[0540] The use amount of compound [XXI] used in the present reaction may
be appropriately selected from the range of 0.3 to 10 mol, and is preferably 0.4 to 3.0 mol,
relative to 1 mol of compound [XX].
[0541] Examples of the solvent that can be used in the present reaction
include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or
methyltert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or
chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N
dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such
as methanol, ethanol, 2-propanol, or methyl cellosolve; aliphatic hydrocarbons such as
pentane, hexane, cyclohexane, or heptane; water, or mixed solvents thereof. The use amount
of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound
[XX].
[0542] Examples of the catalyst that can be used in the present reaction
include palladium catalysts such as palladium-carbon, palladium chloride, palladium acetate,
tris(dibenzylideneacetone)dipalladium, bis(dibenzylideneacetone)palladium, bis(triphenylphosphine)palladium dichloride, tetrakis(triphenylphosphine)palladium, [1,1' bis(diphenylphosphino)ferrocene]palladium dichloride, or [1,2 bis(diphenylphosphino)ethane]palladium dichloride; or copper catalysts such as metal copper, copper (I) acetate, coper (II) acetate, copper (I) oxide, copper (II) oxide, copper (I)chloride, or copper (I) iodide.
[0543] Besides the above, a palladium catalyst prepared from a palladium
catalyst and a ligand may be used. Examples of the palladium catalyst include palladium
acetate, tris(dibenzylidene acetone)dipalladium, and bis(dibenzylidene acetone)palladium.
Examples of the ligand include triphenylphosphine, tri(tert-butyl)phosphine,
tricyclohexylphosphine, SPhos, Xantphos, and BINAP.
[0544] The use amount of the catalyst may be appropriately selected from the
range of 0.001 to 1.0 mol, and is preferably 0.01 to 0.5 mol, relative to 1 mol of compound
[XX].
[0545] Examples of the base that can be used in the present reaction include
organic bases such as pyridine, diisopropylethylamine, or triethylamine; hydroxides of alkali
metal such as sodium hydroxide or potassium hydroxide; carbonates of alkali metal such as
sodium carbonate, potassium carbonate, or cesium carbonate; bicarbonates of alkali metal
such as sodium hydrogen carbonate or potassium hydrogen carbonate; metal salts of alcohol
such as sodium methoxide, sodium ethoxide, or potassium tert-butoxide; potassium phosphate,
potassium fluoride, or cesium fluoride. The use amount of the base may be appropriately
selected from the range of 0.1 to 10 mol, and is preferably 1.0 to 5.0 mol, relative to 1 mol of
compound [XX].
[0546] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -30°C to a reflux temperature in a reaction system,
and is preferably in the range of0°C to 150°C.
[0547] The reaction time of the present reaction is typically 1 minute to 72
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0548] After end of the reaction, water is added to the reaction mixture, and
then the precipitated solid is filtered off or extracted with an organic solvent, followed by
concentration or the like operation, and thus compound [XII] can be isolated. The isolated
compound [XII] can be further purified by column chromatography, recrystallization, or the
like as necessary.
<Production method 11>
A compound represented by general formula [XXII] among the present
compounds can be produced, for example, by using a compound represented by general
formula [XVII] in accordance with the following method.
[0549] [Chemical formula 13]
R3 R2 0 O R3 R2 S 7 R N R4 NR * 4 1 N Q N-Q 1 5 R' R 5 R R
[XVII] [XXII]
(wherein, R', R 2, R 3, R4, R , R 6, R 7 and Q are as defined above.)
That is, the compound represented by general formula [XXII] can be produced by
reacting compound [XVII] with an appropriate sulphidizing agent.
[0550] Examples of the solvent that can be used in the present reaction
include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or
methyltert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or
chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N
dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; halogenated
hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon
tetrachloride; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; water,
or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3
to 50 liters relative to 1 mol of compound [XVII].
[0551] Examples of the sulphidizing agent that can be used in the present reaction include phosphorus pentasulfide, or Lawesson's reagent. The use amount of the sulphidizing agent may be appropriately selected from the range of 0.5 to 30 mol, and is preferably 0.5 to 5 mol, relative to 1 mol of compound [XVII].
[0552] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -70°C to a reflux temperature in a reaction system,
and is preferably in the range of0°C to 150°C.
[0553] The reaction time of the present reaction is typically 10 minutes to 24
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0554] After end of the reaction, water is added to the reaction mixture, and
then extraction with an organic solvent is conducted, and then concentration or the like
operation is conducted, and thus compound [XXII] can be isolated. Alternatively,
compound [XXII] can also be isolated by concentrating the solvent of the reaction mixture.
The isolated compound [XXII] can be further purified by column chromatography,
recrystallization, or the like as necessary.
[0555] <Production method 12>
A compound represented by general formula [XXVI] among the present
compounds can be produced, for example, by using a compound represented by general
formula [XXIII] in accordance with the following method.
[0556] [Chemical formula 14]
R3 R2 O R3 R2 O
4 N, NH 2 4 N N R' R5 R1 R5
[XXIII] [XXIV]
HR R3 R2 O O
[XXV] N N R21 S4N- N 1 R R5
[ XXVI]
(wherein, R 2 1 represents a Ci-C6 alkoxy group, amino group, mono(C1-C6
alkyl)amino group, di(Ci-C 6 alkyl)amino group, Ci-C6 alkylthio group, or Ci-C6 alkoxy Ci
C6 alkoxy group, and Ri, R 2, R3 , R4 , R and Q are as defined above.)
[0557] That is, the compound represented by general formula [XXVI] can be
produced by (step 1) making compound [XXIII] into compound [XXIV] by using oxalyl
chloride in an appropriate solvent or in the absence of a solvent, and then (step 2) reacting
with compound [XXV] or a salt thereof in an appropriate solvent or in the absence of a
solvent.
[0558] (Step 1)
The use amount of oxalyl chloride may be appropriately selected from the range
of 1.0 to 1000 mol, and is preferably 1.0 to 300 mol, relative to 1 mol of compound [XXIII].
[0559] Examples of the solvent that can be used in the present reaction
include ethers such as diethyl ether, tetrahydrofuran, methyltert-butyl ether, or 1,4-dioxane;
aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; halogenated
hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, or carbon
tetrachloride; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide,
N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; nitriles such as acetonitrile or
propionitrile; esters such as ethyl acetate or ethyl propionate, or mixed solvents thereof. The
use amount of the solvent is 0.1 to 500 liters, preferably 0.2 to 50 liters relative to 1 mol of
compound [XXIII].
[0560] The reaction temperature of the present reaction may be selected from
any range of temperature typically from 0°C to a reflux temperature in a reaction system, and
is preferably in the range of 20°C to 90°C.
[0561] The reaction time of the present reaction is typically 1 minute to 6
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0562] After end of the reaction, compound [XXIV] can be isolated by
conducting concentration or the like operation.
[0563] (Step 2)
The use amount of compound [XXV] used in the present reaction may be
appropriately selected from the range of typically 1.0 to 500 mol, and is preferably 1.0 to 300
mol, relative to 1 mol of compound [XXIV].
[0564] Examples of the solvent that can be used in the present reaction
include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or
methyl tert-butyl ether; halogenated hydrocarbons such as dichloromethane, chloroform, 1,2
dichloroethane, or carbon tetrachloride; aprotic polar solvents such as N,N
dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or
sulfolane; nitriles such as acetonitrile or propionitrile; esters such as ethyl acetate or ethyl
propionate, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters,
preferably 0.2 to 50 liters relative to 1 mol of compound [XXIV].
[0565] The reaction temperature of the present reaction may be selected from
any range of temperature typically from -30°C to a reflux temperature in a reaction system,
and is preferably in the range of -10°C to 100°C.
[0566] The reaction time of the present reaction is typically 5 minutes to 24
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0567] After end of the reaction, water is added to the reaction mixture, and
then the precipitated solid is filtered off or extracted with an organic solvent, followed by
concentration or the like operation, and thus compound [XXVI] can be isolated. The
isolated compound [XXVI] can be further purified by column chromatography,
recrystallization, or the like as necessary.
[0568] <Production method 13>
A compound represented by general formula [XVII] among the present
compounds can be produced, for example, by using a compound represented by general
formula [XXVII] in accordance with the following method.
[0569] [Chemical formula 15]
R3 RN2 'H R 7-X 2 R3 R2 O R7 R4 R.- N' NRN R4 /\ N N- RCQ 7 R -0-R7 N- R R1 R [ XXIX] R1 R 5
[ XXVII] [ XVII]
(wherein, X 2 represents a halogen atom, C1 -C 6 alkylsulfonyloxy group,
trifluoromethanesulfonyloxy group, nonafluorobutylsulfonyloxy group, phenylsulfonyloxy
group, 4-toluenesulfonyloxy group, C 1-C 6 alkylsulfonyl group, phenylsulfonyl group or 4
toluenesulfonyl group, and R, R2 , R3, R4, RI, R6, R 7 and Q are as defined above.)
That is, the compound represented by general formula [XVII] can be produced by
reacting compound [XXVII] and compound [XXVIII] or compound [XXIX] in an appropriate
solvent in the presence or absence of an appropriate base.
[0570] The use amount of compound [XXVIII] or compound [XXIX] used in
the present reaction may be appropriately selected from the range of 1.0 to 10 mol, and is
preferably 1.0 to 5.0 mol, relative to 1 mol of compound [XXVII].
[0571] Examples of the solvent that can be used in the present reaction
include ethers such as diethyl ether, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, or
methyl tert-butyl ether; aromatic hydrocarbons such as benzene, toluene, xylene, or
chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N
dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; nitriles such as
acetonitrile or propionitrile; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or
heptane; pyridines such as pyridine or picoline; water, or mixed solvents thereof. The use
amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of
compound [XXVII].
[0572] Examples of the base that can be used in the present reaction include
inorganic bases such as hydroxides of alkali metal(e.g. sodium hydroxide or potassium
hydroxide); hydroxides of alkali earth metal(e.g. calcium hydroxide or magnesium
hydroxide); carbonates of alkali metal(e.g. sodium carbonate or potassium
carbonate); bicarbonates of alkali metal(e.g. sodium hydrogen carbonate or potassium hydrogen carbonate); metal hydrides(e.g. sodium hydride or potassium hydride); metal salts of alcohol(e.g. sodium methoxide, sodium ethoxide, or potassium tert-butoxide); or organic bases such as triethylamine, N,N-dimethylaniline, pyridine, 4-N,N-dimethylaminepyridine,
1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of the base may be
appropriately selected from the range of 1.0 to 10 mol, and is preferably 1.0 to 6.0 mol,
relative to 1 mol of compound [XXVII]. The organic bases such as triethylamine or pyridine
can also be used as the solvent.
[0573] The present reaction can be conducted in the presence of a catalyst as
necessary, and examples of the catalyst include pyridine, 4-(N,N-dimethyl)aminopyridine, or
4-pyrrolidinopyridine. The use amount of the catalyst may be appropriately selected from
the range of 0.001 to 1.0 mol, and is preferably 0.01 to 0.1 mol, relative to 1 mol of
compound [XXVII].
[0574] The reaction temperature of the present reaction may be selected from
any range of temperature from -70°C to a reflux temperature in a reaction system, and is
preferably in the range of0°C to 150°C.
[0575] The reaction time of the present reaction is typically 10 minutes to 24
hours although it differs depending on the reaction temperature, the reaction substrate, the
reaction amount, and the like.
[0576] After end of the reaction, water is added to the reaction mixture, and
then extraction with an organic solvent is conducted, and then concentration or the like
operation is conducted, and thus compound [XVII] can be isolated. The isolated compound
[XVII] can be further purified by column chromatography, recrystallization, or the like as
necessary.
[0577] An agrochemical composition of the present invention contains the
pyrazole derivative or an agriculturally acceptable salt thereof represented by general formula
[I] or [II] of the present invention, as an active ingredient.
[0578] The agrochemical composition can contain an additive component
(carrier) that is typically used in an agrochemical formulation, as necessary.
[0579] The present pest control agent contains the pyrazole derivative or an
agriculturally acceptable salt thereof represented by general formula [I] or [II] of the present
invention, as an active ingredient. The present pest control agent is representatively an
insecticide and a miticide.
[0580] The present pest control agent can contain an additive component
(carrier) that is typically used in an agrochemical formulation, as necessary.
[0581] Examples of the additive component include a carrier such as a solid
carrier or a liquid carrier, a surfactant, a binder or a tackifier, a thickener, a coloring agent, a
spreader, a sticker, an antifreezing agent, an anticaking agent, a disintegrating agent, and a
stabilizing agent, and besides the above, an antiseptic, a plant piece, or the like may be added
to the additive component as necessary. These additive components may be used singly or
in combination of two or more kinds.
[0582] Hereinafter, the aforementioned additive components are described.
[0583] Examples of the solid carrier include mineral carriers such as
pyrophyllite clay, kaolin clay, silica clay, talc, diatomite, zeolite, bentonite, Japanese acid clay,
activated clay, attapulgus clay, vermiculite, pearlite, pumice, white carbon (synthetic silicic
acid, synthetic silicate, or the like), or titanium dioxide; vegetal carriers such as woody
powder, corn haulm, walnut shell, fruit stone, chaff, sawdust, bran, soybean meal, powdered
cellulose, starch, dextrin, or saccgarudes; inorganic salt carriers such as calcium carbonate,
ammonium sulfate, sodium sulfate, or potassium chloride; and polymeric carriers such as
polyethylene, polypropylene, polyvinyl chloride, polyvinyl acetate, ethylene-vinyl acetate
copolymer, or urea-aldehyde resin.
[0584] Examples of the liquid carrier include monohydric alcohols such as
methanol, ethanol, propanol, 2-propanol, butanol, or cyclohexanol; polyhydric alcohols such
as ethylene glycol, diethylene glycol, propylene glycol, hexylene glycol, polyethylene glycol,
polypropylene glycol, or glycerin; polyhydric alcohol derivatives such as propylene glycol
ether; ketones such as acetone, methylethyl ketone, methylisobutyl ketone, diisobutyl ketone,
cyclohexanone, or isophoron; ethers such as ethyl ether, 1,4-dioxane, Cellosolve, dipropyl ether, or tetrahydrofuran; aliphatic hydrocarbons such as normal paraffin, naphthene, isoparaffin, kerosene, or mineral oil; aromatic hydrocarbons such as toluene, Co-Cio alkylbenzene, xylene, solvent naphtha, alkyl naphthalene, or high boiling point aromatic hydrocarbons; halogenated hydrocarbons such as 1,2-dichloroethane, chloroform, or carbon tetrachloride; esters such as ethyl acetate, diisopropyl phthalate, dibutyl phthalate, dioctyl phthalate, or dimethyl adipate; lactones such as y-butyrolactone; amides such as N,N dimethylformamide, N,N-diethylformamide, N,N-dimethylacetamide, or N-methyl-2 pyrrolidone; nitriles such as acetonitrile; sulfur compounds such as dimethyl sulfoxide; vegetable oils such as soybean oil, rapeseed oil, cottonseed oil, coconut oil, or castor oil; and water.
[0585] Although not particularly limited, the surfactant preferably gelates or
shows swelling property in water, and examples of the surfactant include noionic surfactants
such as sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sucrose fatty acid
ester, polyoxyethylene fatty acid ester, polyoxyethylene resin acid ester, polyoxyethylene
fatty acid diester, polyoxyethylene alkyl ether, polyoxyethylene alkylphenyl ether,
polyoxyethylene dialkylphenyl ether, polyoxyethylene alkylphenyl ether formalin condensate,
polyoxyethylene polyoxypropylene block polymer, alkylpolyoxyethylene polypropylene
block polymer ether, polyoxyethylene alkyl amine, polyoxyethylene fatty acid amide,
polyoxyethylene fatty acid bisphenyl ether, polyalkylene benzyl phenyl ether,
polyoxyalkylene styryl phenyl ether, acetylene diol, polyoxyalkylene-added acetylene diol,
polyoxyethylene ether silicone, ester silicone, fluorine surfactant, polyoxyethylene castor oil,
or polyoxyethylene hardened castor oil; anionic surfactants such as alkyl sulfates,
polyoxyethylene alkyl ether sulfates, polyoxyethylene alkyl phenyl ether sulfates,
polyoxyethylene styryl phenyl ether sulfate, alkyl benzenesulfonates, lignin sulfonate, alkyl
sulfosuccinates, naphthalene sulfonate, alkylnaphthalene sulfonates, salts of formalin
condensate of naphthalene sulfonate, salts of formalin condensate of alkylnaphthalene
sulfonate, fatty acid salts, polycarboxylates, N-methyl-fatty acid Sarcosinates, resinates,
polyoxyethylene alkyl ether phosphates, or polyoxyethylene alkyl pheny ether phosphates; cationic surfactants such as alkyl amine salts such as lauryl amine hydrochloride, stearyl amine hydrochloride, oleyl amine hydrochloride, stearyl amine acetate, stearyl aminopropylamine acetate, alkyl trimethyl ammonium chlorides, or alkyl dimethylbenzarconium chloride; and amphoteric surfactants including a betaine type such as dialkyl diaminoethyl betaine, or alkyl dimethylbenzyl betaine, and an amino acid type such as dialkylaminoethyl glycin, or alkyl dimethylbenzyl glycin.
[0586] Examples of the binder or the tackifier include
carboxymethylcelullose or a salt thereof, dextrin, soluble starch, xanthan gum, guar gum,
sucrose, polyvinylpyrrolidone, gum arabic, polyvinyl alcohol, polyvinyl acetate, sodium
polyacrylate, polyethylene glycol having an average molecular weight of 6000 to 20000,
polyethylene oxide having an average molecular weight of 100000 to 5000000, and naturally
occurring phospholipid (for example, Cephalin, lecithin, or the like).
[0587] Examples of the thickener include water-soluble polymers such as
xanthan gum, guar gum, carboxymethylcelullose, polyvinylpyrrolidone, carboxyvinyl
polymer, acrylic polymer, starch derivatives, or polysaccharides; and inorganic fine powder
such as high purity bentonite or white carbon.
[0588] Examples of the coloring agent include inorganic pigments such as
iron oxide, titanium oxide, or Prussian blue; and organic dyes such as an alizarin dye, an azo
dye, or a metal phthalocyanine dye.
[0589] Examples of the spreader include a silicone surfactant, cellullose
powder, dextrin, processed starch, a polyaminocarboxylic acid chelete compound, a cross
linked polyvinylpyrrolidone, malic acid and styrenes, methacrylic acid copolymer, a half ester
of a polymer of polyhydric alcohol and dicarboxylic acid anhydride, and a water-soluble salt
of polystyrene sulfonic acid.
[0590] Examples of the sticker include various surfactants such as sodium
dialkyl sulfosuccinate, polyoxyethylene alkyl ether, polyoxyethylene alkylphenyl ether, or
polyoxyethylene fatty acid ester; paraffin, terpene, polyamide resin, polyacrylate,
polyoxyethylene, wax, polyvinylalkyl ether, an alkylphenol formalin condensate, and a synthetic resin emulsion.
[0591] Examples of the antifreezing agent include polyhydric alcohols such
as ethylene glycol, diethylene glycol, propylene glycol, or glycerin.
[0592] Examples of the anticaking agent include polysaccharides such as
starch, alginic acid, mannose, or galactose; polyvinylpyrrolidone, white carbon, ester gum,
and petroleum resin.
[0593] Examples of the disintegrating agent include sodium tripolyphosphate,
sodium hexametaphosphate, a stearic metal salt, cellulose powder, dextrin, copolymer of
methacrylic ester, polynylpyrrolidone, polyaminocarboxylic chelate compound, styrene
sulfonate-isobutylene-maleic anhydride copolymer, and starch-polyacrylonitrile graft
copolymer.
[0594] Examples of the stabilizing agent include a desiccant such as zeolite,
calcined lime, or magnesium oxide; an antioxidant based on phenol, amine, sulfur, phosphoric
acid, or the like; an ultraviolet absorber based on salicylic acid, benzophenone, or the like.
[0595] In the present pest control agent, when the additive component is
contained, the content thereof is selected typically in a range of 5 to 95%, preferably in the
range of 20 to 90% on the mass basis in the case of a carrier such as a solid carrier or a liquid
carrier, selected typically in a range of 0.1% to 30%, preferably in a range of 0.5 to 10% in the
case of a surfactant, and selected typically in a range of 0.1 to 30%, preferably in a range of
0.5 to 10% in the case of other additive.
[0596] The present pest control agent is used while it is prepared into any
formulation including dusts, dusts and granules, granules, water-dispersible powders, water
soluble powders, water-dispersible granules, tablets, Jumbos, emulsifiable concentrates, oils,
solutions, flowable concentrates, emulsions, microemulsions, suspoemulsions, ultra-low
volume dusting powders, microcapsules, smoking agents, aerosols, baiting agents, and pastes.
[0597] In actual use of the formulation, the formulation can be used per se or
after dilution with a diluent such as water in a predetermined concentration. Application of
various formulations containing the present compound, and dilution products thereof can be conducted by a method ordinarily used, such as dispersion (e.g., spraying, misting, atomizing, powder dispersion, granule dispersion, on-water-surface dispersion, or inbox dispersion), in soil application (e.g., mixing or drenching), on-surface application (e.g., coating, dust coating, or covering), seed treatment (e.g., smearing or dressing treatment), immersion, poison bait, smoking, and the like. It is also possible to mix the above-mentioned active ingredient with a livestock feed in order to prevent the infestation and growth of pests, particularly harmful insects in the excreta of the livestock.
[0598] A method for controlling a pest of the present invention can be
conducted by using an active ingredient amount of the pyrazole derivative represented by
general formula [I] or [II] of the present invention or an agriculturally acceptable salt thereof
in the above-mentioned application method described above.
[0599] The mixing proportion (% by mass) of the active ingredient in the
present pest control agent is appropriately selected as needed. For example, the mixing
proportion may be appropriately selected in the following ranges: 0.01 to 20%, preferably
0.05 to 10% for dusts, dusts and granules, microgranules, or the like; 0.1 to 30%, preferably
0.5 to 20% for granules or the like;1 to 70%, preferably 5 to 50% for water-dispersible
powders, water-dispersible granules, or the like; 1 to 95%, preferably 10 to 80% for water
soluble powders, solutions, or the like; 5 to 90%, preferably 10 to 80% for emulsifiable
concentrates or the like; I to 50%, preferably 5 to 30% for oils or the like; 5 to 60%,
preferably 10 to 50% for flowable concentrates or the like; 5 to 70%, preferably 10 to 60% for
emulsions, microemulsions, suspoemulsions, or the like; 1 to 80%, preferably 5 to 50% for
tablets, baiting agents, pastes, or the like; 0.1 to 50%, preferably I to 30% for smoking agents
or the like; and 0.05 to 20%, preferably 0.1 to 10% for aerosols or the like.
[0600] The formulation is sprayed after dilution in an appropriate
concentration, or applied directly.
[0601] When present pest control agent is used after dilution with a diluent,
the concentration of the active ingredient is generally 0.1 to 5000 ppm. When the
formulation is used per se, the application amount thereof per unit area is 0.1 to 5000 g per 1 ha in terms of the active ingredient compound; however, the application amount is not restricted thereto.
[0602] It goes without saying that the present pest control agent is
sufficiently effective when the present compound is used alone as an active ingredient.
However, the present pest control agent may be mixed or used in combination, as necessary,
with other fertilizers and agricultural chemicals such as insecticide, miticide, nematicide,
synergist, fungicide, antiviral agent, attractant, herbicide, plant growth-controlling agent, and
the like. In this case, a more excellent effect can be exhibited.
[0603] Below are shown examples of known insecticides, miticides,
nematicides, and synergist compounds, which may be mixed or used in combination.
[0604] Insecticide active ingredients:
acrinathrin, azadirachtin, azamethiphos, acynonapyr, azinphos-ethyl, azinphos
methyl, acequinocyl, acetamiprid, acetoprole, acephate, azocyclotin, abamectin, afidopyropen,
afoxolaner, amidoflumet, amitraz, alanycarb, aldicarb, aldoxycarb, allethrin [including d-cis
trans-form, and d-trans-form], isazophos, isamidofos, isocarbophos, isoxathion,
isocycloseram, isofenphos-methyl, isoprocarb, epsilon-metofluthrin, epsilon-momfluorothrin,
ivermectin, imicyafos, imidacloprid, imiprothrin, indoxacarb, esfenvalerate, ethiofencarb,
ethion, ethiprole, ethylene dibromide, etoxazole, etofenprox, ethoprophos, etrimfos,
emamectin, emamectin benzoate, endosulfan, empenthrin, oxazosulfyl, oxamyl, oxydemeton
methyl, oxydeprofos, omethoate, cadusafos, kappa-tefluthrin, kappa-bifenthrin, karanjin,
cartap, carbaryl, carbosulfan, carbofuran, gamma-BHC, xylylcarb, quinalphos, kinoprene,
chinomethionat, coumaphos, cryolite, clothianidin, clofentezine, chromafenozide,
chlorantraniliprole, chlorethoxyfos, chlordane, chloropicrin, chlorpyrifos, chlorpyrifos-methyl,
chlorfenapyr, chlorfenvinphos, chlorfluazuron, chlormephos, chloroprallethrin, cyazypyr,
cyanophos, diafenthiuron, diamidafos, cyantraniliprole, dienochlor, cyenopyrafen,
dioxabenzofos, diofenolan, cyclaniliprole, cycloxaprid, dicrotophos, dichlofenthion,
cycloprothrin, dichlorvos, dicloromezotiaz, dicofol, dicyclanil, disulfoton, dinotefuran,
dinobuton, cyhalodiamide, cyhalothrin [including gamma-form, and lambda-form], cyphenothrin [including (1R)-trans-form], cyfluthrin) [including beta-form], diflubenzuron, cyflumetofen, diflovidazin, cyhexatin, cypermethrin [including alpha-form, beta-form, theta form, and zeta-form], dimpropyridaz, dimethyl-2,2,2-trichloro-1-hydroxyethyl phosphate
(DEP), dimethylvinphos, dimethoate, dimefluthrin, silafluofen, cyromazine, spinetoram,
spinosad, spirodiclofen, spirotetramat, spiropidion, spiromesifen, sulcofuron-sodium,
sulfluramid, sulfoxaflor, sulfotep, diazinon, thiacloprid, thiamethoxam, tioxazafen, thiodicarb,
thiocyclam, thiosultap, thionazin, thiofanox, thiometon, tyclopyrazoflor,
tetrachlorantraniliprole, tetrachlorvinphos, tetradifon, tetraniliprole, tetramethylfluthrin,
tetramethrin, tebupirimfos, tebufenozide, tebufenpyrad, tefluthrin, teflubenzuron, demeton-S
methyl, temephos, deltamethrin, terbufos, tralomethrin, transfluthrin, triazamate, triazophos,
trichlorfon, triflumuron, triflumezopyrim, trimethacarb, tolfenpyrad, naled, nicotine,
nitenpyram, nemadectin, novaluron, noviflumuron, Verticillium lecanii, hydroprene, Bacillus
sphaericus, Bacillus subtillis, Bacillus thuringiensis, insect toxin produced by Bacillus
thuringiensis, Bacillus thuringiensis subsp. Aizawai, Bacillus thuringiensis subsp. Israelensis,
Bacillus thuringiensis subsp. Kurstaki, Bacillus thuringiensis subsp. Tenebrionis, Bacillus
popilliae, Pasteuriapenetrans spore, vamidothion, parathion, parathion-methyl, halfenprox,
halofenozide, bioallethrin, bioallethrin S-cyclopentenyl, bioresmethrin, bis-(2-chloro-1
methylethyl)ether (DCIP), bistrifluron, hydramethylnon, bifenazate, bifenthrin, pyflubumide,
piperonyl butoxide, pymetrozine, pyraclofos, pyrafluprole, pyridaphenthion, pyridaben,
pyridalyl, pyrifluquinazon, pyriprole, pyriproxyfen, pirimicarb, pyrimidifen, pyriminostrobin,
pirimiphos-methyl, pyrethrine, famphur, fipronil, fenazaquin, fenamiphos, fenitrothion,
fenoxycarb, fenothiocarb, phenothrin [including (R)-trans-form], fenobucarb, fenthion,
phenthoate, fenvalerate, fenpyroximate, fenbutatin oxide, fenpropathrin, fonofos, sulfuryl
fluoride, butocarboxim, butoxycarboxim, buprofezin, furathiocarb, prallethrin, fluacrypyrim,
fluazaindolizine, fluazuron, fluensulfone, fluopyram, sodium fluoroacetate, fluxametamide,
flucycloxuron, flucythrinate, flusulfamide, fluthrin, fluvalinate [including tau-form],
flupyradifurone, flupyrazofos, flupyrimin, flufiprole, flufenerim, flufenoxystrobin,
flufenoxuron, fluhexafon, flubendiamide, flumethrin, fluralaner, flurimfen, prothiofos, protrifenbute, flonicamid, propaphos, propargite, profenofos, broflanilide, profluthrin, propetamphos, propoxur, flometoquin, bromopropylate, hexythiazox, hexaflumuron,
Pacilimyces tenuipes, Paecilomyces fumosoroceus, heptafluthrin, heptenophos, permethrin,
benclothiaz, benzpyrimoxan, bensultap, benzoximate, bendiocarb, benfuracarb, Beauveria
tenella, Beauveria bassiana, Beauveria brongniartii, phoxim, phosalone, fosthiazate, fosthietan,
phosphamidon, phosmet, polynactins, formetanate, phorate, machine oil, malathion,
milbemectin, mecarbam, mesulfenfos, methomyl, metaldehyde, metaflumizone,
methamidophos, metham, methiocarb, methidathion, methyl isothiocyanate, methyl bromide,
methoxychlor, methoxyfenozide, methothrin, metofluthrin, methoprene, metolcarb,
mevinphos, meperfluthrin, Monacrosporium phymatophagum, monocrotophos,
momfluorothrin, litlure-A, litlure-B, aluminium phosphide, zinc phosphide, phosphine,
lufenuron, rescalure, resmethrin, lepimectin, rotenone, nuclear polyhedrosis virus silkworm
embedded form, fenbutatin oxide, calcium cyanide, organotins, nicotine-sulfate, (Z)-11
tetradecenyl=acetate, (Z)-11-hexadecenal, (Z)-11-hexadecenyl=acetate, (Z)-9,12
tetradecadienyl=acetate, (Z)-9-tetradecene-1-ol, (Z,E)-9,11-tetradecadienyl=acetate, (Z,E)
9,12-tetradecadienyl=acetate, 1,1,1-trichloro-2,2-bis(4-chlorophenyl)ethane (DDT), 1,3
dichloropropene(1,3-dichloropropene), 2,4-dichloro-5-{2-[4
(trifluoromethyl)phenyl]ethoxy}phenyl 2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS
registry number: 1472050-04-6), 2,4-dichloro-5-{2-[4-(trifluoromethyl)phenyl]ethoxy}pheny
2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry number: 1472052-11-1), 2,4
dimethyl-5-[6-(trifluoromethylthio)hexyloxy]phenyl-2,2,2-trifluoroethyl sulfoxide (Chemical
name, CAS registry number: 1472050-34-2), 2-{2-fluoro-4-methyl-5-[(2,2,2
trifluoroethyl)sulfinyl]phenoxy}-5-(trifluoromethy)pyridine (Chemical name, CAS registry
number: 1448758-62-0), 3-chloro-2-{2-fluoro-4-methyl-5-[(2,2,2
trifluoroethyl)sulfinyl]phenoxy}-5-(trifluoromethyl)pyridine (Chemical name, CAS registry
number: 1448761-28-1), 4,6-dinitro-o-cresol (DNOC), 4-fluoro-2-methyl-5-(5,5
dimethylhexyloxy]phenyl-2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry
number: 1472047-71-4), Bt protein (CrylAb, CrylAc, CrylFa, Cry2Ab, mCry3A, Cry3Ab,
Cry3Bb, Cry34/35Abl), CL900167 (code number), NA-85 (code number), NI-30 (code
number), O,0-diethyl-O-[4-(dimethylsulfamoyl)phenyl]-phosphorothioate(DSP), O-ethyl-O
4-(nitrophenyl)phenylphosphonothioate (EPN), RU15525 (code number), XMC(XMC), Z-13
icosen-10-one, ZX18901 (code number).
[0605] Next, examples of known bactericides or disease controller
compounds that can be mixed or used in combination are shown below.
[0606] Bactericide active ingredients:
azaconazole, acibenzolar-S-methyl, azoxystrobin, anilazine, amisulbrom,
aminopyrifen, ametoctradin, aldimorph, isotianil, isopyrazam, isofetamid, isoflucypram,
isoprothiolane, ipconazole, ipflufenoquin, ipfentrifluconazole, iprodione, iprovalicarb,
iprobenfos, imazalil, iminoctadine-albesilate, iminoctadine-triacetate, imibenconazole,
inpyrfluxam, imprimatin A, imprimatin B, edifenphos, etaconazole, ethaboxam, ethirimol,
ethoxyquin, etridiazole, enestroburin, enoxastrobin, epoxiconazole, organic oils, oxadixyl,
oxazinylazole, oxathiapiprolin, oxycarboxin, oxine-copper, oxytetracycline, oxpoconazole
fumarate, oxolinic acid, copper dioctanoate, octhilinone, ofurace, orysastrobin, o
phenylphenol, kasugamycin, captafol, carpropamid, carbendazim, carboxin, carvone,
quinoxyfen, quinofumelin, chinomethionat, captan, quinconazole, quintozene, guazatine,
cufraneb, coumethoxystrobin, coumoxystrobin, kresoxim-methyl, clozylacon, chlozolinate,
chlorothalonil, chloroneb, cyazofamid, diethofencarb, diclocymet, dichlofluanid,
dichlobentiazox, diclomezine, dicloran, dichlorophen, dithianon, diniconazole, diniconazole
M, zineb, dinocap, dipymetitrone, diphenylamine, difenoconazole, cyflufenamid,
diflumetorim, cyproconazole, cyprodinil, simeconazole, dimethirimol, dimethyl disulfide,
dimethomorph, cymoxanil, dimoxystrobin, Pseudomonas rhodesiae HAI-0804, ziram,
silthiofam, streptomycin, spiroxamine, sedaxane, zoxamide, solatenol, dazomet, Talaromyces
flavus, tiadinil, thiabendazole, thiram, thiophanate, thiophanate-methyl, thifluzamide, thiram,
tecnazene, tecloftalam, tetraconazole, debacarb, tebuconazole, tebufloquin, terbinafine,
dodine, dodemorph, triadimenol, triadimefon, triazoxide, trichlamide, triclopyricarb,
Trichoderma atroviride, tricyclazole, triticonazole, tridemorph, triflumizole, trifloxystrobin, triforine, tolylfluanid, tolclofos-methyl, tolnifanide, tolprocarb, nabam, natamycin, naftifine, nitrapyrin, nitrothal-isopropyl, nuarimol, copper nonyl phenol sulphonate, Bacillus subtilis)(strain: QST 713, validamycin, valifenalate, picarbutrazox, bixafen, picoxystrobin, pydiflumetofen, bitertanol, binapacryl, hinokitiol, biphenyl, piperalin, hymexazol, pyraoxystrobin, pyraclostrobin, pyraziflumid, pyrazophos, pyrapropoyne, pyrametostrobin, pyriofenone, pyrisoxazole, pyridachlometyl, pyrifenox, pyributicarb, pyribencarb, pyrimethanil, pyroquilon, vinclozolin, ferbam, famoxadone, phenazine oxide, fenamidone, fenaminstrobin, fenarimol, fenoxanil, ferimzone, fenpiclonil, fenpicoxamid, fenpyrazamine, fenbuconazole, fenfuram, fenpropidin, fenpropimorph, fenhexamid, folpet, phthalide, bupirimate, fuberidazole, blasticidin-S, furametpyr, furalaxyl, furancarboxylic acid, fluazinam, fluindapyr, fluoxastrobin, fluoxapiprolin, fluopicolide, fluopimomide, fluopyram, fluoroimide, fluxapyroxad, fluquinconazole, furconazole, furconazole -cis, fludioxonil, flusilazole, flusulfamide, flutianil, flutolanil, flutriafol, flufenoxystrobin, flumetover, flumorph, proquinazid, prochloraz, procymidone, prothiocarb, prothioconazole, bronopol, propamocarb hydrochloride, propiconazole, propineb, probenazole, bromuconazole, flometoquin, florylpicoxamid, hexaconazole, benalaxyl, benalaxyl-M, benodanil, benomyl, pefurazoate, penconazole, pencycuron, benzovindiflupyr, benthiazole, benthiavalicarb-isopropyl, penthiopyrad, penflufen, boscalid, fosetyl (alminium, calcium, sodium), polyoxin, polycarbamate, Bordeaux mixture, mancopper, mancozeb, mandipropamid, mandestrobin, maneb, myclobutanil, mineral oils, mildiomycin, methasulfocarb, metam, metalaxyl, metalaxyl-M, metiram, metyltetraprole, metconazole, metominostrobin, metrafenone, mepanipyrim, mefentrifluconazole, meptyldinocap, mepronil, iodocarb, laminarin, Rhizobium vitis, phosphorous acid and salts, copper oxychloride, silver, cuprous oxide, copper hydroxide, potassium bicarbonate, sodium bicarbonate, sulfur, oxyquinoline sulfate, copper sulfate, (3,4 dichloroisothiazole-5-yl)methyl 4-(tert-butyl)benzoic ester (Chemical name, CAS registry number: 1231214-23-5), BAF-045 (code number), BAG-010 (code number), UK-2A (code number), dodecylbenzenesulfonic acid bisethylenediamine copper [II] salt (DBEDC), MIF
1002 (code number), NF-180 (code number), triphenyltin acetate (TPTA), triphenyltin chloride (TPTC), triphenyltin hydroxide (TPTH), avirulent Erwinia carotovora.
[0607] Next, examples of known herbicides or plant growth regulator
compounds that can be mixed or used in combination are shown below.
[0608] Herbicide active ingredients:
ioxynil, aclonifen, acrolein, azafenidin, acifluorfen (including a salt with sodium
or the like), azimsulfuron, asulam, acetochlor, atrazine, anilofos, amicarbazone,
amidosulfuron, amitrole, aminocyclopyrachlor, aminopyralid, amiprofos-methyl, ametryn,
alachlor, alloxydim, ancymidol, isouron, isoxachlortole, isoxaflutole, isoxaben,
isodecylalkoholethoxylate, isoproturon, ipfencarbazone, imazaquin, imazapic (including a salt
with amine or the like), imazapyr (including a salt of isopropylamine or the like),
imazamethabenz-methyl, imazamox, imazethapyr, imazosulfuron, indaziflam, indanofan,
eglinazine-ethyl, esprocarb, ethametsulfuron-methyl, ethalfluralin, ethidimuron,
ethoxysulfuron, ethoxyfen-ethyl, ethofumesate, etobenzanid, endothal-disodium, oxadiazon,
oxadiargyl, oxaziclomefone, oxasulfuron, oxyfluorfen, oryzalin, orthosulfamuron, orbencarb,
oleic acid, cafenstrole, carfentrazone-ethyl, karbutilate, carbetamide, quizalofop, quizalofop
ethyl, quizalofop-P-ethyl, quizalofop-P-tefuryl, quinoclamine, quinclorac, quinmerac,
cumyluron, clacyfos, glyphosate (including a salt of sodium, potassium, amine, propylamine,
isopropylamine, dimethylamine, trimesium, or the like), glufosinate (including a salt of amine,
sodium, or the like), glufosinate-P, glufosinate-P-sodium, clethodim, clodinafop-propargyl,
clopyralid, clomazone, chlomethoxyfen, clomeprop, cloransulam-methyl, chloramben,
chloridazon, chlorimuron-ethyl, chlorsulfuron, chlorthal-dimethyl, chlorthiamid,
chlorphthalim, chlorflurenol-methyl, chlorpropham, chlorbromuron, chloroxuron,
chlorotoluron, ketospiradox (including a salt of sodium, calcium, ammonia, or the like),
saflufenacil, sarmentine, cyanazine, cyanamide, diuron, diethatyl-ethyl, dicamba (including a
salt of amine, diethylamine, isopropylamine, diglycolamine, sodium, lithium, or the like),
cycloate, cycloxydim, diclosulam, cyclosulfamuron, cyclopyranil, cyclopyrimorate,
dichlobenil, diclofop-P-methyl, diclofop-methyl, dichlorprop, dichlorprop-P, diquat, dithiopyr,
siduron, dinitramine, cinidon-ethyl, cinosulfuron, dinoseb, dinoterb, cyhalofop-butyl, diphenamid, difenzoquat, diflufenican, diflufenzopyr, simazine, dimethachlor, dimethametryn, dimethenamid, dimethenamid-P, simetryn, dimepiperate, dimefuron, cinmethylin, swep, sulcotrione, sulfentrazone, sulfosate, sulfosulfuron, sulfometuron-methyl, sethoxydim, terbacil, daimuron, thaxtomin A, dalapon, thiazopyr, tiafenacil, thiencarbazone (including sodium salt, methyl ester, or the like), tiocarbazil, thiobencarb, thidiazimin, thidiazuron, thifensulfuron-methyl, desmedipham, desmetryne, tetflupyrolimet, thenylchlor, tebutam, tebuthiuron, tepraloxydim, tefuryltrione, terbuthylazine, terbutryn, terbumeton, tembotrione, topramezone, tralkoxydim, triaziflam, triasulfuron, triafamone, tri-allate, trietazine, triclopyr, triclopyr-butotyl, tritosulfuron, trifludimoxazin, triflusulfuron-methyl, trifluralin, trifloxysulfuron-sodium, tribenuron-methyl, tolpyralate, naptalam (including a salt with sodium or the like), naproanilide, napropamide, napropamide-M, nicosulfuron, neburon, norflurazon, vernolate, paraquat dichloride, halauxifen-benzyl, halauxifen-methyl, haloxyfop, haloxyfop-P, haloxyfop-etotyl, halosafen, halosulfuron-methyl, bixlozone, picloram, picolinafen, bicyclopyrone, bispyribac-sodium, pinoxaden, bifenox, piperophos, pyraclonil, pyrasulfotole, pyrazoxyfen, pyrazosulfuron-ethyl, pyrazolynate, bilanafos, pyraflufen-ethyl, pyridafol, pyrithiobac-sodium, pyridate, pyriftalid, pyributicarb, pyribenzoxim, pyrimisulfan, pyriminobac-methyl, pyroxasulfone, pyroxsulam, phenisopham, fenuron, fenoxasulfone, fenoxaprop (including methyl, ethyl, isopropylester), fenoxaprop-P (including methyl, ethyl, isopropyl ester), fenquinotrione, fenthiaprop-ethyl, fentrazamide, phenmedipham, foramsulfuron, butachlor, butafenacil, butamifos, butylate, butenachlor, butralin, butroxydim, flazasulfuron, flamprop (including methyl, ethyl, isopropyl ester), flamprop-M (including methyl, ethyl, isopropyl ester), primisulfuron-methyl, fluazifop-butyl, fluazifop-P-butyl, fluazolate, fluometuron, fluoroglycofen-ethyl, flucarbazone-sodium, fluchloralin, flucetosulfuron, fluthiacet-methyl, flupyrsulfuron-methyl (including a salt of sodium, calcium, ammonia, or the like), flufenacet, flufenpyr-ethyl, flupropanate, flupoxame, flumioxazin, flumiclorac-pentyl, flumetsulam, fluridone, flurtamone, fluroxypyr (including an ester such as butomethyl or meptyl, a salt of sodium, calcium, ammonia, or the like), flurochloridone, pretilachlor, procarbazone-sodium, prodiamine, prosulfuron, prosulfocarb, propaquizafop, propachlor, propazine, propanil, propyzamide, propisochlor, propyrisulfuron, propham, profluazol, prohexadione-calcium, propoxycarbazone, propoxycarbazone-sodium, profoxydim, bromacil, brompyrazon, prometryn, prometon, bromoxynil (including an ester of butyric acid, octanoic acid, heptanoic acid, or the like), bromofenoxim, bromobutide, florasulam, florpyrauxifen, florpyrauxifen benzyl, hexazinone, pethoxamid, benazolin, penoxsulam, heptamaloxyloglucan, beflubutamid, beflubutamid-M, pebulate, pelargonic acid, bencarbazone, pendimethalin, benzfendizone, bensulide, bensulfuron-methyl, benzobicyclon, benzofenap, bentazone, pentanochlor, pentoxazone, benfluralin, benfuresate, fosamine, fomesafen, foramsulfuron, forchlorfenuron, mecoprop (including a salt of sodium, potassium, isopropylamine, triethanolamine, dimethylamine, or the like), mecoprop-P-potassium, mesosulfuron (including an ester of methyl or the like), mesotrione, metazachlor, metazosulfuron, methabenzthiazuron, metamitron, metamifop, metam, disodium methanearsonate (DSMA), methiozolin, methyldymuron, metoxuron, metosulam, metsulfuron-methyl, metobromuron, metobenzuron, metolachlor, metribuzin, mepiquat chloride, mefenacet, monosulfuron (including methyl, ethyl, isopropylester), monolinuron, molinate, iodosulfuron, iodosulfulon-methyl-sodium, iofensulfuron, iofensulfuron-sodium, lactofen, lancotrione, linuron, rimsulfuron, lenacil,
2,2,2-trichloroacetic acid (TCA) (including a salt of sodium, calcium, ammonia, or the like),
2,3,6-trichlorobenzoic acid (2,3,6-TBA), 2,4,5-trichlorophenoxyacetic acid (2,4,5-T), 2,4
dichlorophenoxyacetic acid (2,4-D) (including a salt of amine, diethylamine, triethanolamine,
isopropylamine, sodium, lithium, or the like), 2-amino-3-chloro-1,4-naphthoquinone (ACN),
2-methyl-4-chlorophenoxyacetic acid (MCPA) (including a sodium salt, ethyl ester, or the
like), 2-methyl-4-chlorophenoxyacetic acid (MCPB) (including a sodium salt, ethyl ester, or
the like), 4-(2,4-dichlorophenoxy)butyric acid (2,4-DB), 4,6-dinitro-O-cresol (DNOC)
(including a salt of amine, sodium, or the like), AE-F-150944 (code number), IR-6396 (code
number), MCPA-thioethyl, SYP-298 (code number), SYP-300 (code number), S
ethyldipropylthiocarbamate (EPTC), S-metolachlor, S-9750 (code number), MSMA, HW-02
(code number).
[0609] Plant growth regulators:
1-naphthylacetamide, 1-methylcyclopropene, 2,6-diisopropylnaphthalene, 4-oxo
4-(2-phenylethyl)aminobutyric acid (Chemical name, CAS registry number: 1083-55-2), 4
chlorophenoxyacetic acid (4-CPA), n-decanol, aviglycine, ancymidol, abscisic acid,
inabenfide, indole acetic acid, indole butyric acid, uniconazole, uniconazole-P, Ecolyst,
ethychlozate, ethephon, epocholeone, oxine-sulfate, carvone, calcium formate, cloxyfonac,
cloxyfonac-potassium, cloprop, chlormequat, choline, cytokinins, cyclanilide, dikegulac,
gibberellin acid, dimethipin, sintofen, daminozide, thidiazuron, triacontanol, trinexapac-ethyl,
paclobutrazol, paraffin, flumetralin, flurprimidol, flurenol, prohydrojasmon, prohexadione
calcium, heptamaloxyloglucan, benzylaminopurine, forchlorfenuron, maleic hydrazide,
mepiquat chloride, mefluidide, calcium peroxide.
[0610] Next, examples of known phytotoxicity alleviating compounds that
can be mixed or used in combination are shown below.
[0611] Isoxadifen, isoxadifen-ethyl, oxabetrinil, cloquintcet-mexyl,
dietholate, cyometrinil, dichlormid, dicyclonone, cyprosulfamide, 1,8-Naphthalic Anhydride,
fenchlorazole-O-ethyl, fenclorim, furilazole, fluxofenim, flurazole, benoxacor, mephenate,
mefenpyr, mefenpyr-ethyl, mefenpyr-diethyl, lower alkyl-substituted benzoic acid, 2,2
dichloro-N-(1,3-dioxane-2-ylmethyl)-N-(2-propenyl)acetamide(PPG-1292), 2
dichloromethyl-2-methyl-1,3-dioxane(MG-191),3-dichloroacetyl-2,2,5-trimethyl-1,3
oxazolidine (R-29148), 4-dichloroacetyl-1-oxa-4-azaspiro[4.5]decane (AD-67), MON4660
(code number), metcamifen, Ni,N2-diallyl-N2-dichloroacetyl glycineamide (DKA-24), TI-35
(code number).
[0612] The present pest control agent configured as described above exhibits
excellent controlling effect on Orthoptera pests, Thysanoptera pests, Hemiptera pests,
Coleoptera pests, Diptera pests, Lepidoptera pests, Hymenoptera pests, Collembola pests,
Thysanura pests, Blattodea pests, Isoptera pests, Psocoptera pests, Mallophage pests,
Anoplura pests, plant parasitic Acari, plant parasitic nematoda, plant parasitic mollusks, and
other pests such as harmful animals, uncomfortable animals, sanitary insects, and parasites.
As such pests, the following organism species can be exemplified.
[0613] Examples of the Orthopteran pests include Ruspolia lineosa or the like
of Tettigoniidae, Teleogryllus emma, Truljalia hibinonis, or the like of Gryllidae, Gryllotalpa
orientalis or the like of Gryllotalpidae, Oxya hyla intricate, Locusta migratoria, Melanoplus
sanguinipes, Melanoplus differentialis, Melanoplus femurrubrum, or the like of Acrididae,
Atractomorpha lata of Pyrgomorphidae, Euscyrtus japonicus of Eneopteridae, and Xya
japonicus or the like of Tridactylidae.
[0614] Examples of the Thysanoptera pests include Frankliniella intonsa,
Frankliniella occidentalis, Scirtothrips dorsalis, Thrips palmi, Thrips tabaci, Thrips setosus,
Heliothrips haemorrhoidalis, Stenchaetothrips biformis, or the like of Thripidae, and
Ponticulothrips diospyrosi, Liothrips wasabiae, Haplothrips aculeatus, or the like of
Phlaeothripidaes.
[0615] Examples of the Hemipteran pests include Mogannia minuta or the
like of Cicadidae, Aphrophora intermedia or the like of Aphrophoridae, Machaerotypus
sibiricus or the like of Membracidae, Arboridia apicalis, Empoasca onukii, Nephotettix
cincticeps, Nephotettix malayanus, Nephotettix virescens, Nephotettix nigropictus, Recilia
dorsalis, Okura Leafhopper (Amrasca biguttula), Mango Leafhopper (Idioscopus nitidulus,
Idioscopus clypealis, Amritodus atkinsoni), Recilia dorsalis, Empoasca fabae, or the like of
Cicadellidae, Pentastiridius apicalis or the like of Cixiidae, Laodelphax striatellus, Nilaparvata
lugens, Sogatella furcifera, or the like of Delphacidae, Nisia nervosa or the like of
Meenoplidae, Kamendaka saccharivora or the like of Derbidae, Achilus flammeus or the like
of Cixidia, Orosanga japonicus or the like of Ricaniidae, Mimophantia maritima or the like of
Flatidae, Cacopsylla pyrisuga, Diaphorina citri, or the like of Psyllidae, Calophya mangiferae
or the like of Calophyidae, Daktulosphaira vitifoliae or the like of Phylloxeridae, Adelges
laricis, Adelges tsugae, or the like of Adelgidae, Acyrthosiphon pisum, Aphis gossypii, Aphis
spiraecola, Lipaphis erysimi, Brevicoryne brassicae, Myzuspersicae, Schizaphis graminum,
Rhopalosiphum padi, Toxoptera aurautii, Aulacorthum solani, Macrosiphum euphorbiae,
Nasonovia ribisnigri, Sitobion avenae, Aphis glycines, or the like of Aphydidae,
Aleurocanthus camelliae, Aleurocanthus spiniferus, Bemisia tabaci, Bemisia argentifolii,
Trialeurodes vaporariorum, or the like of Aleyrodidae, Drosicha corpulenta, Icerya purchasi,
or the like of Margarodidae, Dysmicoccus brevipes, Planococcus citri, Pseudococcus
comstocki, or the like of Pseudococcidae, Ceroplastes ceriferus, Ceroplastes rubens, or the
like of Coccidae, Aclerda takahashii or the like of Aclerdidae, Aonidiella aurantii,
Diaspidiotus perniciosus, Pseudaulacaspis pentagoa, Unaspis yanonensis, or the like of
Diaspididae, Lygus lineolaris, Trigonotylus caelestialium, Apolygus lucorum, Nesidiocoris
tenuis, Halticus bractatus, or the like of Miridae, Stephanitis pyrioides, Stephanitis nashi, or
the like of Tingidae, Eurydema rugosum, Eysarcoris lewisi, Eysarcoris aeneus, Lagynotomus
elongatus, Nezara viridula, Plautia crossota, Nezara antennata, Eushistus heros, or the like of
Pentatomidae, Megacopta cribraria or the like of Plataspidae, Urochela luteovoria or the like
of Urostylididae, Cavelerius saccharivorus or the like of Lygaeidae, Malcus japonicus or the
like of Malcidae, Dysdercus cingulatus or the like of Pyrrhocoridae, Leptocorisa acuta,
Leptocorisa chinensis, or the like of Alydidae, Anacanthocoris striicornis or the like of
Coreidae, Rhopalus maculatus or the like of Rhopalidae, and Cimex lectularis or the like of
Cimicidae.
[0616] Examples of the Coleoptera pests include Anomara cuprea, Anomara
rufocuprea, Popilliajaponica, Oxycetoniajucunda, Anomala geniculata, Oryctes rhinoceros,
Heptophylla picea, or the like of Scarabaeidae, Agriotes ogurae, Agriotes lineatus, Agriotes
obscurus, Melanotus okinawensis, Melanotus fortnumi, or the like of Elateridae, Anthrenus
verbasci or the like of Dermestidae, Heterobostrychus hamatipennis or the like of
Bostrychidae, Stegobium paniceum or the like of Anobiidae, Pitinus clavipes or the like of
Ptinidae, Tenebroides mauritanicus or the like of Trogossitidae, Necrobia rufipes of Cleridae,
Carpophilus hemipterus, Meligethes aeneus, or the like of Nitidulidae, Ahasverus advena or
the like of Silvanidae, Cryptolestes ferrugineus or the like of Laemophloeidae, Epilachna
varivestis, Henosepilachna vigintioctopunctata or the like of Coccinellidae, Tenebrio molitor,
Tribolium castaneum, or the like of Tenebrionidae, Epicauta gorhami or the like of Meloidae,
Anoplophora glabripennis, Xylotrechus pyrrhoderus, Monochamus alternatus, Dectes texanus, or the like of Cerambycidae, Callosobruchus chinensis or the like of Bruchidae, Leptinotarsa decemlineata, Diabrotica virgifera virgifera, Diabrotica barberi, Diabrotica undecimpunctata howardi, Aulacophora femoralis, Phaedon brassicae, Cassida nebulosa, Oulema oryzae,
Epilachna varivestis, Phyllotreta striolata, Demotina fasciculata, Psylliodes chrysocephala,
Cerotoma trifurcate, Colaspis brunnea, Colaspis crinnicornis, Odontota horni, Chaetocnema
pulicaria, or the like of Chrysomelidae, Cylas formicarius or the like of Brentidae, Hypera
postica, Listroderes costirostris, Euscepes postfasciatus, Curculio sikkimensis, or the like of
Curculionidae, Echinocnemus bipunctatus, Lissorhoptrus oryzophilus, Oryzophagus oryzae,
or the like of Erirhinidae, Sitophilus zeamais, Sphenophrus venatus, or the like of
Dryophthoridae, Tomicus piniperda or the like of Scolytidae, Crossotarsus niponicus or the
like of Platypodidae, and Lyctus brunneus or the like of Lyctidae.
[0617] Examples of the Diptera pests include Tipula aino or the like of
Tipulidae, Plecia nearctica or the like of Bibionidae, Exechia shiitakevora or the like of
Mycetophidae, Pnyxiascabiei, Bradysia agrestis, or the like of Sciaridae, Asphondylia
yushimai, Mayetiola destructor, Dasineura oxycoccana, or the like of Cecidomyiidae, Aedes
aegypti, Culex pipiens pallens, or the like of Culicidae, Simulium takahashii or the like of
Simuliidae, Chironomus oryzae or the like of Chironomidae, Chrysops suavis, Tabanus
trigonus, or the like of Tabanidae, Eumerus strigatus or the like of Syrphidae, Bactrocera
dorsalis, Euphranta japonica, Ceratitis capitata, or the like of Tephritidae, Liriomyza trifolii,
Liriomyza sativae, Agromyza oryzae, Liriomyza bryoniae, Chromatomyia horticola,
Liriomyza chinensis, Liriomyza trifolii, or the like of Agromyzidae, Meromyza nigriventris or
the like of Chloropidae, Drosophila suzukii, Drosophila melanogaster, or the like of
Drosophilidae, Hydrellia griseola or the like of Ephydridae, Hippobosca equina or the like of
Hippoboscidae, Parallelpmma sasakawae or the like of Scatophagidae, Delia antiqua, Delia
platura, or the like of Anthomyiidae, Fannia canicularis or the like of Fanniidae, Musca
domestica, Stomoxys calcitrans or the like of Muscidae, Sarcophaga peregrina or the like of
Sarcophagidae, Gasterophilus intestinalis or the like of Gasterophilidae, Hypoderma lineatum
or the like of Hypodermatidae, and Oestrus ovis or the like of Oestridae.
[0618] Examples of the Lepidoptera pests include Endoclita excrescens or
the like of Hepialidae, Antispila ampelopsia or the like of Heliozelidae, Zeuzera leuconotum,
Cossus insularis, or the like of Cossidae, Archips fuscocupreanus, Adoxophyes orana fasciata,
Grapholita molesta, Homona magnanima, Leguminivora glycinivorella, Cydia pomonella,
Lobesia botrana, or the like of Tortricidae, Eupoecilia ambiguella or the like of Cochylidae,
Bambalina sp., Eumeta minuscula, or the like of Psychidae, Nemapogon granella, Tinea
translucens, or the like of Tineidae, Bucculatrix pyrivorella or the like of Bucculatricidae,
Lyonetia clerkella, Lyonetiaprunifoliella malinella, or the like of Lyonetiidae, Caloptilia
theivora, Phyllonorycter ringoniella, or the like of Gracilariidae, Phyllocnistis citrella or the
like of Phyllocnistidae, Acrolepiopsis sapporensis or the like of Acrolepiidae, Plutella
xylostella of Plutellidae, Yponomeuta orientalis, or the like of Yponomeutidae, Argyresthia
conjugella or the like of Argyresthidae, Nokona regalis, Synanthedin hector or the like of
Sesidae, Phthorimaea operculella, Sitotroga cerealella, Pectinophora gossypiella, Tuta
absoluta, or the like of Gelechiidae, Carposina sasakii or the like of Carposinidae, Illiberis
pruni or the like of Zygaenidae, Monema flavescens or the like of Limacodidae, Ancylolomia
japonica, Chilo suppressalis, Cnaphalocrocis medinalis, Ostrinia furnacalis, Hellulla undalis,
Conogethes punctiferlis, Diaphania indica, Parapediasia teterrella, Ostrinia nubilalis, or the
like of Crambidae, Diatraea saccharalis, Cadra cautella, Galleria mellonella, or the like of
Pyralidae, Nippoptilia vitis or the like of Pterophoridae, Papilio xuthus or the like of
Papilionidae, Pieris rapae or the like of Pieridae, Parnara guttata or the like of Hesperiidae,
Ascotis selenaria or the like of Geometridae, Dendrolimus spectabilis, Malacosoma neustrium
testaceum, or the like of Lasiocampidae, Agrius convolvuli or the like of Sphingidae, Arna
pseudoconspersa, Orygia recens approximans, Lymantria dispar, or the like of Lymantriidae,
Hyphantria cunea or the like of Arctiidae, and Agrotis ipsilon, Agrotis segetum, Autographa
nigrisigna, Helicoverpa armigera, Helicoverpa zea, Heliothis virescens, Spodoptera exigua,
Spodoptera litura, Chrysodeix includens, Spodoptera frugiperda, Nephelodes minians, or the
like of Noctuidae.
[0619] Examples of the Hymenoptera pests include Arge pagana or the like of Argidae, Apethymus kuri, Athalia rosae ruficornis, or the like of Tenthredinidae,
Dryocosmus kuriphilus, or the like of Cynipidae, Vespa simillima xanthoptera or the like of
Vespidae, Solenopsis invicta, Linepithema humile, or the like of Formicidae, and Megachile
nipponica or the like of Megachilidae.
[0620] Examples of the Collembola pests include Bourletiellahortensis or the
like of Sminthuridae.
[0621] Examples of the Thysanura pests include Lepisma saccharina,
Ctenolepisma villosa, or the like of Lepismatidae.
[0622] Examples of the Blattodea pests include Periplaneta americana of
Blattidae, and Blattella germanica or the like of Blattellidae.
[0623] Examples of the Isoptera pests include Incisitermes minor or the like
of Kalotermitidae, Coptotermes formosanus or the like of Rhinotermitidae, and Odontotermes
formosanus or the like of Termitidae.
[0624] Examples of the Psocoptera pests include Trogium pulsatorium or the
like of Trogiidae, and Liposcelis corrodens or the like of Liposcelididae.
[0625] Examples of the Dermaptera pests include Labodura riparia or the like
of Labiduridae.
[0626] Examples of the Mallophaga pests include Lipeurus caponis or the
like of Menoponidae, and Damalinia bovis or the like of Trichodectidae.
[0627] Examples of the Anoplura pests include Haematopinus suis or the like
of Haematopinidae, Pediculus humanus or the like of Pediculine, Linognathus setosus or the
like of Linognathidae, and Pthirus pubis or the like of Pthiridae
[0628] Examples of the Acari pests include Penthaleus major or the like of
Eupodidae, Phytonemus pallidus, Polyphagotarsonemus latus, or the like of Tarsonemidae,
one species of Siteroptes sp. or the like of Pyemotidae, Brevipalpus lewisi or the like of
Tenuipalpidae, Tuckerella pavoniformis or the like of Tuckerellidae, Eotetranychusboreus,
Panonychus citri, Panonychus ulmi, Tetranychus urticae, Tetranychus kanzawai, or the like of
Tetranychidae, Trisetacus pini or the like of Nalepellidae, Aculops pelekassi, Epitrimerus pyri,
Phyllocoptruta oleivora, Aculops lycopersici, or the like of Eriophyidae, Diptacus crenatae or
the like of Diptilomiopida, Aleuroglyphus ovatus, Tyrophagus putrescentiae, or Rhizoglyphus
robini of Acaridae, Varroajacobsoni or the like of Varroidae, Dermanyssus gallinae or the
like of Dermanyssidae, Ornithonyssus sylvialum or the like of Macronyssidae, Boophilus
microplus, Rhipicephalussanguineus, Haemaphysalis longicornis, or the like of Ixodidae, and
Sarcoptes scabiei or the like of Sarcoptidae.
[0629] Examples of the plant parasitic nematoda, include Xiphinema index or
the like of Longidoridae, Paratrichodorus minor or the like of Trichodoridae, one species of
Rhabditidae (Rhabditella sp.) or the like, one species of Tylenchidae (Aglenchus sp.) or the
like, one species of Tylodoridae (Cephalenchus sp.) or the like, Nothotylenchus acris,
Ditylenchus destructor, or the like of Anguinidae, Rotylenchulus reniformis, Helicotylenchus
dihystera, or the like of Hoplolaimidae, Paratylenchus curvitatus or the like of
Paratylenchidae, Meloidogyne incognita, Meloidogyne hapla,
Meloidogynejavanica, Meloidogyne arenaria, Melidogyne chitwoodi, Meloidogyne fallax or
the like of Meloidogynidae, Globodera rostochiensis, Globodera pallida, Heterodera glycines
or the like of Heteroderidae, Tylenchorhynchus claytoni or the like of Telotylenchidae, one
species of Psilenchidae (Psilenchus sp.) or the like, one species of Criconematidae
(Criconemoides sp.) or the like, Tylenchulus semipenetrans or the like of Tylenchulidae,
Sphaeronema camelliae or the like of Sphaeronematidae, Sphaeronema camelliae,
Radopholus citrophilus, Radopholus similis, Nacobbus aberrans, Pratylenchus penetrans,
Pratylenchus coffeae, Platylechus zeae, Platylenchus brachyurus or the like of Pratylenchidae,
Iotonchium ungulatum or the like of Iotonchiidae, Aphelenchus avenae or the like of
Aphelenchidae, Aphelenchoides besseyi, Aphelenchoides fragariae, or the like of
Aphelenchoididae, and Bursaphelenchus xylophilus or the like ofPalasitaphelenchidae.
[0630] Examples of the plant parasitic mollusks include Pomacea
canaliculata or the like of Pilidae, Leavicaulis alte or the like of Veronicellidae, Achatina
fulica or the like of Achatinidae, Meghimatium bilineatum or the like of Philomycidae,
Succinealauta or the like of Succineidae, Discus pauper or the like of Didcidae, Zonitoides yessoensis or the like of Zonitidae, Limax flavus, Lehmannia valentiana, Deroceras reticulatum, or the like of Limacidae, Parakaliella harimensis or the like of Helicarionidae, and Acusta despecta sieboldiana, Bradybaena similaris, or the like of Bradybaenidae.
[0631] Examples of pests such as harmful animals, uncomfortable animals,
sanitary insects, livestock insects, and parasites include Procambarus clarkii or the like of
Decapoda Astacidae, Porcellio scaber or the like of Isopoda Porcellionidae, Chilopoda pests
such as Scutigeromorpha Sutigeridae, Scolopendra subspinipes, or the like, Diplopoda pests
such as Oxidus gracilis, Theridiidae hasseltii or the like of Araneae Latrodectus hasseltii,
Chiracanthiumjaponicum, or the like of Clubionidae, Androctonus crassicauda or the like of
Scorpiones, roundworm endoparasites such as Ascaris lumbricoides or the like, Syphacia sp.
or the like, and Wuchereria bancrofti or the like, and flatworm endoparasites such as
Distomum sp., Paragonimus westermanii, Metagonimus yokokawai, Schistosoma japonicum,
Taenia solium, Taeniarhynchus saginatus, Echinococcus sp., or Diphyllobothrium latum.
[0632] The present pest control agent exhibits a controlling effect also on the
pests and the like exemplified above that have acquired the resistance to existing
pest control agents. Furthermore, the present pest control agent can be applied to plants that
have acquired characteristics such as pest tolerance, disease tolerance, herbicide tolerance, or
the like by gene recombination, artificial mating, or the like.
[0633] The "plant provided with tolerance by a breeding method or a gene
recombination technique" in the present invention includes plants provided with tolerance by
new plant breeding techniques (NBTs) established by combining molecular biological
techniques with existing mating techniques, as well as those provided with tolerance by
classical mating, or by gene recombinant techniques. The new plant breeding techniques
(NBTs) are described in the publication "Atarashii syokubutu ikusyu wo rikaishiyo" (Kokusai
bunken sha, written by Ryo OSAWA, and Hiroshi EZURA), the review "Genome Editing
Tools in Plants" (Genes 2017,8, 399, written by Tapan Kumar Mohanta, Tufail Bashir, Abeer
Hashem, Elsayed Fathi AbdAllah and Hanhong Bae), and so on.
[0634] Next, the production methods, formulation methods and applications of the present compound will be described in detail by way of Examples. However, the present invention is in no way restricted by these Examples. The melting point which is a physical property value of the present compound was determined by a MP-500V micro melting point measuring apparatus available from Yanaco. The refractive index was determined by using an Abbe refractometer available from ATAGO CO., LTD.. 'H NMR spectrum was determined by using JNM-LA400 (400 MHz), JNM-LA300 (300 MHz) or
JNM-ECS300 (300 MHz) available from JEOL Ltd. and tetramethylsilane (TMS) as the
internal standard.
[0635] Methods for producing production intermediates of the present
compound are also described.
(Examples)
[0636] (Example 1)
Production of 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3
carboxamide (present compound number: A-0044)
[0637] 1) Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-1H
pyrazole-3-carboxylate (present compound number: D-0008)
Ethyl 4-hydroxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (15.0 g, 64.3
mmol) synthesized by the method described in Reference examples 1 and 2 of WO
2016/027790 A, triethylamine (13.0 g, 128.5 mmol), and nanofluorobutanesulfonic acid
fluoride (27.2 g, 90.0 mmol) were sequentially added into dichloromethane (300 mL) under
ice-cooling, and stirred overnight at room temperature. The reaction solution was poured
into saturated brine, and extracted with dichloromethane. The obtained organic layer was
dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced
pressure. The residue was washed with diisopropyl ether to give ethyl 4
{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (29.0 g, yield: 88%).
Melting point: 103-104°C 1H-NMR data (400 MHz, CDCl 3/TMS 6(ppm)): 1.44(3H, t), 4.50(2H, q), 7.48(H, dd), 8.08(1H, s), 8.15(1H, dd), 8.70(1H, d), 8.99(1H, d)
[0638] 2) Ethyl 1-(pyridine-3-yl)-4-(2-(trifluoromethyl)phenyl)-1H-pyrazole
3-carboxylate (present compound number: C-0044)
Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-lH-pyrazole-3
carboxylate (4.0 g, 7.8 mmol), 2-(trifluoromethyl)phenylboronic acid (2.4 g, 12.6 mmol),
sodium carbonate (2.7 g, 25.5 mmol), and tetrakis(triphenylphosphine) palladium (0.45 g,
0.39 mmol) were added to a mixed solvent of tetrahydrofuran (30 mL) and water (6 mL), and
refluxed under heating for 5 hours in a nitrogen atmosphere. After end of the reaction, the
reaction solution was poured into saturated brine, and extracted with ethyl acetate. The
obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was
distilled off under reduced pressure. The residue was purified by silica gel column
chromatography, to give ethyl 1-(pyridine-3-yl)-4-{2-(trifluoromethyl)phenyl}-1H-pyrazole
3-carboxylate (2.6 g, yield: 93%).
Melting point: 131-134°C
1H-NMR data (400 MHz, CDCl 3/TMS 6(ppm)): 1.13(3H, t), 4.24(2H, q), 7.30
7.70(4H, m), 7.77(1H, d), 7.98(1H, s), 8.21(1H, ddd), 8.65(1H, dd), 9.04(1H, d)
[0639] 3) 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3
carboxamide (present compound number: A-0044)
Ethyl 1-(pyridine-3-yl)-4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylate
(2.5 g, 6.9 mmol) was dissolved in ethanol (30 mL), and sodium hydroxide (0.84 g, 21.0
mmol) and water (5.0 mL) were added at room temperature, and further, the resultant solution
was heated to 40°C with an oil bath and stirred for 1 hour. The solvent of the reaction
solution was distilled off under reduced pressure, and 6 N hydrochloric acid was added to the
residue, and the precipitated solid was filtered off, and dried to give crude1-(pyridine-3-yl)-4
[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylic acid. The obtained 1-(pyridine-3-yl)
4-[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylic acid was dissolved in
dichloromethane (50 mL), and oxalyl chloride (5.9 g, 46.5 mmol) and N,N
dimethylformamide (catalytic amount) were added, and allowed to react at room temperature for 1 hour. The solvent was distilled off under reduced pressure, and the residue was dissolved intetrahydrofuran (10 mL). The solution was then added to a mixed solution of tetrahydrofuran (20 mL) and aqueous ammonia (content: 28%, 10 mL) at 0°C, and then stirred at room temperature for 1 hour. The solvent of the reaction solution was distilled off under reduced pressure. The residue was washed sequentially with water and 2-propanol, and the obtained crude product was recrystallized in chloroform to give1-(pyridine-3-yl)-4
[2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide (1.1 g, yield: 48%).
Melting point: 178-181°C 1H-NMR data (400 MHz, CDCl 3/TMS 6(ppm)): 5.34(1H, brs), 6.79(1H, brs),
7.44-7.61(4H, m), 7.75(1H, d), 7.96(1H, s), 8.09(1H, dd), 8.64(1H, d), 9.04(1H, d)
[0640] (Example 2)
Production of 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3
carboxamide (present compound number: B-100)
[0641] 1) Ethyl 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3
carboxylate (present compound number: D-0108)
Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-1H-pyrazole-3
carboxylate (3.4 g, 6.6 mmol), 4-(methylpyridine-3-yl)boronic acid (1.0 g, 7.3 mmol), sodium
carbonate (1.6 g, 15.1 mmol), and tetrakis(triphenylphosphine) palladium (0.38 g, 0.33 mmol)
were added to a mixed solvent of 1,2-dimethoxyethane (30 mL) and water(6 mL), and
refluxed under heating for 9 hours in a nitrogen atmosphere. After end of the reaction, the
reaction solution was poured into saturated brine, and extracted with ethyl acetate. The
obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was
distilled off under reduced pressure. The residue was purified by silica gel column
chromatography, to give ethyl 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3
carboxylate (1.3 g, yield: 64%).
Melting point: 120-123°C 1H-NMR data (300 MHz, CDCl 3/TMS 6(ppm)): 1.20(3H, t), 2.24(3H, s), 4.28(2H,
q), 7.21(1H, d), 7.47(1H, dd), 7.96(1H, s), 8.21(1H, ddd), 8.41(1H, s), 8.48(H, dd), 8.65(H, dd), 9.05(1H, d)
[0642] 2) 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-H-pyrazole-3
carboxylic acid (present compound number: F-0108)
Ethyl 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate
(1.2 g, 3.9 mmol) was dissolved in ethanol (15 mL), and sodium hydroxide (0.47 g, 11.8
mmol) and water (3.0 mL) were added at room temperature, and stirred for 1 hour. The
solvent of the reaction solution was distilled off under reduced pressure, and 6 N hydrochloric
acid was added to the residue, and the precipitated solid was filtered off, and washed with
water and hexane, and dried to give 4-(4-methylpyridine-3-yl)--(pyridine-3-yl)-1H-pyrazole
3-carboxylic acid (0.8 g, yield: 73%).
Melting point: 277-280°C 1H-NMR data (300 MHz, DMSO-d 6 /TMS 6(ppm)): 2.05(3H, s),7.29(1H, d),
7.58(1H, dd), 8.30(1H, dd), 8.34(1H, s), 8.39(1H, d), 8.59(1H, d), 8.80(1H, s), 9.15(H, d)
[0643] 3) 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3
carboxamide (present compound number: B-0100)
4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid (0.20
g, 0.71 mmol) was dissolved in N,N-dimethylformamide (5.0 mL), and ammonium chloride
(0.076 g, 1.4 mmol), 1-hydroxybenzotriazole (0.12 g, 0.89 mmol), 1-ethyl-3-(3
dimethylaminopropyl)carbodiimide hydrochloride (0.20 g, 1.0 mol), and triethylamine (0.15 g,
1.5 mmol) were added, and the mixture was allowed to react at room temperature for 2 hours.
The reaction solution was poured into a saturated aqueous solution of sodium hydrogen
carbonate, and the solid was filtered off, and washed sequentially with water and n-hexane, to
give 4-(4-methylpyridine-3-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (0.16 g, yield:
80%).
Melting point: 264-267°C 1H-NMR data (400 MHz, DMSO-d 6 /TMS 6(ppm)): 2.22(3H, s)7.30(1H, d),
7.43(1H, brs), 7.62(1H, dd), 7.87(1H, brs), 8.37(1H, s), 8.38-8.45(2H, m), 8.61(1H, d),
8.80(1H, s), 9.28(1H, d)
[0644] (Example 3)
Production of 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-H-pyrazole-3
carboxamide (present compound number: A-0634)
[0645] 1) Ethyl 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H
pyrazole-3-carboxylate (present compound number: C-0634)
Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-lH-pyrazole-3
carboxylate (0.42 g, 0.82 mmol), 4-chloro-2-methoxyphenylboronic acid (0.20 g, 1.1 mmol),
sodium carbonate (0.19 g, 1.8 mmol), and tetrakis(triphenylphosphine) palladium (0.050 g,
0.043 mmol) were added to a mixed solvent of tetrahydrofuran (5.0 mL) and water (0.50 mL),
and refluxed under heating for 3 hours in a nitrogen atmosphere. After end of the reaction,
the reaction solution was poured into saturated brine, and extracted with ethyl acetate. The
obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was
distilled off under reduced pressure. The residue was purified by silica gel column
chromatography, to give ethyl 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole
3-carboxylate (0.25g, yield: 86%).
Melting point: 133-134°C 1H-NMR data (300 MHz, CDCl 3/TMS 6(ppm)): 1.27(3H, t), 3.78(3H, s), 4.32(2H,
q), 6.94(1H, d), 7.00(1H, dd), 7.26(1H, d), 7.44(1H, dd), 7.99(1H, s), 8.17(H, ddd), 8.61(1H,
dd), 9.02(1H, d)
[0646] 2) 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole-3
carboxamide (present compound number: A-0634)
Ethyl 4-(4-chloro-2-methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole-3
carboxylate (0.15 g, 0.42 mmol) was dissolved in a 7 M ammonia solution in methanol (20
mL), and stirred at room temperature for 2 days. Further, a 7 M ammonia solution in
methanol (30 mL) was added to the reaction solution, and stirred at room temperature for 3
days. The solvent of the reaction solution was distilled off under reduced pressure, and the
residue was purified by silica gel column chromatography to give 4-(4-chloro-2
methoxyphenyl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (0.12 g, yield: 87%).
Melting point: 192-194°C 1H-NMR data (300 MHz, CDCl 3/TMS 6(ppm)): 3.81(3H, s), 5.44(1H, brs),
6.77(1H, brs), 6.94(1H, d), 6.99(1H, dd), 7.40(1H, d), 7.42-7.48(1H, in), 8.05(1H, s), 8.05
8.11(lH, m), 8.57-8.67(1H, m), 8.98-9.09(1H, m)
[0647] (Example 4)
Production of ethyl 4-iodo-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (present
compound number: D-0003)
[0648] Ethyl 1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (0.92 g, 4.2 mmol)
was dissolved in acetonitrile (10 mL), and iodine (1.1 g, 4.3 mmol) and ammonium
hexanitratocerate (V) (2.4 g, 4.3 mmol) were added, and refluxed under heating for 10 hours.
After end of the reaction, a saturated aqueous solution of sodium thiosulfate was added to the
reaction solution, and extracted with ethyl acetate. The obtained organic layer was dried
over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced
pressure, and the residue was purified by silica gel column chromatography to give ethyl 4
iodo-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (0.75 g, yield: 52%).
Melting point: 128-130°C 1H-NMR data (300 MHz, CDCl 3/TMS 6(ppm)): 1.44(3H, t), 4.47(2H, q), 7.45(1H,
dd),8.07(lH, s), 8.10(lH, ddd), 8.64(lH, dd), 8.97(1H, d)
[0649] (Example 5)
Production of 3-[3-carbamoyl-4-(2-methylphenyl)-1H-pyrazole-1-yl]pyridine-1
oxide (present compound number: A-8862)
[0650] In chloroform (50 mL), 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H
pyrazole-3-carboxamide (present compound number: A-0020; 0.30g, 1.1 mmol) was
dissolved, and m-chloroperbenzoic acid (content: 77%, 0.48 g, 2.1 mmol) was added, and
refluxed under heating for 2 hours. After end of the reaction, the solvent was distilled off
under reduced pressure, and the residue was purified by silica gel column chromatography to
give 3-[3-carbamoyl-4-(2-methylphenyl)-1H-pyrazole-1-yl]pyridine-1-oxide (0.31 g, yield:
98%).
1H-NMR data (400 MHz, CDCl 3/TMS 6(ppm)): 2.24(3H, s), 5.39(1H, brs),
6.63(1H, brs), 7.23-7.34(4H, m), 7.40(1H, dd), 7.62(1H, d), 7.84(1H, s), 8.19(1H, d), 8.81(H,
s)
[0651] [Example 6]
Production of 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3
carboxamide (present compound number: B-0027)
[0652] 1) Ethyl 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-H-pyrazole-3
carboxylate (present compound number: D-0035)
Ethyl 4-{[(nonafluorobutyl)sulfonyl]oxy}-1-(pyridine-3-yl)-lH-pyrazole-3
carboxylate (3.1 g, 6.0 mmol), bis(pinacolato)diboron (2.3 g, 9.1 mmol), potassium acetate
(1.8 g, 18.3 mmol), and [1,'-bis(diphenylphosphino)ferrocene]palladium dichloride
dichloromethane adduct (0.49 g, 0.60 mmol) were dissolved in N,N-dimethylformamide (60
mL), and heated to 90°C and stirred for 4 hours in a nitrogen atmosphere by using an oil bath.
After end of the reaction, the reaction solution was poured into saturated brine, and extracted
with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate,
and then the solvent was distilled off under reduced pressure. Further, silica gel column
chromatography was conducted to give crude (3-(ethoxycarbonyl)--(pyridine-3-yl)-1H
pyrazole-4-yl)boronic acid. The obtained (3-(ethoxycarbonyl)-1-(pyridine-3-yl)-1H
pyrazole-4-yl)boronic acid was dissolved in a mixed solvent of tetrahydrofuran (15 mL) and
water (3 mL), and 2-bromo-3-methylpyridine (0.44 g, 2.6 mmol), sodium carbonate (0.53 g,
5.0 mmol), and tetrakis(triphenylphosphine)palladium (0.25 g, 0.22 mmol) were added, and
refluxed under heating for 1 hour in a nitrogen atmosphere. After end of the reaction, the
reaction solution was poured into saturated brine, and extracted with ethyl acetate. The
obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was
distilled off under reduced pressure. The residue was purified by silica gel column
chromatography, to give ethyl 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H- pyrazole-3
carboxylate (0.74 g, yield; 40%).
Melting point: 97-100°C
1H-NMR data (400MHz,DMSO/TMS 6(ppm)): 0.86(3H, t), 2.25(3H, s), 4.19(2H,
q), 7.31(1H, dd), 7.64(1H, dd), 7.71(1H, d), 8.30-8.39(1H, m), 8.40(1H, d), 8.64(1H, d),
8.90(1H, s), 9.19(1H, d)
[0653] 2) 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-lH-pyrazole-3
carboxamide (present compound number: B-0027)
Ethyl 4-(3-methylpyridine-2-yl)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate
(0.69 g, 2.2 mmol) was dissolved in ethanol (15 mL), and sodium hydroxide (0.27 g, 6.8
mmol) and water (3.0 mL) were added at room temperature, and stirred for 2 hours. The
solvent of the reaction solution was distilled off under reduced pressure, and the residue was
dissolved in water, and 2N hydrochloric acid was added to adjust the pH to 4 to 7. Further, water was distilled off under reduced pressure to give crude 4-(3-methylpyridine-2-yl)-1
(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid. The obtained 4-(3-methylpyridine-2-yl)-1
(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid was dissolved in N,N-dimethylformamide (10
mL), and ammonium chloride (0.24 g, 4.5 mmol), 1-hydroxybenzotriazole (0.36 g, 2.7 mmol),
1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (0.64 g, 3.3mol) and
triethylamine (1.1 g, 10.9 mmol) were added, and allowed to react at room temperature for 2
hours. The reaction solution was poured into a saturated aqueous solution of sodium
hydrogen carbonate, and extracted with ethyl acetate. The obtained organic layer was dried
over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced
pressure. Ethyl acetate and hexane were added to the residue, and the precipitated solid was
washed with ethyl acetate and hexane, to give 4-(3-methylpyridine-2-yl)--(pyridine-3-yl)
1H-pyrazole-3-carboxamide (0.11 g, yield; 18%).
Melting point: 145-148°C 1H-NMR data (400MHz,DMSO/TMS 6(ppm)): 2.22(3H, s), 7.28(1H, dd),
7.40(1H, s), 7.60(1H, dd), 7.67(1H, d), 7.90(1H, s), 8.35-8.43(2H, m), 8.60(H, d), 8.80(H,
s), 9.27(1H, d)
[0654] [Example 7]
Production of ethyl 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3- carbonyl carbamate (present compound number: A-5414)
[0655] In oxalyl chloride (15 g, 118 mmol), 1-(pyridine-3-yl)-4-(2
methylphenyl)-1H-pyrazole-3-carboxamide (present compound number: A-0020; 0.50 g, 1.8
mmol) was dissolved, and the resultant solution was refluxed under heating for 10 minutes.
Oxalyl chloride was distilled off under reduced pressure, and the residue was dissolved in
ethanol (7.9 g, 171 mmol), and stirred at room temperature for 10 minutes. After end of the
reaction, the reaction solution was poured into a saturated aqueous solution of sodium
hydrogen carbonate, and extracted with ethyl acetate. The obtained organic layer was dried
over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced
pressure. The residue was purified by silica gel column chromatography, to give ethyl 1
(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3-carbonyl carbamate (0.18 g, yield: 29%). 1H-NMR data(300MHz,CDC3/TMS (ppm)): 1.40(3H, t), 2.22(3H, s), 4.41(2H,
q), 7.13-7.37(4H, m), 7.51(1H, dd), 7.97(1H, s), 8.14(1H, dd), 8.68(1H, d), 9.07(1H, d),
10.75(1H, s)
[0656] [Example 8]
Production of N-(2-methoxyacetyl)-1-(pyridine-3-yl)-4-(2-methylphenyl)-1H
pyrazole-3-carboxamide (present compound number: A-4808)
[0657] In toluene (5 mL), 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole
3-carboxamide (present compound number: A-0020; 0.20 g, 0.72 mmol) was dissolved, and
2-methoxyacetyl chloride (0.17 g, 1.6 mmol) was added and refluxed under heating for 2
hours. The reaction solution was poured into water and extraction with ethyl acetate was
conducted. The obtained organic layer was dried over anhydrous magnesium sulfate, and
then the solvent was distilled off under reduced pressure. The residue was purified by silica
gel column chromatography, to give N-(2-methoxyacetyl)-1-(pyridine-3-yl)-4-(2
methylphenyl)-1H-pyrazole-3-carboxamide (0.080 g, yield: 32%). 1H-NMR data (300MHz,CDCl 3/TMS 6(ppm)): 2.24(3H, s), 3.50(3H, s), 4.42(2H,
s), 7.23-7.37(4H, m), 7.52(1H, dd), 8.00(1H, s), 8.14(1H, dd), 8.69(1H, d), 9.06(1H, d),
9.89(1H, s)
[0658] [Example 9]
Production of 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H-pyrazole-3
carbothioamide (present compound number: A-8646)
[0659] In 1,4-dioxane (10 mL), 1-(pyridine-3-yl)-4-(2-methylphenyl)-1H
pyrazole-3-carboxamide (present compound number: A-0020; 0.70 g, 2.5 mmol) was
dissolved, and Lawesson's reagent (1.2 g, 3.0 mmol) was added and stirred at 80°C for 40
minutes. After end of the reaction, the solvent was distilled off under reduced pressure, and
the residue was purified by silica gel column chromatography, to give1-(pyridine-3-yl)-4-(2
methylphenyl)-1H-pyrazole-3-carbothioamide (0.66 g, yield: 89%).
1H-NMR data (400MHz,CDCl 3/TMS 6(ppm)): 2.24(3H, s), 7.22-7.38(5H, m),
7.47(1H, dd), 7.90(1H, s), 8.00(1H, s), 8.12(1H, dd), 8.64(1H, d), 9.06(1H, d)
[0660] Physical property values, including those in the above-described
examples, of the present compound [I] synthesized in accordance with the above-described
examples are shown in the following Table 315 to Table 323, and physical property values of
the present compound [II] are similarly shown in the following Table 324 to Table 334. The
compound numbers and the signs in Tables are as defined above.
[0661]
[Table 315] com pound physical property value A-0001 m eating point (°C) 161-163 A-0002 m eating point (°C) 183-185 A-0003 m eating point (°C) 204-207 A-0004 m eating point (°C) 203-206 A-0005 m eating point (°C) 164-166 A-0006 m eating point (°C) 169-172 A-0007 m eating point (°C) 203-206 A-0008 m eating point (°C) 171-174 A-0014 m eating point (°C) 171-174 A-0020 m eating point (°C) 181-184 A-0021 m eating point (°C) 170-173 A-0022 m eating point (°C) 177-179 A-0023 m eating point (°C) 166-168 A-0025 m eating point (°C) 170-173 A-0029 m eating point (°C) 192-194 A-0041 m eating point (°C) 188-190 A-0044 m eating point (°C) 178-181 A-0045 m eating point (°C) 179-181 A-0046 m eating point (°C) 205-208 A-0047 m eating point (°C) 202-205 A-0059 m eating point (°C) 140-143 A-0086 m eating point (°C) 145-147 A-0101 m eating point (°C) 162-165 A-0103 m eating point (°C) 205-208 A-0119 m eating point (°C) 177-179 A-0120 m eating point (°C) 123-126 A-0121 m eating point (°C) 168-171 A-0122 m eating point (°C) 205-207 A-0123 m eating point (°C) 170-173 A-0124 m eating point (°C) 190-193 A-0125 m eating point (°C) 169-170 A-0128 m eating point (°C) 190-193 A-0134 m eating point (°C) 129-132 A-0137 m eating point (°C) 147-149 A-0143 m eating point (°C) 154-157 A-0144 m eating point (°C) 160-162 A-0145 m eating point (°C) 182-183 A-0146 m eating point (°C) 163-166 A-0147 m eating point (°C) 150-153 A-0148 m eating point (°C) 190-192 A-0152 m eating point (°C) 193-196
[0662]
[Table 316] com pound physicalproperty value A-0176 m e Iting po int (C) 126-128 A-0177 m e Iting po int (C) 138-141 A-0179 m e Iting po int (C) 127-130 A-0183 m e Iting po int (C) 183-185 A-0185 m e Iting po int (C) 201-202 A-0186 m e Iting po int (C) 186-188 A-0188 m e Iting po int (C) 204-206 A-0189 m e Iting po int (C) 167-170 A-0192 m e Iting po int (C) 250-253 A-0198 m e Iting po int (C) 157-160 A-0227 m e Iting po int (C) 200-202 A-0239 m e Iting po int (C) 226-229 A-0242 m e Iting po int (C) 297-300 A-0260 m e Iting po int (C) 155-157 A-0263 m e Iting po int (C) 180-182 A-0266 m e Iting po int (C) 147-150 A-0269 m e Iting po int (C) 200-203 A-0320 m e Iting po int (C) 196-199 A-0329 m e Iting po int (C) 173-175 A-0338 m e Iting po int (C) 185-188 A-0340 m e Iting po int (C) 218-221 A-0347 m e Iting po int (C) 190-193 A-0512 m e Iting po int (C) 163-166 A-0521 m e Iting po int (C) 245-248 A-0524 m e Iting po int (C) 237-240 A-0542 m e Iting po int (C) 243-245 A-0548 m e Iting po int (C) 195-198 A-0549 m e Iting po int (C) 263-266 A-0550 m e Iting po int (C) 197-200 A-0551 m e Iting po int (C) 239-242 A-0553 m e Iting po int (C) 297-300 A-0555 m eating po int (C) 202-205 A-0557 m eating po int (C) 199-202 A-0561 m eating po int (C) 239-242 A-0563 m eating po int (C) 176-178 A-0571 m eating po int (C) 170-173 A-0573 m eating po int (C) 177-178 A-0574 m eating po int (C) 170-173 A-0577 m eating po int (C) 147-150 A-0578 m eating po int (C) 195-198 A-0582 m eating po int (C) 170-173
[0663]
[Table 317] com pound physicaIproperty value A-0583 m eking point (0C) 186-188 A-0587 m eking point (C)0 203-206 A-0588 m eking point (0C) 213-216 A-0591 m eking point (C)0 196-199 A-0593 m eking point (C)0 127-130 A-0594 m eking point (0C) 90-93 A-0597 m eking point (C)0 170-173 A-0598 m eking point (0C) 202-203 A-0600 m eking point (0C) 214-216 A-0603 m eking point (C)0 216-219 A-0608 m eking point (0C) 167-170 A-0609 m eking point (C)0 215-218 A-0613 m eking point (C)0 167-170 A-0614 m eking point (0C) 197-198 A-0618 m eking point (C)0 195-198 A-0624 m eking point (0C) 209-212 A-0629 m eking point (0C) 203-206 A-0633 m eking point (C)0 200-203 A-0634 m eking point (0C) 192-194 A-0636 m eking point (C)0 163-166 A-0637 m eking point (C)0 179-182 A-0638 m eking point (0C) 113-116 A-0639 m eking point (C)0 220-223 A-0644 m e ting po int (°C) 171-174 A-0645 m eking point (C)0 194-196 A-0649 m eking point (C)0 156-159 A-0652 m eking point (0C) 175-178 A-0653 m eking point (C)0 213-216 A-0654 m eking point (C)0 145-148 A-0655 m eking point (0C) 154-157 A-0656 m eking point (C)0 144-147 A-0659 m eking point (0C) 141-144 A-0660 m eking point (C)0 210-213 A-0663 m eking point (C)0 213-216 A-0664 m eking point (0C) 143-146 A-0665 m eking point (C)0 253-256 A-0670 m eking point (0C) 192-195 A-0671 m eking point (C)0 206-209 A-0688 m eking point (C)0 144-147 A-0689 m eking point (0C) 161-163 A-0691 m eking point (C)0 165-168
[0664]
[Table 318] com pound physicalproperty value A-0692 m eating point (C) 150-153 A-0693 m eating point (C) 165-166 A-0697 m eating point (C) 160-163 A-0701 m eating point (C) 171-173 A-0705 m eating point (C) 156-159 A-0709 m eating point (C) 150-153 A-0712 m eating point (C) 173-175 A-0713 m eating point (°C) 113-115 A-0733 m eating point (C) 183-186 A-0875 m eating point (C) 220-223 A-0906 m eating point (C) 177-180 A-0907 m eating point (C) 188-190 A-0908 m eating point (C) 194-197 A-0909 m eating point (C) 137-140 A-0910 m eating point (C) 186-189 A-0911 m eating point (C) 230-233 A-0912 m eating point (C) 196-198 A-0913 m eating point (C) 160-162 A-1067 m eating point (C) 225-227 A-1076 m eating point (C) 145-148 A-1077 m eating point (C) 198-201 A-1097 m eating point (C) 233-236 A-1102 m eating point (C) 256-258 A-1117 m eating point (C) 209-211 A-1134 m eating point (C) 205-208 A-1136 m eating point (C) 222-225 A-1140 m eating point (C) 180-183 A-1141 m eating point (C) 131-134 A-1145 m eating point (C) 155-157 A-1146 m eating point (C) 183-184 A-1147 m eating point (C) 193-196 A-1148 m eating point (C) 166-167 A-1151 m eating point (C) 206-208 A-1152 m eating point (C) 127-130 A-1153 m eating point (C) 173-175 A-1154 m eating point (C) 172-174 A-1155 m eating point (C) 133-136 A-1156 m eating point (C) 156-159 A-1157 m eating point (°C) 171-174 A-1158 m eating point (C) 180-183 A-1159 m eating point (C) 169-171
[0665]
[Table 319] com pound physicalproperty value A-1160 m eating point (C) 184-187 A-1161 m eating point (C) 140-143 A-1162 m eating point (C) 85-88 A-1163 m eating point (C) 167-170 A-1164 m eating point (C) 167-170 A-1165 m eating point (C) 200-203 A-1166 m eating point (C) 130-133 A-1980 m eating point (C) 90-93 A-2182 m eating point (C) 136-139 A-2384 refractive index (n zo2) 1.5741 A-2586 m eating point (C) 157-160 A-2600 m eating point (C) 139-141 A-2788 m eating point (C) 110-113 A-2990 m eating point (C) 157-160 A-3192 m eating point (C) 153-156 A-3596 m eating point (C) 90-93 A-3798 m eating point (C) 159-161 A-3812 m eating point (C) 103-106 A-4000 m eating point (C) 172-174 A-4202 refractive index (n ou) 1.5991 A-4404 m eating point (C) 140-143 A-4606 m eating point (C) 166-168 A-5616 m eating point (C) 97-100 A-6020 refractive index (nzo2) 1.6006 A-6222 m eating point (C) 132-134 A-6424 m eating point (C) 200-203 A-6626 m eating point (C) 217-219 A-7030 refractive index (nD20) 1.5688 A-7232 m eating point (C) 204-206 A-7434 m eating point (C) 136-139 A-7636 m eating point (C) 117-120 A-7838 m eating point (C) 150-152 A-8040 m eating point (C) 129-132 A-8242 m eating point (C) 120-123 A-8444 m eating point (C) 75-78 A-8646 m eating point (C) 134-135 A-8862 m eating point (C) 147-150 A-9435 m eating point (C) 236-239 A-9480 m eating point (C) 176-179 A-9993 refractive index (n20) 1.6292 A-9994 m eating point (C) 72-75
[0666]
[Table 320]
com pound physicalproperty value hydrochloride of A-0593 m eIting point (C) 147-150
[0667]
[Table 321]
com pound physicalproperty valje ('H-NM R data, in CDC TM S 6(ppm))
5.34(1H , brs), 6.79 (1H , brs), 7.44-7.61 (4H , m ), A-0044 400M H z 7.75 (1H , d), 7.96 (1H, s), 8.09 (1H, dd), 8.64 (1H, d), 9.04(1H , d)
2.66 (3H , s), 5.42 (1H, s), 6.90 (1H, s), 7.34 (1H, dd), A-0182 300M H z 7.45-7.57 (2H, m ), 7.64 (1H , dt), 8.02 (1H, s), 8.04 8.12(2H, m ), 8.66 (1H, dd), 9.07 (1H, d)
3.81 (3H , s), 5.44 (1 H , b rs), 6.77 (1 H , b rs), 6.94 (1 H , d), A-0634 300Mhz 6.99 (1H , d d), 7.40 (1H , d), 7.42-7.48 (1H , m ), 8.05 (1H, s), 8.05-8.11 (1H , m ), 8.57-8.67 (1H , m ), 8.98 9.09 (1H , m )
[0668]
[Table 322]
com pound physicalproperty value B-0001 m eating point (°C) 194-197 B-0002 m eating point (C) 193-196 B-0003 m eating point (C) 210-213 B-0004 m eating point (C) 214-217 B-0009 m eating point (C) 175-178 B-0018 m eating point (C) 245-248 B-0027 m eating point (C) 145-148 B-0090 m eating point (C) 254-257 B-0091 m eating point (C) 262-264 B-0095 m eating point (C) 241-243 B-0099 m eating point (C) 188-191 B-0100 m eating point (C) 264-267 B-0107 m eating point (C) 235-237 B-0165 m eating point (C) 217-220 B-0199 m eating point (C) 244-247 B-0205 m eating point (C) 224-227 B-0287 m eating point (C) 178-180 B-0290 m eating point (C) 137-140 B-0293 m eating point (C) 185-188 B-0296 m eating point (C) 140-143 B-0301 m eating point (C) 166-168 B-0367 m eating point (C) 233-236 B-0389 m eating point (C) 242-245 B-0453 m eating point (C) 201-204 B-0454 m eating point (C) 180-183 B-0455 m eating point (C) 167-170 B-0456 m eating point (C) 197-200 B-0457 m eating point (C) 230-233 B-0458 m eating point (C) 270-273 B-0459 m eating point (C) 253-255
[0669]
[Table 323]
com pound physicaIproperty vakje ('H-NM R data, in DM SO-d6 TM S 6(ppm ))
2.22 (3H , s), 7.30 (1 H , d), 7.43 (1H , b rs), 7.62 (1H , dd), B-0100 400M H z 7.87 (1H , b rs), 8.37 (1H , s), 8.38-8.45 (2H , m ), 8.61 (1 H
, d), 8.80 (1H , s), 9.28 (1H , d)
[0670]
[Table 324] com pound physicalproperty value C-0001 m eating po int (C) 57-59 -0003 m eating po int (C) 110-112 -0004 m eating po int (C) 134-136 -0005 m eating po int (C) 113-115 -0006 m eating po int (C) 101-103 -0007 m eating po int (C) 114-116 -0008 m eating po int (C) 131-133 -0020 refractive index ( nzu) 1.6018 -0021 refractive index (nzo2) 1.6099 -0022 m eating po int (C) 113-116 -0023 m eating po int (C) 108-110 -0025 refractive index ( nzo) 1.6062 -0029 m e Iting po int (C) 92-95 -0041 m e Iting po int (C) 119-122 -0044 m e Iting po int (C) 131-134 -0045 m e Iting po int (C) 100-101 -0046 m e Iting po int (C) 124-126 -0047 m e Iting po int (C) 108-109 -0086 m e Iting po int (C) 90-93 -0119 refractive index x ( n ou) 1.5782 -0120 m eating po int (C) 110-112 -0121 m eating po int (C) 97-100 -0122 refractive index (nD20) 1.5981 -0124 m eating point (C) 87-90 -0125 refractive index (nou) 1.5982 -0128 refractive index ( n oD ) 1.5890 -0134 refractive index ( n zoD ) 1.5873 -0137 refractive index (nD20) 1.5901 -0143 m eIting point (C) 78-80 -0144 m eating point (C) 62-63 -0145 m eating point (C) 92-94 -0147 m eating point (C) 93-94 -0152 refractive index (n o ) 1.5951 -0176 m eating point (C) 87-89 -0179 m eating point (C) 88-89 -0182 m eating point (C) 160-163 -0183 m eating point (C) 137-139 -0186 m eating point (C) 190-193 -0198 m eating point (°C) 111-112 -0227 m eating point (C) 105-108 -0239 m eating point (C) 110-113
[0671]
[Table 325] com pound physicalproperty value 0-0263 refractive index (n zo2) 1.5818 0-0266 refractive index (n zo2 ) 1.5869 0-0269 m eating point (C) 87-90 0-0320 m eating point (°C) 90-92 0-0329 m eating point (°C) 96-98 0-0338 m eating point (°C) 117-119 0-0340 m eating point (°C) 113-116 0-0512 refractive index (n ou) 1.6076 0-0518 m eating point (C) 134-136 0-0520 m eating point (°C) 140-143 0-0549 m eating point (°C) 191-194 0-0550 m eating point (C) 170-173 0-0553 m eating point (C) 144-147 0-0555 m eating point (C) 103-104 0-0557 m eating point (C) 99-100 0-0561 m eating point (C) 96-98 0-0563 m eating point (C) 97-100 0-0571 m eating point (C) 109-111 0-0573 m eating point (C) 95-97 0-0574 m eating point (C) 46-49 0-0577 m eating point (C) 116-118 0-0578 m eating point (C) 116-118 0-0587 m eating point (C) 153-155 0-0588 m eating point (C) 127-129 0-0591 m eating point (C) 150-153 0-0593 m eating point (C) 118-120 0-0594 refractive index (n zo) 1.5904 0-0597 m eating (C) point 142-144 0-0598 m eating (C) point 92-93 0-0600 m eating (C) point 123-126 0-0608 refractive index (n o ) 1.5777 0-0613 m eating (C) point 111-113 0-0614 refractive index (n zo2) 1.6008 0-0624 m eating point (C) 93-96 0-0629 refractive index (nD20) 1.5092 0-0633 m eating (C) point 151-154 0-0634 m eating (C) point 133-134 0-0636 m eating (C) point 89-91 0-0637 m eating (C) point 75-77 0-0638 refractive index (nD20) 1.6013 0-0639 refractive index (nzo~) 1.5971
[0672]
[Table 326] com pound physicalproperty value C-0644 melting point (C) 137-140 C-0652 m eating point (C) 87-90 C-0653 refractive index (n zo2) 1.6039 C-0655 refractive index (n zo2) 1.5994 C-0656 m eating po int (C) 85-88 C-0659 m eating po int (C) 124-127 C-0660 m eating po int (°C) 110-113 -0663 refractive index (n D20) 1.6038 20 C-0664 refractive index (n D ) 1.6066 C-0670 refractive index (nD20) 1.5635 C-0692 refractive index (n Do2) 1.5928 C-0697 refractive index (n zo2) 1.5911 -0705 refractive index (nD20) 1.5889 C-0712 m eating point (C) 131-133 C-0906 m eating point (°C) 92-94 C-0907 refractive index (n zo2) 1.5875 C-0908 m eating point (°C) 92-95 C-0910 refractive index (n zo2 ) 1.5816 C-0911 refractive index (nD20) 1.5919 C-0912 refractive index (n zo2 ) 1.5881 C-1067 m eating point (C) 146-148 C-1097 m eating point (C) 173-175 C-1102 m eating point (C) 93-96 C-1117 m eating point (C) 119-120 C-1136 m eating point (C) 120-123 C-1140 refractive index (n zo2) 1.5821 C-1141 m eating point (C) 95-97 C-1145 m eIting point (C) 80-83 C-1148 m eIting point (C) 98-100 C-1152 m eIting point (C) 150-153 C-1155 m eIting point (C) 130-133 C-1156 m eating point (C) 145-148 C-1162 m eIting point (C) 92-95 C-1163 refractive index (n zo2) 1.5996 C-1165 m eating point (C) 84-87
[0673]
[Table 327] com pound physicalproperty value D-0002 m eating point (C) 207-210 D-0003 m eating point (C) 128-130 D-0004 m eating point (C) 114-117 D-0005 m eating point (C) 96-98 D-0008 m eating point (C) 103-104 D-0012 m eating point (C) 109-111 D-0035 m eating point (C) 97-100 D-0098 m eating point (C) 156-159 D-0099 m eating point (C) 163-166 D-0103 m eating point (C) 126-129 D-0107 m eating point (C) 95-98 D-0108 m eating point (C) 120-123 D-0115 m eating point (C) 87-90 D-0207 m eating point (C) 145-148 D-0213 m eating point (C) 123-126 D-0295 m eating point (C) 100-102 D-0301 m eating point (C) 97-100 D-0309 m eating point (C) 96-98 D-0375 m eating point (C) 182-185 D-0464 m eating point (C) 120-123 D-0466 m eating point (C) 146-149
[0674]
[Table 328] com pound physicalproperty value E-0002 m eating point (C) 190-193 E-0003 m eating point (C) 235-237 E-0004 m eating point (C) 220-223 E-0005 m eating point (C) 204-207 E-0006 m eating point (C) 224-227 E-0007 m eating point (C) 228-231 E-0008 m eating point (C) 225-227 E-0020 m eating point (C) 200-203 E-0021 m eating point (C) 153-156 E-0022 m eating point (C) 235-238 E-0023 m eating point (C) 200-203 E-0025 m eating point (C) 243-246 E-0029 m eating point (C) 182-185 E-0041 m eating point (C) 219-222 E-0044 m eating point (C) 193-196 E-0046 m eating point (C) 237-240 E-0047 m eating point (C) 220-223 E-0086 m eating point (C) 195-198 E-0119 m eating point (C) 171-174 E-0120 m eating point (C) 185-188 E-0121 m eating point (C) 242-245 E-0122 m eating point (C) 219-222 E-0123 m eating point (C) 172-175 E-0124 m eating point (C) 263-263 E-0125 m eating point (C) 222-225 E-0128 m eating point (C) 217-220 E-0134 m eating point (C) 203-206 E-0137 m eating point (C) 210-213 E-0147 m eating point (C) 210-212 E-0148 m eating point (C) 223-226 E-0152 m eating point (C) 233-236 E-0176 m eating point (C) 211-214 E-0177 m eating point (C) 176-178 E-0179 m eating point (C) 211-214 E-0227 m eating point (C) 225-228 E-0263 m eating point (C) 212-214 E-0266 m eating point (C) 202-205 E-0269 m eating point (C) 183-186 E-0320 m eating point (C) 221-224 E-0329 m eating point (C) 183-186 E-0338 m eating point (C) 240-243
[0675] [Table 329]
com pound physicaIproperty value E-0340 m etoig point (C) 223-226 E-0518 m etoig point (C) 260-263 E-0520 m etoig point (C) 247-250 E-0521 m etoig point (C) 155-158 E-0542 m etoig point (C) 203-206 E-0549 m etoig point (C) 204-207 E-0553 m etoig point (C) 275-277 E-0555 m etoig point (C) 239-241 E-0557 m etoig point (C) 221-224 E-0561 m etoig point (C) 238-240 E-0563 m etoig point (C) 200-203 E-0571 m etoig point (C) 246-248 E-0573 m etoig point (C) 234-236 E-0574 m etoig point (C) 197-200 E-0577 m etoig point (C) 240-241 E-0578 m etoig point (C) 199-201 E-0587 m etoig point (C) 231-234 E-0588 m etoig point (C) 245-248 E-0591 m etoig point (C) 217-220 E-0593 m etoig point (C) 224-226 E-0594 m etoig point (C) 223-225 E-0597 m etoig point (C) 239-241 E-0598 m etoig point (C) 248-250 E-0600 m etoig point (C) 219-221 E-0608 m etoig point (C) 247-250 E-0609 m etoig point (C) 217-220 E-0613 m etoig point (C) 251-254 E-0614 m etoig point (C) 236-239 E-0618 m etoig point (C) 250-253 E-0624 m etoig point (C) 234-237 E-0629 m etoig point (C) 197-200 E-0633 m etoig point (C) 235-238 E-0636 m etoig point (C) 199-201 E-0638 m etoig point (C) 232-234 E-0639 m etoig point (C) 220-223 E-0644 m etoig point (C) 197-200 E-0652 m etoig point (C) 227-230 E-0653 m etoig point (C) 221-224 E-0655 m etoig point (C) 221-224 E-0656 m etoig point (C) 264-267 E-0659 m etoig point (C) 233-236
[0676]
[Table 330] com pound physical property valje E-0660 m eating point (C) 208-211 E-0663 m ekting po int (C) 240-243 E-0664 m ekting po int (C) 237-240 E-0665 m ekting po int (C) 267-270 E-0670 m ekting po int (C) 220-223 E-0688 m ekting po int (C) 203-206 E-0689 m ekting po int (C) 228-231 E-0691 m eating po int (C) 211-213 E-0692 m eating po int (C) 230-233 E-0693 m eating po int (C) 219-222 E-0697 m eating po int (C) 192-195 E-0701 m eating po int (C) 180-183 E-0705 m eating po int (C) 251-253 E-0712 m eating po int (C) 257-260 E-0733 m eating po int (C) 210-213 E-0906 m eating po int (C) 203-205 E-0907 m eating po int (°C) 215-218 E-0908 m eating po int (C) 226-229 E-0910 m eating po int (C) 190-193 E-0911 m eating po int (C) 223-226 E-0912 m eating po int (C) 198-201 E-0913 m eating po int (°C) 155-157 E-1067 m eating po int (C) 240-243 E-1076 m eating po int (C) 264-267 E-1077 m eating po int (C) 253-256 E-1102 m eating po int (C) 260-263 E-1117 m eating po int (C) 233-236 E-1136 m eating po int (C) 246-248 E-1140 m eating po int (C) 237-240 E-1148 m eating po int (C) 198-200 E-1152 m eating po int (C) 233-236 E-1153 m eating po int (C) 217-220 E-1155 m eating po int (C) 241-244 E-1156 m eating po int (C) 232-235 E-1160 m eating po int (C) 165-168 E-1163 m eating po int (C) 240-243 E-1165 m eating po int (C) 165-168
[0677]
[Table 331] com pound physicalproperty value F-0003 m elting point (C) 261-264 F-0008 m eating po int (C) 237-240 F-0012 m eating po int (C) 240-243 F-0017 m eating po int (C) 243-246 F-0099 m eating po int (C) 292-295 F-0108 m eating po int (C) 277-280 F-0115 m eating po int (C) 213-216 F-0207 m eating po int (C) 260-263 F-0213 m eating po int (C) 264-267 F-0295 m eating po int (C) 245-248 F-0301 m eating po int (C) 201-204 F-0309 m eating po int (C) 172-174 F-0375 m eating po int (C) 267-270 F-0461 m eating po int (C) 242-245 F-0462 m eating po int (C) 200-202 F-0463 m eating po int (C) 263-266 F-0464 m elting po int (C) 294-297 F-0466 m elting po int (C) 227-230
[0678]
[Table 332] com pound physical property value ('H-NM R data, in CDC I3 TM S 8(ppm ))
1.29 (3H, t), 4.37 (2H, q), 7.11-7.29 (2H, m ), 7.32 C-0002 300M H z 7.51 (3H, m ), 8.08 (1H, s), 8.20(1H, ddd), 8.65 (1H, dd), 9.04(1H, d)
1.13 (3H, t), 4.24 (2H, q), 7.30-7.70 (4H, m ), 7.77(1H, C-0044 400M H z d), 7.98 (1H, s), 8.21 (1H, ddd), 8.65 (1H, dd), 9.04(1H, d)
1.33 (3H , t), 1.43 (3H , t), 4.38 (2H , q), 4.70 (2H , q),
C-01 23 300M H z 6.86-6.92 (1H, m ), 7.03-7.09 (2H, m ), 7.28 (1H, dd), 7.44(1H, dd), 8.00(1H, s), 8.16 (1H, dd), 8.62 (1H, d), 9.03 (1H, d)
1.3 2 (3 H , t), 2.5 2 (3 H , s), 4.39 (2 H , q), 7.2 4-7.37 (3 H
, C-0177 400M H z m ), 7.41 (1H, s), 7.42-7.50(1H, m ), 8.04(1H, s), 8.16 8.21 (1H, m ), 8.63 (1H, d), 9.08 (1H, s)
1.22 (3H, t), 2.62 (3H, s), 4.28 (2H, q), 7.42 (1H, d), C-0185 400M H z 7.47 (1H, dd), 7.59-7.70 (2H, m ), 8.14-8.26(3H, m) 8.67 (1H, d), 9.09(1H, d)
1.32 (3H, t), 4.38 (2H, q), 7.26-7.35 (1H, m ), 7.41 C-0189 400M Hz 7.62 (3H, m ), 7.67 (1H, d), 8.04(1H, s), 8.20(1H, d), 8.65 (1H, d), 9.05 (1H, d)
1.27 (3H, t), 3.78 (3H, s), 4.32 (2H, q), 6.94(1H, d), C-0634 300M Hz 7.00(1H, dd), 7.26 (1H, d), 7.44(1H, dd), 7.99 (1H, s), 8.17 (1H, ddd), 8.61 (1H, dd), 9.02 (1H, d)
1.21 (3H, t), 3.76 (6H, s), 4.29 (2H, q), 6.62 (2H , d), C-0665 300M H z 7.30(1H, d), 7.43 (1H, dd), 8.03 (1H, s), 8.18 (1H, dd), 8.80(1H, d), 9.19(1H, d)
0.63-0.72 (2H, m ),0.78-0.90 (2H, m ), 1.15 (3H, t), C-0689 300M H z 11.66-1.78 (1H, m ), 4.27 (2H, q), 6.72 (1H, d), 6.95 (1H, t), 7.25 (1H , dd), 7.47 (1H, dd), 8.03 (1H, s), 8.22(1H, ddd), 8.63 (1H, dd), 9.05 (1H, d)
1.21 (3H, t), 2.23 (3H, s), 4.30 (2H, q), 7.30-7.68 (4H, C-1077 300M Hz m ),8.05 (1H, s), 8.23 (1H, dd), 8.67 (1H, d), 9.07(1H, d)
1.35 (3H, t), 4.40 (2H, q), 6.00 (2H, s), 6.80-6.93 (2H, C-1134 300M Hz m ), 7.09(1H, d), 7.47 (1H, dd), 8.12-8.23 (2H,, m) 8.63 (1H, d), 9.04(1H, s)
[0679]
[Table 333] com pound physialproperty vaije (IH-NM R data, in CDC TM S 6(ppm))
1.21 (3H , t), 2.41 (3H , s), 4.30 (2H , q), 7.01 (1H , t), C-1153 400M H z 7.16-7.30 (1 H , m ), 7.48 (1H , dd), 8.03 (1 H , s), 8.22 (1 H
, d), 8.63 (1 H , d), 9.0 6 (1 H , s)
1.15 (3H , t), 3.28 (3H , s), 4.21 (2H , s), 4.25 (2H , q), C-1160 400M H z 7.35 (1H , t), 7.39-8.01 (3H , m ), 8.01 (1 H , s), 8.23 (1 H
, d), 8.65 (1H , d), 9.07 (1 H , s)
1.31 (3H , t), 4.39 (2H , q), 7.42-7.56 (3 H , m ), 7.64 (1H
, D -0017 300M H z d), 7.82-7.92 (3 H , m ), 7.98 (1H , s), 8.11 (1H , s), 8.22 (1H , d), 8.65 (1H , d), 9.09 (1 H , s)
1.20 (3H , t), 2.24 (3H , s), 4.28 (2H , q), 7.21 (1H , d), D-0108 300M H z 7.47 (1H, dd), 7.96 (1H, s), 8.21 (1H, ddd), 8.41 (1H, s), 8.48 (1H , dd), 8.65 (1H , dd), 9.05 (1H , d)
1.33 (3 H , t), 2.18 (3 H , s), 2.30 (3 H , s), 4.38 (2H , q), D-0461 400M H z 7.50 (1H, dd), 7.93 (1H, s), 8.19 (1H, dd), 8.67 (1H, d), 9.04 (1H , d)
1.10-1.31 (9H , m ), 2.55 (2H , q), 2.63 (2H , q), 4.32 (2H
, D -0462 400M H z q), 7.48 (1H , dd), 7.91 (1H , s), 8.18 (1H , dd), 8.63 (1H
, d), 9.03 (1H , d)
0.87 (3H , t), 4.10 (2H , q), 7.39 (1H , d), 7.45-7.57 (2H ,
D -0463 300M H z m ), 7.70-7.80 (2H , m ), 8.12 (1H , s), 8.18 (1H , d), 8.25 (1H , d), 8.67 (1H , d), 8.96 (1H , d), 9.09 (1H , d)
[0680]
[Table 334] com pound physicaIproperty vaje (H-NM R data, in DM SO-d6 TM S 6(ppm))
7.48 (1H , dd), 7.60 (1H , dd), 7.90 (1H , dd), 8.29 (1H
, F-0103 300M H z ddd), 8.40 (1H , dd), 8.60 (1H , dd), 8.89 (1H , s), 9.14 (1H , d)
2.05 (3H , s),7.29 (1H , d), 7.58 (1H , dd), 8.30 (1H , dd), F-0108 300M H z 8.3 4 (1 H , s), 8.39 (1 H , d), 8.59 (1 H , d), 8.80 (1 H , s), 9.15 (1 H , d)
[0681] Next, formulation examples of the pest control agent of the present
invention using the pyrazole derivative of the present invention produced in the manner as
described above, or an agriculturally acceptable salt thereof will be specifically described. It
is to be noted that the compound, the kinds and the mixing ratios of additives are not limited
to this, but may be changed in a wide range. In the following description, "part" means a
part by mass.
[0682] (Formulation example 1) Emulsifiable concentrate
Compound described in Table 1 to Table 334 10 parts
Cyclohexanone 30 parts
Polyoxyethylene alkyl aryl ether 11 parts
Calcium alkylbenzene sulfonate 4 parts
Methylnaphthalene 45 parts
These ingredients were uniformly dissolved to give an emulsifiable concentrate.
[0683] (Formulation example 2) Water-dispersible powder
Compound described in Table 1 to Table 334 10 parts
Sodium salt of naphthalene sulfonic acid formalin condensate 0.5 parts
Polyoxyethylene alkyl aryl ether 0.5 parts
Diatomaceous earth 24 parts
Clay 65 parts
These ingredients were uniformly mixed and ground to give a water-dispersible powder.
[0684] (Formulation example 3) Dust
Compound described in Table 1 to Table 334 2 parts
Diatomaceous earth 5 parts
Clay 93 parts
These ingredients were uniformly mixed and ground to give a dust.
[0685] (Formulation example 4) Granules
Compound described in Table 1 to Table 334 5 parts
Sodium salt of lauryl alcohol sulfate ester 2 parts
Sodium lignin sulfonate 5 parts
Carboxymethylcellulose 2 parts
Clay 86 parts
These ingredients were uniformly mixed and ground. To this mixture, water in
an amount corresponding to 20 parts was added and kneaded, and processed into 14 to 32
mesh granules by using an extruding granulator, and then dried to give granules.
[0686] (Formulation example 5) Flowable concentrate
Compound described in Table 1 to Table 334 20 parts
Polyoxyethylene styrenated phenyl ether sulfate 4 parts
Ethylene glycol 7 parts
Silicone AF-118N (available from Asahi Kasei Corporation) 0.02 parts
Water 68.98 parts
These ingredients were mixed with a high-speed stirrer for 30 minutes, and then
ground with a wet grinder to give a flowable concentrate.
[0687] (Formulation example 6) Water-dispersible granule
Compound described in Table I to Table 334 10 parts
Sodium lignin sulfonate 5 parts
Polyoxyethylene alkyl aryl ether 1 part
Sodium polycarboxylate 3 parts
White carbon 5 parts
Pregelatinized starch 1 part
Calcium carbonate 65 parts
Water 10 parts
These ingredients were mixed and kneaded and extrusion granulated. The
obtained granules were dried by a fluidized-bed dryer, to give a water-dispersible granule.
[0688] Next, the effect exerted by the pest control agent of the present
invention will be described by way of test examples.
[0689] (Test example 1) Plutella xylostella killing test
The water-dispersible powder prepared in accordance with Formulation example
2 was diluted in water so that the concentration of the active ingredient was 500 ppm. A
cabbage leaf was dipped in this liquid agent, and air-dried, and then put into a plastic cup.
Ten second instar larvae of Plutella xylostella were released in the cup, and the cup was
lidded. Then, the cup was placed in a thermostatic chamber at 25°C, and the number of dead
insects was examined after 6 days, and the insect mortality was determined by the calculation
formula of numerical formula 1. The test was conducted singly.
[0690] [Numerical formula 1] Insect mortality(%)=[1-(number of living insects)/(number of tested insects)] X100
[0691] The compounds showing an insect mortality of 50% or more in this
test are as follows.
A-0020, A-0023, A-0025, A-0029, A-0047, A-0059, A-0125, A-0134, A-0144, A-0147, A
0148, A-0152, A-0176, A-0182, A-0183, A-0185, A-0186, A-0192, A-0227, A-0260, A-0263,
A-0266, A-0269, A-0329, A-338, A-0340, A-0524, A-0542, A-0551, A-0555, A-0557, A
0571, A-0573, A-0574, A-0577, A-0578, A-0587, A-0588, A-0593, A-0594, A-0597, A-0598,
A-0600, A-0613, A-0614, A-0618, A-0624, A-0634, A-0636, A-0637, A-0638, A-0639, A
0645, A-0649, A-0654, A-0655, A-0659, A-0663, A-0670, A-0671, A-0688, A-0692, A
0693, A-0697, A-0701, A-0709, A-0875, A-0906, A-0907, A-0908, A-0909, A-0911, A
1067, A-1077, A-1097, A-1117, A-1136, A-1141, A-1145, A-1151, A-1155, A-1156, A-
1162, A-1164, A-1980, A-2182, A-2384, A-2600, A-2990, A-3192, A-3812, A-4404, A
4606, A-5414, A-7030, A-7838, A-8646, A-9993, A-9994,B-0003, B-0018, B-0027, B-0090,
B-0095,B-0099,B-0100,B-0107,B-0165,B-0199,B-0205,B-0290,B-0296,B-0367,B
0456, B-0457,B-0458, C-0001, C-0002, C-0008, C-0020, C-0021, C-0023, C-0047, C-0086,
C-0134, C-0137, C-0144, C-0145, C-0152, C-0176, C-0179, C-0185, C-0186, C-0189, C
0198, C-0239, C-0263, C-0269, C-0329, C-0340, C-0520, C-0555, C-0557, C-0561, C
0563, C-0571, C-0573, C-0587, C-0588, C-0594, C-0597, C-0598, C-0600, C-0614, C-0624,
C-0629, C-0634, C-0637, C-0638, C-0656, C-0663, C-0907, C-0910, C-1067, C-1097, C
1145, C-1153, C-1162, C-1165, D-0035, D-0098, D-0099, D-0103, D-0107, D-0108, D-0207,
D-0309, D-0466, E-0002, E-0003, E-0006, E-0008, E-0020, E-0023, E-0041, E-0047, E-0086,
E-0119, E-0125,E-0128, E-0134,E-0137, E-0176, E-0177, E-0179,E-0263,E-0329,E-0340,
E-0518, E-0557,E-0561, E-0563,E-0571, E-0573, E-0587, E-0588,E-0593,E-0594,E-0597,
E-0598, E-0600,E-0609, E-0613,E-0614, E-0618, E-0624, E-0633,E-0644,E-0652,E
0653, E-0663, E-0693,E-0733,E-0907, E-0908,E-1067,E-1076,E-1077, E-1117, E
1148, E-1152,F-0012,F-0108,F-0207,F-0295,F-0301,F-0309,F-0464,F-0466
[0692] (Test example 2) Helicoverpa armigera killing test
The water-dispersible powder prepared in accordance with Formulation example
2 was diluted in water so that the concentration of the active ingredient was 500 ppm. A
cabbage leaf was dipped in this liquid agent, and air-dried, and then put into a plastic cup.
Five newly hatched larvae of Helicoverpa armigera were released in the cup, and the cup was
lidded. Then, the cup was placed in a thermostatic chamber at 25°C, and the number of dead
insects was examined after 6 days, and the insect mortality was determined by the calculation
formula of numerical formula 1. The test was conducted in duplicate.
[0693] The compounds showing an insect mortality of 50% or more in this
test are as follows.
A-0002, A-0008, A-0014, A-0020, A-0023, A-0029, A-0086, A-0103, A-0128, A-0137, A
0145, A-0148, A-0152, A-0179, A-0183, A-0188, A-0242, A-0263, A-0266, A-0329, A
0338, A-0340, A-0512, A-0524, A-0542, A-0551, A-0553, A-0555, A-0561, A-0574, A-
0583, A-0587, A-0588, A-0591, A-0593, A-0594, A-0597, A-0608, A-0614, A-0633, A-0634,
A-0638, A-0639, A-0644, A-0645, A-0653, A-0654, A-0655, A-0659, A-0660, A-0671, A
0688, A-0689, A-0691, A-0692, A-0693, A-0705, A-0709, A-0713, A-0906, A-0907, A
0908, A-0909, A-0910, A-0911, A-0912, A-0913, A-1076, A-1117, A-1140, A- 141, A
1145, A- 146, A- 148, A-1151, A-1153, A-1158, A- 162, A-1163, A-1164, A-1 165, A
1166, A-2182, A-2384, A-2586, A-2600, A-2990, A-6020, A-7838, A-9480, A-9993, A
9994, B-0004, B-0027, B-0090, B-0091, B-0095, B-0099, B-0100, B-0165, B-0199, B-0287,
B-0290, B-0367, B-0454,B-0455,B-0457, C-0004, C-0008, C-0021, C-0022, C-0041, C
0046, C-0086, C-0120, C-0125, C-0134, C-0137, C-0147, C-0179, C-0189, C-0227, C
0239, C-0263, C-0266, C-0269, C-0320, C-0329, C-0340, C-0512, C-0518, C-0553, C
0557, C-0561, C-0563, C-0573, C-0574, C-0577, C-0578, C-0587, C-0588, C-0594, C
0597, C-0598, C-0600, C-0608, C-0614, C-0633, C-0636, C-0637, C-0653, C-0656, C
0659, C-0660, C-0689, C-0692, C-0705, C-0906, C-0907, C-0908, C-0911, C-117, C
1140, C-1141, C-1162, C-1163, C-i165, D-0003, D-0004, D-0012, D-0035, D-0099, D-0107,
D-0108, D-0115, D-0207, D-0295, D-0301, D-0375, D-0464, E-0006, E-0008, E-0047, E
0086, E-0119, E-0121,E-0128,E-0148, E-0177,E-0263,E-0329,E-0521, E-0542, E-0561,
E-0563, E-0571,E-0573, E-0587,E-0588, E-0594, E-0597, E-0600,E-0614,E-0633,E
0639, E-0644, E-0659,E-0660,E-0688, E-0692,E-0693,E-0705,E-0733, E-0906, E-0907,
E-0908, E-0911,E-0912, E-1076,E-1117, E-1160,F-0003,F-0012,F-0017,F-0099,F-0108,
F-0207,F-0301,F-0375,F-0461,F-0466
[0694] (Test example 3) Aphis gossypii killing test
The water-dispersible powder prepared in accordance with Formulation example
2 was diluted in water so that the concentration of the active ingredient was 500 ppm. A
nursery plant of cucumber preliminarily inoculated with nymphs of Aphis gossypii was
dipped in this liquid agent, and air-dried. The nursery plant of cucumber after the treatment
was placed in a thermostatic chamber at 25°C, and the number of live insects was counted
after 3 days, and the insect mortality was determined by the calculation formula of numerical
formula 1. The test was conducted singly.
[0695] The compounds showing an insect mortality of 50% or more in this
test are as follows.
A-0001, A-0002, A-0004, A-0005, A-0006, A-0007, A-0008, A-0014, A-0020, A-0021, A
0022, A-0023, A-0025, A-0029, A-0044, A-0045, A-0046, A-0047, A-0059, A-0086, A
0101, A-0103, A-0119, A-0120, A-0121, A-0122, A-0123, A-0124, A-0143, A-0144, A-0145,
A-0146, A-0147, A-0148, A-0152, A-0176, A-0177, A-0179, A-0182, A-0183, A-0185, A
0186, A-0189, A-0260, A-0263, A-0266, A-0269, A-0320, A-0340, A-0347, A-0512, A
0524, A-0550, A-0555, A-0557, A-0561, A-0563, A-0571, A-0573, A-0574, A-0577, A-0578,
A-0582, A-0583, A-0591, A-0593, A-0594, A-0597, A-0598, A-0603, A-0609, A-0613, A
0614, A-0618, A-0634, A-0636, A-0637, A-0639, A-0644, A-0652, A-0653, A-0654, A
0655, A-0656, A-0659, A-0660, A-0663, A-0665, A-0670, A-0688, A-0689, A-0691, A
0692, A-0693, A-0697, A-0701, A-0705, A-0709, A-0712, A-0713, A-0875, A-0906, A-0907,
A-0908, A-0909, A-0913, A-1067, A-1077, A-1102, A-1117, A-1 134, A-1 140, A-1141, A
1145, A-i 146, A-i 147, A-i152, A-i157, A-i158, A-i 160, A-i161, A-i162, A-i 163, A
1165, A-1166, A-2182, A-2586, A-2600, A-3596, A-3798, A-3812, A-4202, A-4404, A
4606, A-4808, A-5414, A-5616, A-6020, A-6022, A-7434, A-7636, A-7838, A-8040, A
8862, A-9993, A-9994, B-0001, B-0002, B-0003, B-0004, B-0009, B-0027, B-0091, B-0095,
B-0099,B-0107,B-0290,B-0293,B-0301,B-0367,B-0389,B-0453,B-0455,C-0001,C
0002, C-0003, C-0006, C-0007, C-0020, C-0021, C-0025, C-0044, C-0045, C-0047, C-0119,
C-0122, C-0125, C-0128, C-0134, C-0137, C-0145, C-0176, C-0177, C-0183, C-0186, C
0189, C-0227, C-0239, C-0320, C-0553, C-0557, C-0561, C-0574, C-0578, C-0594, C-0600,
C-0637, C-0638, C-0639, C-0653, C-0655, C-0660, C-0697, C-0907, C-0910, C-0911, C
1077,C-1117,C-1141,C-1162, D-0002,D-0003,D-0005,D-0008,D-0012,D-0035,D-0103,
D-0107, D-0108, D-0115, D-0207, D-0213, D-0301, D-0375, D-0463, D-0464, E-0023, E
0121, E-0124, E-0128,E-0269,E-0609, E-0656,E-0693,E-1067,F-0003
[0696] (Test example 4) Nilaparvata lugens killing activity test
The water-dispersible powder prepared in accordance with Formulation example
2 was diluted in water so that the concentration of the active ingredient was 500 ppm. Paddy was dipped in this liquid agent, and then put into a plastic cup. Ten second instar larvae of
Nilaparvata lugens were released in the plastic cup, and the cup was lidded, and placed in a
thermostatic chamber at 25°C. After 6 days, the number of live insects was counted, and the
insect mortality was determined by the calculation formula of numerical formula 1. The test
was conducted singly.
[0697] The compounds showing an insect mortality of 50% or more in this
test are as follows.
A-0002, A-0003, A-0004, A-0005, A-0007, A-0008, A-0014, A-0020, A-0021, A-0022, A
0023, A-0025, A-0041, A-0045, A-0046, A-0047, A-0059, A-0086, A-0101, A-0119, A-0120,
A-0121, A-0122, A-0123, A-0124, A-0125, A-0128, A-0134, A-0145, A-0146, A-0147, A
0148, A-0152, A-0176, A-0177, A-0179, A-0182, A-0183, A-0185, A-0186, A-0188, A-0189,
A-0198, A-0227, A-0239, A-0242, A-0260, A-0263, A-0266, A-0269, A-0320, A-0329, A
0340, A-0347, A-0548, A-0550, A-0551, A-0555, A-0557, A-0561, A-0563, A-0571, A-0577,
A-0578, A-0583, A-0587, A-0588, A-0591, A-0593, A-0594, A-0597, A-0598, A-0600, A
0603, A-0609, A-0613, A-0614, A-0618, A-0624, A-0629, A-0633, A-0634, A-0636, A-0637,
A-0638, A-0639, A-0644, A-0645, A-0653, A-0654, A-0655, A-0656, A-0659, A-0660, A
0663, A-0664, A-0665, A-0670, A-0671, A-0688, A-0689, A-0692, A-0693, A-0697, A
0701, A-0705, A-0709, A-0712, A-0713, A-0733, A-0907, A-0910, A-1067, A-1076, A
1077, A-1097, A-1102, A-1117, A-1134, A-1136, A-i 140, A-1145, A-1146, A- 147, A
1148, A-1151, A-1153, A-1154, A-1155, A-1156, A-1158, A-1159, A-1161, A-1 162, A
1163, A-1164, A-1166, A-1980, A-2182, A-2384, A-2586, A-2600, A-2788, A-2990, A
3192, A-3596, A-3798, A-3812, A-4000, A-4202, A-4404, A-4808, A-5414, A-5616, A
6020, A-6222, A-6424, A-7030, A-7232, A-7434, A-7636, A-7838, A-8040, A-8242, A
8444, A-8646, A-8862, A-9435, A-9993, A-9994, B-0001, B-0004, B-0018, B-0027, B-0090,
B-0091,B-0095,B-0099,B-0100,B-0107,B-0165,B-0205,B-0287,B-0290,B-0296,B
0301, B-0389, B-0454, B-0455, B-0456, B-0457, B-0458, B-0459, C-0001, C-0002, C-0021,
C-0022, C-0023, C-0025, C-0041, C-0044, C-0047, C-0086, C-0119, C-0120, C-0121, C
0123, C-0124, C-0125, C-0128, C-0134, C-0137, C-0145, C-0147, C-0152, C-0176, C-0177,
C-0179, C-0185, C-0186, C-0189, C-0227, C-0239, C-0263, C-0269, C-0320, C-0340, C
0549, C-0557, C-0561, C-0571, C-0574, C-0577, C-0578, C-0587, C-0588, C-0591, C-0593,
C-0594, C-0597, C-0598, C-0600, C-0614, C-0624, C-0633, C-0636, C-0637, C-0638, C
0639, C-0653, C-0665, C-0656, C-0660, C-0663, C-0665, C-0689, C-0692, C-0697, C
0705, C-0712, C-0912, C-1067, C-1077, C-1097,C-1102, C- 1134, C- 1140, C- 1141, C
1145, C-1152, C-1153, C-1162, C-1163, C-1165, D-0005, D-0012, D-0017, D-0035,D-0098,
D-0099, D-0103, D-0107, D-0213, D-0295, D-0375, D-0462, D-0463, D-0464, D-0466, E
0044, E-0086, E-0125,E-0134,E-0148, E-0152,E-0177,E-0179,E-0227, E-0266, E-0329,
E-0521, E-0555,E-0578, E-0587,E-0588, E-0600, E-0614, E-0618,E-0629,E-0633,E
0660, E-0693, E-0908,E-1077,F-0003,F-0012, F-0099,F-0295, F-0462
[0698] The present invention provides a novel compound having excellent
insecticide activity, and is useful in pesticide fields and agricultural fields, and has industrial
applicability.

Claims (13)

WHAT IS CLAIMED IS:
1. A pyrazole derivative represented by general formula [I] or an
agriculturally acceptable salt thereof
[Chemical formula 1]
R3 R2 /N A NR77 dR R4 N6 N N- (O), R1 R 5
[1] wherein,
p represents an integer of 0 or 1,
R 1, R 2, R 3, R4, and R' each independently represent a hydrogen atom, halogen
atom, C 1 -C 6 alkyl group, hydroxy group, C1-C6 haloalkyl group, CI-C6 alkoxy group, CI-C6
haloalkoxy group, C 3-C 6 cycloalkyl group, C1 -C 6 alkylthio group, C1 -C 6 alkylsulfinyl group,
Cl-C6 alkylsulfonyl group, amino group, mono(C1-C6 alkyl)amino group, di(Ci-C
alkyl)amino group, cyano group, or nitro group,
A represents an oxygen atom or sulfur atom,
Q represents a halogen atom, or C6 -C 10 aryl group that is unsubstituted or substituted with (R8)m, or heteroaryl group that is unsubstituted or substituted with (R)m,
R 6 and R7 each independently represent a hydrogen atom, CI-C6 alkyl group, C 3
C6 cycloalkyl group, C3-C6 cycloalkyl C1-C6 alkyl group, C2-C7 alkynyl group, C2-C6
alkenyl group, hydroxy group, CI-C6 alkoxy group, CI-C6 alkoxy CI-C6 alkyl group, C-C6
haloalkyl group, 2-tetrahydrofuranyl group, 3-tetrahydrofuranyl group, 2-tetrahydropyranyl
group, 4-tetrahydropyranyl group, cyano CI-C6 alkyl group, cyano C 3-C 6 cycloalkyl group,
hydroxy C1-C6 alkyl group, formyl group, amino group, mono(CI-C alkyl)amino group,
di(CI-C6 alkyl)amino group, C1 -C 6 alkylcarbonyl group, CI-C6 alkoxy C-C6 alkylcarbonyl
group, C3-C6 cycloalkylcarbonyl group, C3-C6 cycloalkyl CI-C6 alkylcarbonyl group, Ci-C alkoxycarbonyl group, carbamoyl group, mono(C1-C6 alkyl)aminocarbonyl group, di(CI-C6 alkyl)aminocarbonyl group, phenylcarbonyl group that is unsubstituted or substituted with
(R9),, C 7-CI aralkylcarbonyl group that is unsubstituted or substituted with (R 9)n,
pyridylcarbonyl group that is unsubstituted or substituted with (R9)n, pyrazolylcarbonyl group
that is unsubstituted or substituted with (R9)n, pyridine-2-ylmethyl group, pyridine-3
ylmethyl group, (CI-C6 alkyl)thiocarbonyl group, (CI-C 6 alkoxy)thiocarbonyl group,
thiocarbamoyl group, mono(CI-C6 alkyl)aminothiocarbonyl group, di(CI-C6
alkyl)aminothiocarbonyl group, C 1-C 6 alkylsulfonyl group, sulfamoyl group, mono(CI-C6
alkyl)aminosulfonyl group, di(CI-C6 alkyl)aminosulfonyl group, R 10R11 N-CI-C6 alkyl group,
C1-C6 alkoxycarbonyl C1-C6 alkyl group, aminocarbonyl C1-C6 alkyl group, mono(C1-C
alkyl)aminocarbonyl C 1-C 6 alkyl group, mono(C 3-C 6 cycloalkyl)aminocarbonyl CI-C6 alkyl
group, mono(C1-C6 haloalkyl)aminocarbonyl C1-C6 alkyl group, di(C-C
alkyl)aminocarbonyl C 1-C 6 alkyl group, hydroxyimino group, C1 -C 6 alkoxyimino group,
hydroxyimino CI-C 6 alkyl group, or Ci-C6 alkoxyimino Ci-C6 alkyl group, R 6 and R7 may
together form =CR1 2N(R 3)R 4 or =CR12OR", and further, R 6 and R 7 may form together with
carbon atoms bound thereto, a 3 to 6-membered carbon ring, or a 3 to 6-membered hetero ring
having 1 to 4 hetero atoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom,
the hetero ring may be substituted a halogen atom, cyano group, nitro group, CI-C6 alkyl
group, CI-C6 alkoxy group, CI-C 6 haloalkyl group, or oxo group,
R 8 represents a hydrogen atom, halogen atom, hydroxy group, thiol group, CI-C
alkyl group, C1-C6 haloalkyl group, C 3-C 6 cycloalkyl group, C3-C 6 cycloalkyl CI-C6 alkyl
group, C3-C6 cycloalkyl C2-C6 alkynyl group, C3-C6 halocycloalkyl group, C3-C6
halocycloalkyl Ci-C 6 alkyl group, C 2 -C 6 alkenyl group, C 2 -C haloalkenyl group, C2 -C 7
alkynyl group, C2-C6 haloalkynyl group, CI-C6 alkoxy group, CI-C6 haloalkoxy group, C3
C 6 cycloalkoxy group, oxirane-2-yl group, mono(oxirane-2-yl)Ci-C 3 alkyl group, C3-C 6
halocycloalkoxy group, Ci-C6 alkylthio group, Ci-C 6 alkylsulfinyl group, Ci-C 6
alkylsulfonyl group, C 3-C 6 cycloalkylthio group, C 3-C 6 cycloalkylsulfmyl group, C 3-C 6
cycloalkylsulfonyl group, CI-C6 haloalkylthio group, Ci-C6 haloalkylsulfinyl group, C-C haloalkylsulfonyl group, formyl group, C1-C6 alkylcarbonyl group, C1-C haloalkylcarbonyl group, Ci-C6 alkoxycarbonyl group, aminocarbonyl group, mono(Ci-C alkyl)aminocarbonyl group, di(C1-C 6 alkyl)aminocarbonyl group, amino C1-C6 alkyl group, mono(C1-C alkyl)amino Ci-C6 alkyl group, di(Ci-C6 alkyl)amino Ci-C6 alkyl group, tri(Ci-C6 alkyl)silyloxy C1-C 6 alkyl group, C1-C6 alkylcarbonyl C1-C 6 alkyl group, C1
C 6 alkylcarbonyloxy Ci-C 6 alkyl group, Ci-C6 haloalkylcarbonyl C1-C 6 alkyl group, C1-C6
alkoxycarbonyl C1-C 6 alkyl group, hydroxy C1-C 6 alkyl group, C1-C6 alkoxy C1-C6 alkyl
group, C1-C 6 haloalkoxy C1-C 6 alkyl group, C1-C6 alkoxy C1-C6 haloalkyl group, C1-C
haloalkoxy C1-C 6 haloalkyl group, formyloxy group, C1-C6 alkylcarbonyloxy group, C1-C6
haloalkylcarbonyloxy group, aminocarbonyloxy group, mono(Ci-C alkyl)aminocarbonyloxy
group, di(C1-C6 alkyl)aminocarbonyloxy group, aminocarbonyloxy C1-C6 alkyl group,
mono(Ci-C6 alkyl)aminocarbonyloxy Ci-C6 alkyl group, di(Ci-C6 alkyl)aminocarbonyloxy
Ci-C 6 alkyl group, Ci-C6 alkoxycarbonyloxy group, Ci-C6 alkoxycarbonyloxy Ci-C6 alkyl
group, Ci-C6 alkylsulfonyloxy group, C-C6 haloalkylsulfonyloxy group, C-C6 alkylthio
Ci-C 6 alkyl group, Ci-C6 alkylsulfinyl Ci-C6 alkyl group, C-C6 alkylsulfonyl C-C6 alkyl
group, Ci-C6 haloalkylthio Ci-C6 alkyl group, Ci-C6 haloalkylsulfinyl Ci-C6 alkyl group,
Ci-C6 haloalkylsulfonyl Ci-C6 alkyl group, C3-C6 cycloalkyl Ci-C6 alkoxy group, C3-C6
halocycloalkyl Ci-C6 alkoxy group, C 3 -C 6 cycloalkyl C-C6 alkylthio group, C 3 -C
cycloalkyl Ci-C6 alkylsulfinyl group, C 3 -C 6 cycloalkyl C-C6 alkylsulfonyl group, C 3 -C
halocycloalkyl Ci-C6 alkylthio group, C3-C6 halocycloalkyl Ci-C6 alkylsulfinyl group, C3
C6 halocycloalkyl Ci-C6 alkylsulfonyl group, phenyl group that is unsubstituted or substituted
with (R9)n, phenoxy group that is unsubstituted or substituted with (R9)n, benzyl group that is
unsubstituted or substituted with (R9), benzyloxy group that is unsubstituted or substituted
with (R9)n, amino group, mono(Ci-C6 alkyl)amino group, di(Ci-C6 alkyl)amino group,
carboxy group, 1,3-dioxolane-2-yl group, 1,3-dioxane-2-yl group, 1H-imidazole-2-yl group,
thiazole-2-yl group, oxazole-2-yl group, (hydroxyimino)methyl group,
(methyloxyimino)methyl group, isoxazole-3-yl, 4,5-dihydro-3-isoxazolyl group, cyano group,
or nitro group, and further, neighboring two R8 s may form, together with a carbon atom bound to each R8, a 4 to 8-membered carbon ring, or a 4 to 8-membered hetero ring having 1 to 4 hetero atoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, the carbon ring or hetero ring formed at this time may be substituted with one or more chemically acceptable substituents selected from a halogen atom, cyano group, nitro group, C1-C6 alkyl group, C1-C 6 haloalkyl group, C1-C6 alkoxy group, C1-C6 haloalkoxy group, or oxo group,
R9 represents a halogen atom, C 1 -C 6 alkyl group, C1-C6 haloalkyl group, C1-C6
alkoxy group, C1-C 6 haloalkoxy group, C1-C6 alkylthio group, C1-C alkylsulfinyl group,
Ci-C 6 alkylsulfonyl group, Ci-C6 haloalkylthio group, C1-C6 haloalkylsulfinyl group, C1-C6
haloalkylsulfonyl group, amino group, mono(C1-C6 alkyl)amino group, di(C1-C6 alkyl)amino
group, cyano group, or nitro group,
R 10 and R 1 e ach independently represent a hydrogen atom, C1-C 6 alkyl group,
Ci-C6 haloalkyl group, or C3-C6 cycloalkyl group, and further, R10 and R 1 may form,
together with carbon atoms bound thereto, a 3 to 6-membered ring,
R 12 represents a hydrogen atom, C1-C6 alkyl group, or C 3 -C cycloalkyl group,
R 1 3 and R 14 each independently represent a hydrogen atom, Ci-C6 alkyl group,
Ci-C6 haloalkyl group, C3-C6 cycloalkyl group, or Ci-C6 alkoxy group, and further, R1 3 and
R14 may form, together with carbon atoms bound thereto, a 3 to 6-membered carbon ring, or a
3 to 6-membered hetero ring having 1 to 4 hetero atoms selected from an oxygen atom, a
sulfur atom, and a nitrogen atom,
R r e presents a Ci-C6 alkyl group,
m represents a number of chemically acceptable Rs and is an integer of 0 to 7,
R 8s may be the same or different from each other when m is 2 or more,
n represents a number of chemically acceptable R9 s and is an integer of 0 to 5,
and R9s may be the same or different from each other when n is 2 or more.
2. A pyrazole derivative represented by general formula [II] or an
agriculturally acceptable salt thereof
[Chemical formula 2]
R3 R2 O 1R 1
R4 N
(O)p R 1 R5
wherein,
p represents an integer of 0 or 1,
R 1, R 2, R 3, R4, and R' each independently represent a hydrogen atom, halogen
atom, C1-C6 alkyl group, hydroxy group, C1-C6 haloalkyl group, CI-C6 alkoxy group, C-C
haloalkoxy group, C 3-C 6 cycloalkyl group, C1 -C 6 alkylthio group, C1 -C 6 alkylsulfinyl group,
Ci-C6 alkylsulfonyl group, amino group, mono(C1-C6 alkyl)amino group, di(Ci-C6
alkyl)amino group, cyano group, or nitro group,
R 16 represents a hydrogen atom or C1 -C 6 alkyl group,
Q'represents a halogen atom, C1 -C alkylsulfonyloxy group, C1 -C
haloalkylsulfonyloxy group, di(Ci-C6 alkyl)sulfamoyloxy group, phenylsulfonyloxy group
that is unsubstituted or substituted with (R9)n, C6-Cio aryl group that is unsubstituted or
substituted with (R')m, or heteroaryl group that is unsubstituted or substituted with (R),.
R 8 represents a hydrogen atom, halogen atom, hydroxy group, thiol group, C1 -C
alkyl group, C1-C6 haloalkyl group, C 3-C 6 cycloalkyl group, C3-C6 cycloalkyl CI-C6 alkyl
group, C3-C 6 cycloalkyl C 2 -C 6 alkynyl group, C 3-C 6 halocycloalkyl group, C 3-C 6
halocycloalkyl CI-C6 alkyl group, C2-C6 alkenyl group, C2-C6 haloalkenyl group, C2-C7
alkynyl group, C 2 -C 6 haloalkynyl group, CI-C6 alkoxy group, CI-C6 haloalkoxy group, C 3
C6 cycloalkoxy group, oxirane-2-yl group, mono(oxirane-2-yl)Ci-C3 alkyl group, C3-C
halocycloalkoxy group, C1 -C 6 alkylthio group, C1 -C 6 alkylsulfinyl group, C1 -C
alkylsulfonyl group, C 3-C 6 cycloalkylthio group, C 3-C 6 cycloalkylsulfmyl group, C 3-C 6
cycloalkylsulfonyl group, C1-C 6 haloalkylthio group, C1 -C 6 haloalkylsulfinyl group, C1 -C
haloalkylsulfonyl group, formyl group, Ci-C6 alkylcarbonyl group, C-C haloalkylcarbonyl group, C1-C6 alkoxycarbonyl group, aminocarbonyl group, mono(C1-C alkyl)aminocarbonyl group, di(Ci-C6 alkyl)aminocarbonyl group, amino Ci-C6 alkyl group, mono(Ci-C alkyl)amino C1-C 6 alkyl group, di(C1-C6 alkyl)amino C1-C6 alkyl group, tri(C1-C6 alkyl)silyloxy Ci-C6 alkyl group, Ci-C6 alkylcarbonyl Ci-C6 alkyl group, Ci-C alkylcarbonyloxy Ci-C 6 alkyl group, Ci-C6 haloalkylcarbonyl C1-C 6 alkyl group, C1-C6 alkoxycarbonyl C1-C 6 alkyl group, hydroxy C1-C 6 alkyl group, C1-C6 alkoxy C1-C6 alkyl group, C1-C 6 haloalkoxy C1-C 6 alkyl group, C1-C6 alkoxy C1-C6 haloalkyl group, C1-C6 haloalkoxy C1-C 6 haloalkyl group, formyloxy group, C1-C6 alkylcarbonyloxy group, C-C6 haloalkylcarbonyloxy group, aminocarbonyloxy group, mono(C-C6 alkyl)aminocarbonyloxy group, di(Ci-C6 alkyl)aminocarbonyloxy group, aminocarbonyloxy Ci-C6 alkyl group, mono(Ci-C 6 alkyl)aminocarbonyloxy Ci-C 6 alkyl group, di(C-C6 alkyl)aminocarbonyloxy
Ci-C6 alkyl group, Ci-C6 alkoxycarbonyloxy group, Ci-C6 alkoxycarbonyloxy Ci-C6 alkyl
group, Ci-C6 alkylsulfonyloxy group, C-C6 haloalkylsulfonyloxy group, C-C6 alkylthio
Ci-C6 alkyl group, Ci-C6 alkylsulfinyl Ci-C6 alkyl group, Ci-C6 alkylsulfonyl Ci-C6 alkyl
group, Ci-C6 haloalkylthio Ci-C 6 alkyl group, C-C6 haloalkylsulfinyl C-C6 alkyl group,
Ci-C6 haloalkylsulfonyl Ci-C6 alkyl group, C3-C6 cycloalkyl Ci-C6 alkoxy group, C3-C6
halocycloalkyl Ci-C6 alkoxy group, C3-C6 cycloalkyl Ci-C6 alkylthio group, C3-C6
cycloalkyl Ci-C6 alkylsulfinyl group, C 3 -C 6 cycloalkyl C-C6 alkylsulfonyl group, C 3 -C
halocycloalkyl Ci-C 6 alkylthio group, C 3 -C 6 halocycloalkyl Ci-C 6 alkylsulfinyl group, C 3
C6 halocycloalkyl Ci-C6 alkylsulfonyl group, phenyl group that is unsubstituted or substituted
with (R9), phenoxy group that is unsubstituted or substituted with (R9), benzyl group that is
unsubstituted or substituted with (R9)n, benzyloxy group that is unsubstituted or substituted
with (R9 ), amino group, mono(Ci-C6 alkyl)amino group, di(Ci-C6 alkyl)amino group,
carboxy group, 1,3-dioxolane-2-yl group, 1,3-dioxane-2-yl group, 1H-imidazole-2-yl group,
thiazole-2-yl group, oxazole-2-yl group, (hydroxyimino)methyl group,
(methyloxyimino)methyl group, isoxazole-3-yl, 4,5-dihydro-3-isoxazolyl group, cyano group,
or nitro group, and further, neighboring two R8 s may form, together with a carbon atom
bound to each R8, a 4 to 8-membered carbon ring, or a 4 to 8-membered hetero ring having 1 to 4 hetero atoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, the carbon ring or hetero ring formed at this time may be substituted with one or more chemically acceptable substituents selected from a halogen atom, cyano group, nitro group, C1-C6 alkyl group, Ci-C6 haloalkyl group, Ci-C6 alkoxy group, Ci-C6 haloalkoxy group, or oxo group,
R9 represents a halogen atom, C1-C6 alkyl group, C1-C haloalkyl group, C1-C
alkoxy group, C1-C6 haloalkoxy group, C1-C6 alkylthio group, C1-C alkylsulfinyl group,
Ci-C 6 alkylsulfonyl group, Ci-C6 haloalkylthio group, C1-C6 haloalkylsulfinyl group, C1-C6
haloalkylsulfonyl group, amino group, mono(C1-C6 alkyl)amino group, di(C1-C6 alkyl)amino
group, cyano group, or nitro group,
m represents a number of chemically acceptable Rs and is an integer of 0 to 7,
R 8s may be the same or different from each other when m is 2 or more,
n represents a number of chemically acceptable R9 s and is an integer of 0 to 5,
and R9s may be the same or different from each other when n is 2 or more.
3. A agrochemical composition comprising the pyrazole derivative or an
agriculturally acceptable salt thereof according to claim 1 or 2 as an active ingredient.
4. The agrochemical composition according to claim 3, wherein the
agrochemical composition further comprises a surfactant.
5. A pest control agent comprising the pyrazole derivative or an
agriculturally acceptable salt thereof according to claim 1 or 2 as an active ingredient.
6. The pest control agent according to claim 5 that is an insecticide.
7. The pest control agent according to claim 5 having a control effect on a
pest in a dry field or a paddy field where a farming or gardening plant is cultured.
8. The pest control agent according to claim 7, wherein the farming or
gardening plant is a plant provided with tolerance by a breeding method or a gene
recombination technique.
9. A method for controlling a pest comprising using an active ingredient
amount of the pyrazole derivative or an agriculturally acceptable salt thereof according to
claim 1 or 2.
10. A method for controlling a pest by letting a agrochemical composition
comprising the pyrazole derivative or an agriculturally acceptable salt thereof according to
claim 1 or 2 as an active ingredient act on a farming or gardening crop or a place where the
farming or gardening crop is to be grown or being grown, at once or in batch.
11. The method for controlling a pest according to claim 9 or 10, wherein the
place where the pest control agent is to be applied is a paddy field, a dry field, a lawn, an
orchard, a non-crop land, a greenhouse, a raising seeding facility, or a plant factory.
12. The method for controlling a pest according to any one of claims 9 to 11,
wherein the pyrazole derivative or an agriculturally acceptable salt thereof is used as an
insecticide.
13. A use method of a pest control agent, using the pest control agent
according to any one of claims 5 to 8 for controlling a pest for a farming or gardening crop.
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